메뉴 건너뛰기




Volumn 116, Issue 11, 2016, Pages 6707-6741

Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors

Author keywords

[No Author keywords available]

Indexed keywords

MODULATORS;

EID: 84974602761     PISSN: 00092665     EISSN: 15206890     Source Type: Journal    
DOI: 10.1021/acs.chemrev.5b00656     Document Type: Review
Times cited : (153)

References (345)
  • 1
    • 77952354490 scopus 로고    scopus 로고
    • Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery
    • Kenakin, T.; Miller, L. J. Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery Pharmacol. Rev. 2010, 62, 265-304 10.1124/pr.108.000992
    • (2010) Pharmacol. Rev. , vol.62 , pp. 265-304
    • Kenakin, T.1    Miller, L.J.2
  • 2
    • 0036490942 scopus 로고    scopus 로고
    • 2002. Allosteric Binding Sites on Cell Surface Receptors: Novel Targets for Drug Discovery
    • Christopoulos, A. 2002. Allosteric Binding Sites on Cell Surface Receptors: Novel Targets for Drug Discovery Nat. Rev. Drug Discovery 2002, 1, 198-210 10.1038/nrd746
    • (2002) Nat. Rev. Drug Discovery , vol.1 , pp. 198-210
    • Christopoulos, A.1
  • 3
    • 69649097791 scopus 로고    scopus 로고
    • 7TM Receptor Allostery: Putting Numbers to Shapeshifting Proteins
    • Kenakin, T. P. 7TM Receptor Allostery: Putting Numbers to Shapeshifting Proteins Trends Pharmacol. Sci. 2009, 30, 460-469 10.1016/j.tips.2009.06.007
    • (2009) Trends Pharmacol. Sci. , vol.30 , pp. 460-469
    • Kenakin, T.P.1
  • 4
    • 84876525643 scopus 로고    scopus 로고
    • 2013. Regulation of G Protein-Coupled Receptors by Allosteric Ligands
    • Lane, R. J.; Abdul-Ridha, A.; Canals, M. 2013. Regulation of G Protein-Coupled Receptors by Allosteric Ligands ACS Chem. Neurosci. 2013, 4, 527-534 10.1021/cn400005t
    • (2013) ACS Chem. Neurosci. , vol.4 , pp. 527-534
    • Lane, R.J.1    Abdul-Ridha, A.2    Canals, M.3
  • 5
    • 50449109973 scopus 로고    scopus 로고
    • Allostery: An Illustrated Definition for the Second Secret of Life
    • Fenton, A. W. Allostery: An Illustrated Definition for the Second Secret of Life Trends Biochem. Sci. 2008, 33, 420-425 10.1016/j.tibs.2008.05.009
    • (2008) Trends Biochem. Sci. , vol.33 , pp. 420-425
    • Fenton, A.W.1
  • 6
    • 58149193205 scopus 로고    scopus 로고
    • Allosteric Modulators of GPCRs as a Novel Approach to Treatment of CNS Disorders
    • Conn, P. J.; Christopoulos, A.; Lindsley, C. W. Allosteric Modulators of GPCRs as a Novel Approach to Treatment of CNS Disorders Nat. Rev. Drug Discovery 2009, 8, 41-54 10.1038/nrd2760
    • (2009) Nat. Rev. Drug Discovery , vol.8 , pp. 41-54
    • Conn, P.J.1    Christopoulos, A.2    Lindsley, C.W.3
  • 7
    • 53449093828 scopus 로고    scopus 로고
    • G-Protein Coupled Receptors: From Classical Modes of Modulation to Allosteric Mechanisms
    • Bridges, T. M.; Lindsley, C. W. G-Protein Coupled Receptors: From Classical Modes of Modulation to Allosteric Mechanisms ACS Chem. Biol. 2008, 3, 530-542 10.1021/cb800116f
    • (2008) ACS Chem. Biol. , vol.3 , pp. 530-542
    • Bridges, T.M.1    Lindsley, C.W.2
  • 8
    • 0036258990 scopus 로고    scopus 로고
    • G Protein-Coupled Receptors Allosterism and Complexing
    • Christopoulos, A.; Kenakin, T. G Protein-Coupled Receptors Allosterism and Complexing Pharmacol. Rev. 2002, 54, 323-374 10.1124/pr.54.2.323
    • (2002) Pharmacol. Rev. , vol.54 , pp. 323-374
    • Christopoulos, A.1    Kenakin, T.2
  • 9
    • 84907457165 scopus 로고    scopus 로고
    • 2013 Philip S. Portoghese Medicinal Chemistry Lectureship: Drug Discovery Targeting Allosteric Sites
    • Lindsley, C. W. 2013 Philip S. Portoghese Medicinal Chemistry Lectureship: Drug Discovery Targeting Allosteric Sites J. Med. Chem. 2014, 57, 7485-7498 10.1021/jm5011786
    • (2014) J. Med. Chem. , vol.57 , pp. 7485-7498
    • Lindsley, C.W.1
  • 10
    • 84906827756 scopus 로고    scopus 로고
    • Opportunities and Challenges in the Discovery of Allosteric Modulators of GPCRs for the Treatment of CNS Disorders
    • Conn, P. J.; Lindsley, C. W.; Meiler, J.; Niswender, C. M. Opportunities and Challenges in the Discovery of Allosteric Modulators of GPCRs for the Treatment of CNS Disorders Nat. Rev. Drug Discovery 2014, 13, 692-708 10.1038/nrd4308
    • (2014) Nat. Rev. Drug Discovery , vol.13 , pp. 692-708
    • Conn, P.J.1    Lindsley, C.W.2    Meiler, J.3    Niswender, C.M.4
  • 12
    • 84876720539 scopus 로고    scopus 로고
    • Allosteric Modulation for the Treatment of Schizophrenia: Targeting Glutamatergic Networks
    • Menniti, F. S.; Lindsley, C. W.; Conn, P. J.; Pandit, J.; Zagouras, P.; Volkmann, R. A. Allosteric Modulation for the Treatment of Schizophrenia: Targeting Glutamatergic Networks Curr. Top. Med. Chem. 2013, 13, 26-54 10.2174/1568026611313010005
    • (2013) Curr. Top. Med. Chem. , vol.13 , pp. 26-54
    • Menniti, F.S.1    Lindsley, C.W.2    Conn, P.J.3    Pandit, J.4    Zagouras, P.5    Volkmann, R.A.6
  • 13
    • 78651189765 scopus 로고
    • On the Nature of Allosteric Transitions: A Plausible Model
    • Monod, J.; Wyman, J.; Changeux, J.-P. On the Nature of Allosteric Transitions: A Plausible Model J. Mol. Biol. 1965, 12, 88-118 10.1016/S0022-2836(65)80285-6
    • (1965) J. Mol. Biol. , vol.12 , pp. 88-118
    • Monod, J.1    Wyman, J.2    Changeux, J.-P.3
  • 15
    • 42149181885 scopus 로고    scopus 로고
    • Structural Diversity of G Protein-Coupled Receptors and Significance for Drug Discovery
    • Lagerström, M. C.; Schiöth, H. B. Structural Diversity of G Protein-Coupled Receptors and Significance for Drug Discovery Nat. Rev. Drug Discovery 2008, 7, 339-357 10.1038/nrd2518
    • (2008) Nat. Rev. Drug Discovery , vol.7 , pp. 339-357
    • Lagerström, M.C.1    Schiöth, H.B.2
  • 17
    • 84934999252 scopus 로고    scopus 로고
    • 2014 Prescription Medications in the United States: Tremendous Growth, Speciality/Orphan Drug Expansion and CNS Dispensed Prescriptions Continue to Increase
    • Lindsley, C. W. 2014 Prescription Medications in the United States: Tremendous Growth, Speciality/Orphan Drug Expansion and CNS Dispensed Prescriptions Continue to Increase ACS Chem. Neurosci. 2015, 6, 811-812 10.1021/acschemneuro.5b00148
    • (2015) ACS Chem. Neurosci. , vol.6 , pp. 811-812
    • Lindsley, C.W.1
  • 18
    • 84947484341 scopus 로고    scopus 로고
    • New Paradigms in GPCR Drug Discovery
    • Jacobson, K. A. New Paradigms in GPCR Drug Discovery Biochem. Pharmacol. 2015, 98, 541-555 10.1016/j.bcp.2015.08.085
    • (2015) Biochem. Pharmacol. , vol.98 , pp. 541-555
    • Jacobson, K.A.1
  • 19
    • 84920828713 scopus 로고    scopus 로고
    • DREADDs (Designer Receptors Exclusively Activated by Designer Drugs): Chemogenetic Tools with Therapeutic Utility
    • Urban, D. J.; Roth, B. L. DREADDs (Designer Receptors Exclusively Activated by Designer Drugs): Chemogenetic Tools with Therapeutic Utility Annu. Rev. Pharmacol. Toxicol. 2015, 55, 399-417 10.1146/annurev-pharmtox-010814-124803
    • (2015) Annu. Rev. Pharmacol. Toxicol. , vol.55 , pp. 399-417
    • Urban, D.J.1    Roth, B.L.2
  • 21
    • 36849028142 scopus 로고    scopus 로고
    • Calcium Sensing Receptor Activators: Calcimimetics
    • Harrington, P. E.; Fotsch, C. Calcium Sensing Receptor Activators: Calcimimetics Curr. Med. Chem. 2007, 14, 3027-3034 10.2174/092986707782794096
    • (2007) Curr. Med. Chem. , vol.14 , pp. 3027-3034
    • Harrington, P.E.1    Fotsch, C.2
  • 23
    • 84875192840 scopus 로고    scopus 로고
    • MGlu5 Negative Allosteric Modulators: A Patent Review (2010-2012)
    • Emmitte, K. A. mGlu5 Negative Allosteric Modulators: A Patent Review (2010-2012) Expert Opin. Ther. Pat. 2013, 23, 393-408 10.1517/13543776.2013.760544
    • (2013) Expert Opin. Ther. Pat. , vol.23 , pp. 393-408
    • Emmitte, K.A.1
  • 26
    • 84874035617 scopus 로고    scopus 로고
    • 2 Positive Allosteric Modulators for the Treatment of Schizophrenia?
    • 2 Positive Allosteric Modulators for the Treatment of Schizophrenia? ACS Chem. Neurosci. 2013, 4, 211-213 10.1021/cn400023y
    • (2013) ACS Chem. Neurosci. , vol.4 , pp. 211-213
    • Hopkins, C.R.1
  • 27
    • 27844482134 scopus 로고    scopus 로고
    • A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators
    • Rodriguez, A. L.; Nong, Y.; Sekaran, N. K.; Alagille, D.; Tamagnan, G. D.; Conn, P. J. A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators Mol. Pharmacol. 2005, 68, 1793-1802 10.1124/mol.105.016139
    • (2005) Mol. Pharmacol. , vol.68 , pp. 1793-1802
    • Rodriguez, A.L.1    Nong, Y.2    Sekaran, N.K.3    Alagille, D.4    Tamagnan, G.D.5    Conn, P.J.6
  • 33
    • 47149106805 scopus 로고    scopus 로고
    • Synthesis and SAR of a mGluR5 Allosteric Partial Antagonist Lead: Unexpected Modulation of Pharmacology with Slight Structural Modifications to a 5-(Phenylethynyl)pyrimidine Scaffold
    • Sharma, S.; Rodriguez, A.; Conn, P. J.; Lindsley, C. W. Synthesis and SAR of a mGluR5 Allosteric Partial Antagonist Lead: Unexpected Modulation of Pharmacology with Slight Structural Modifications to a 5-(Phenylethynyl)pyrimidine Scaffold Bioorg. Med. Chem. Lett. 2008, 18, 4098-4101 10.1016/j.bmcl.2008.05.091
    • (2008) Bioorg. Med. Chem. Lett. , vol.18 , pp. 4098-4101
    • Sharma, S.1    Rodriguez, A.2    Conn, P.J.3    Lindsley, C.W.4
  • 34
    • 67650729937 scopus 로고    scopus 로고
    • Discovery of Molecular Switches that Modulate Modes of mGluR5 Pharmacology in Vitro and in Vivo Within a Series of Functionalized 5-(Phenylethynyl)pyrimidines
    • Sharma, S.; Kedrowski, J.; Rook, J. M.; Smith, J. M.; Jones, C. K.; Rodriguez, A. L.; Conn, P. J.; Lindsley, C. W. Discovery of Molecular Switches that Modulate Modes of mGluR5 Pharmacology in Vitro and in Vivo Within a Series of Functionalized 5-(Phenylethynyl)pyrimidines J. Med. Chem. 2009, 52, 4103-4106 10.1021/jm900654c
    • (2009) J. Med. Chem. , vol.52 , pp. 4103-4106
    • Sharma, S.1    Kedrowski, J.2    Rook, J.M.3    Smith, J.M.4    Jones, C.K.5    Rodriguez, A.L.6    Conn, P.J.7    Lindsley, C.W.8
  • 35
    • 79953213637 scopus 로고    scopus 로고
    • 'Molecular Switches' on Allosteric Ligands that Modulate Modes of Pharmacology
    • Wood, M. R.; Hopkins, C. R.; Brogan, J. T.; Conn, P. J.; Lindsley, C. W. 'Molecular Switches' on Allosteric Ligands that Modulate Modes of Pharmacology Biochemistry 2011, 50, 2403-2410 10.1021/bi200129s
    • (2011) Biochemistry , vol.50 , pp. 2403-2410
    • Wood, M.R.1    Hopkins, C.R.2    Brogan, J.T.3    Conn, P.J.4    Lindsley, C.W.5
  • 36
    • 78649919580 scopus 로고    scopus 로고
    • Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and in Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity
    • Rodriguez, A. L.; Grier, M. D.; Jones, C. K.; Herman, E. J.; Kane, A. S.; Smith, R. L.; Williams, R.; Zhou, Y.; Marlo, J. E.; Days, E. L. et al. Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and in Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity Mol. Pharm. 2010, 78, 1105-1123 10.1124/mol.110.067207
    • (2010) Mol. Pharm. , vol.78 , pp. 1105-1123
    • Rodriguez, A.L.1    Grier, M.D.2    Jones, C.K.3    Herman, E.J.4    Kane, A.S.5    Smith, R.L.6    Williams, R.7    Zhou, Y.8    Marlo, J.E.9    Days, E.L.10
  • 37
    • 84882784373 scopus 로고    scopus 로고
    • Biotransformation of a Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Contributes to Seizures in Rats Involving a Receptor Agonism-Dependent Mechanism
    • Bridges, T. M.; Rook, J. M.; Noetzel, M. J.; Morrison, R. D.; Zhou, Y.; Gogliotti, R. D.; Vinson, P. N.; Jones, C. K.; Niswender, C. M.; Lindsley, C. W. et al. Biotransformation of a Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Contributes to Seizures in Rats Involving a Receptor Agonism-Dependent Mechanism Drug Metab. Dispos. 2013, 41, 1703-1714 10.1124/dmd.113.052084
    • (2013) Drug Metab. Dispos. , vol.41 , pp. 1703-1714
    • Bridges, T.M.1    Rook, J.M.2    Noetzel, M.J.3    Morrison, R.D.4    Zhou, Y.5    Gogliotti, R.D.6    Vinson, P.N.7    Jones, C.K.8    Niswender, C.M.9    Lindsley, C.W.10
  • 38
    • 34548677767 scopus 로고    scopus 로고
    • Allosteric Modulation of Nicotinic Acetylcholine Receptors
    • Bertrand, D.; Gopalakrishnan, M. Allosteric Modulation of Nicotinic Acetylcholine Receptors Biochem. Pharmacol. 2007, 74, 1155-1163 10.1016/j.bcp.2007.07.011
    • (2007) Biochem. Pharmacol. , vol.74 , pp. 1155-1163
    • Bertrand, D.1    Gopalakrishnan, M.2
  • 39
    • 84904434885 scopus 로고    scopus 로고
    • A Novel Class of Succinimide-Derived Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Provides Insight into a Disconnect in Activity between Rat and Human Receptors
    • Cho, H. P.; Engers, D. W.; Venable, D. F.; Niswender, C. M.; Lindsley, C. W.; Conn, P. J.; Emmitte, K. A.; Rodriguez, A. L. A Novel Class of Succinimide-Derived Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Provides Insight into a Disconnect in Activity Between Rat and Human Receptors ACS Chem. Neurosci. 2014, 5, 597-610 10.1021/cn5000343
    • (2014) ACS Chem. Neurosci. , vol.5 , pp. 597-610
    • Cho, H.P.1    Engers, D.W.2    Venable, D.F.3    Niswender, C.M.4    Lindsley, C.W.5    Conn, P.J.6    Emmitte, K.A.7    Rodriguez, A.L.8
  • 42
    • 84857497773 scopus 로고    scopus 로고
    • Biased Signalling and Allosteric Machines: New Vistas and Challenges for Drug Discovery
    • Kenakin, T. Biased Signalling and Allosteric Machines: New Vistas and Challenges for Drug Discovery Br. J. Pharmacol. 2012, 165, 1659-1669 10.1111/j.1476-5381.2011.01749.x
    • (2012) Br. J. Pharmacol. , vol.165 , pp. 1659-1669
    • Kenakin, T.1
  • 43
    • 84875227396 scopus 로고    scopus 로고
    • Signalling Bias in New Drug Discovery: Detection, Quantification and Therapeutic Impact
    • Kenakin, T.; Christopoulos, A. Signalling Bias in New Drug Discovery: Detection, Quantification and Therapeutic Impact Nat. Rev. Drug Discovery 2013, 12, 205-216 10.1038/nrd3954
    • (2013) Nat. Rev. Drug Discovery , vol.12 , pp. 205-216
    • Kenakin, T.1    Christopoulos, A.2
  • 44
    • 76749144987 scopus 로고    scopus 로고
    • Molecular Mechanisms of Action and in Vivo Validation of an M4Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties
    • Leach, K.; Loiacono, E. I.; Felder, C. C.; McKinzie, D. L.; Mogg, A.; Shaw, D. B.; Sexton, P. M.; Christopoulos, A. Molecular Mechanisms of Action and in Vivo Validation of an M4Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties Neuropsychopharmacology 2010, 35, 855-869 10.1038/npp.2009.194
    • (2010) Neuropsychopharmacology , vol.35 , pp. 855-869
    • Leach, K.1    Loiacono, E.I.2    Felder, C.C.3    McKinzie, D.L.4    Mogg, A.5    Shaw, D.B.6    Sexton, P.M.7    Christopoulos, A.8
  • 45
    • 27744558560 scopus 로고    scopus 로고
    • Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes
    • Zhang, Y.; Rodriguez, A. L.; Conn, P. J. Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes J. Pharmacol. Exp. Ther. 2005, 315, 1212-1219 10.1124/jpet.105.090308
    • (2005) J. Pharmacol. Exp. Ther. , vol.315 , pp. 1212-1219
    • Zhang, Y.1    Rodriguez, A.L.2    Conn, P.J.3
  • 46
    • 49949084014 scopus 로고    scopus 로고
    • Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 1a Differentially Modulate Independent Signaling Pathways in Baby Hamster Kidney Cells
    • Sheffler, D. J.; Conn, P. J. Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 1a Differentially Modulate Independent Signaling Pathways in Baby Hamster Kidney Cells Neuropharmacology 2008, 55, 419-427 10.1016/j.neuropharm.2008.06.047
    • (2008) Neuropharmacology , vol.55 , pp. 419-427
    • Sheffler, D.J.1    Conn, P.J.2
  • 47
    • 84865441831 scopus 로고    scopus 로고
    • Identification of Molecular Phenotypes and Biased Signaling Induced by Naturally Occurring Mutations of the Human Calcium-Sensing Receptor
    • Leach, K.; Wen, A.; Davey, A. E.; Sexton, P. M.; Conigrave, A. D.; Christopoulos, A. Identification of Molecular Phenotypes and Biased Signaling Induced by Naturally Occurring Mutations of the Human Calcium-Sensing Receptor Endocrinology 2012, 153, 4304-4316 10.1210/en.2012-1449
    • (2012) Endocrinology , vol.153 , pp. 4304-4316
    • Leach, K.1    Wen, A.2    Davey, A.E.3    Sexton, P.M.4    Conigrave, A.D.5    Christopoulos, A.6
  • 48
    • 84857386424 scopus 로고    scopus 로고
    • Positive and Negative Allosteric Modulators Promote Biased Signaling at the Calcium-Sensing Receptor
    • Davey, A. E.; Leach, K.; Valant, C.; Conigrave, A. D.; Sexton, P. M.; Christopoulos, A. Positive and Negative Allosteric Modulators Promote Biased Signaling at the Calcium-Sensing Receptor Endocrinology 2012, 153, 1232-1241 10.1210/en.2011-1426
    • (2012) Endocrinology , vol.153 , pp. 1232-1241
    • Davey, A.E.1    Leach, K.2    Valant, C.3    Conigrave, A.D.4    Sexton, P.M.5    Christopoulos, A.6
  • 49
    • 84859479825 scopus 로고    scopus 로고
    • Allosteric Modulator ORG27569 Induces CB1 Cannabinoid Receptor High Affinity Agonist Binding State, Receptor Internalization, and Gi Protein-Independent ERK1/2 Kinase Activation
    • Ahn, K. H.; Mahmoud, M. M.; Kendall, D. A. Allosteric Modulator ORG27569 Induces CB1 Cannabinoid Receptor High Affinity Agonist Binding State, Receptor Internalization, and Gi Protein-Independent ERK1/2 Kinase Activation J. Biol. Chem. 2012, 287, 12070-12082 10.1074/jbc.M111.316463
    • (2012) J. Biol. Chem. , vol.287 , pp. 12070-12082
    • Ahn, K.H.1    Mahmoud, M.M.2    Kendall, D.A.3
  • 57
    • 84904301809 scopus 로고    scopus 로고
    • International Union of Basic and Clinical Pharmacology. XC. Multisite Pharmacology: Recommendations for the Nomenclature of Receptor Allosterism and Allosteric Ligands
    • Christopoulos, A.; Changeux, J. P.; Catterall, W. A.; Fabbro, D.; Burris, T. P.; Cidlowski, J. A.; Olsen, R. W.; Peters, J. A.; Neubig, R. R.; Pin, J. P. et al. International Union of Basic and Clinical Pharmacology. XC. Multisite Pharmacology: Recommendations for the Nomenclature of Receptor Allosterism and Allosteric Ligands Pharmacol. Rev. 2014, 66, 918-947 10.1124/pr.114.008862
    • (2014) Pharmacol. Rev. , vol.66 , pp. 918-947
    • Christopoulos, A.1    Changeux, J.P.2    Catterall, W.A.3    Fabbro, D.4    Burris, T.P.5    Cidlowski, J.A.6    Olsen, R.W.7    Peters, J.A.8    Neubig, R.R.9    Pin, J.P.10
  • 60
  • 61
    • 79960604663 scopus 로고    scopus 로고
    • Structural Determinants of Allosteric Antagonism at Metabotropic Glutamate Receptor 2: Mechanistic Studies with New Potent Negative Allosteric Modulators
    • Lundstrom, L.; Bissantz, C.; Beck, J.; Wettstein, J. G.; Woltering, T. J.; Wichmann, J.; Gatti, S. Structural Determinants of Allosteric Antagonism at Metabotropic Glutamate Receptor 2: Mechanistic Studies with New Potent Negative Allosteric Modulators Br. J. Pharmacol. 2011, 164, 521-527 10.1111/j.1476-5381.2011.01409.x
    • (2011) Br. J. Pharmacol. , vol.164 , pp. 521-527
    • Lundstrom, L.1    Bissantz, C.2    Beck, J.3    Wettstein, J.G.4    Woltering, T.J.5    Wichmann, J.6    Gatti, S.7
  • 66
    • 4143070533 scopus 로고    scopus 로고
    • Differential Kinetic and Spatial Patterns of β-Arrestin and G Protein-mediated ERK Activation by the Angiotensin II Receptor
    • Ahn, S.; Shenoy, S. K.; Wei, H.; Lefkowitz, R. J. Differential Kinetic and Spatial Patterns of β-Arrestin and G Protein-mediated ERK Activation by the Angiotensin II Receptor J. Biol. Chem. 2004, 279, 35518-35525 10.1074/jbc.M405878200
    • (2004) J. Biol. Chem. , vol.279 , pp. 35518-35525
    • Ahn, S.1    Shenoy, S.K.2    Wei, H.3    Lefkowitz, R.J.4
  • 68
    • 84918494690 scopus 로고    scopus 로고
    • Identification of Positive Allosteric Modulators VU0155904 (ML397) and VU0422288 (ML396) Reveals New Insights into the Biology of Metabotropic Glutamate Receptor 7
    • Jalan-Sakrikar, N.; Field, J. R.; Klar, R.; Mattmann, M. E.; Gregory, K. J.; Zamorano, R.; Engers, D. W.; Bollinger, S. R.; Weaver, C. D.; Days, E. L. et al. Identification of Positive Allosteric Modulators VU0155904 (ML397) and VU0422288 (ML396) Reveals New Insights Into the Biology of Metabotropic Glutamate Receptor 7 ACS Chem. Neurosci. 2014, 5, 1221-1237 10.1021/cn500153z
    • (2014) ACS Chem. Neurosci. , vol.5 , pp. 1221-1237
    • Jalan-Sakrikar, N.1    Field, J.R.2    Klar, R.3    Mattmann, M.E.4    Gregory, K.J.5    Zamorano, R.6    Engers, D.W.7    Bollinger, S.R.8    Weaver, C.D.9    Days, E.L.10
  • 70
    • 27144491979 scopus 로고    scopus 로고
    • Analysis of Allosterism in Functional Assays
    • Ehlert, F. J. Analysis of Allosterism in Functional Assays J. Pharmacol. Exp. Ther. 2005, 315, 740-754 10.1124/jpet.105.090886
    • (2005) J. Pharmacol. Exp. Ther. , vol.315 , pp. 740-754
    • Ehlert, F.J.1
  • 71
    • 0033669603 scopus 로고    scopus 로고
    • Modeling the Functional Effects of Allosteric Modulators at Pharmacological Receptors: An Extension of the Two-State Model of Receptor Activation
    • Hall, D. A. Modeling the Functional Effects of Allosteric Modulators at Pharmacological Receptors: An Extension of the Two-State Model of Receptor Activation Mol. Pharmacol. 2000, 58, 1412-1423
    • (2000) Mol. Pharmacol. , vol.58 , pp. 1412-1423
    • Hall, D.A.1
  • 72
    • 3042557815 scopus 로고    scopus 로고
    • Allosteric Modulation of G Protein-Coupled Receptors
    • May, L. T.; Avlani, V. A.; Sexton, P. M.; Christopoulos, A. Allosteric Modulation of G Protein-Coupled Receptors Curr. Pharm. Des. 2004, 10, 2003-2013 10.2174/1381612043384303
    • (2004) Curr. Pharm. Des. , vol.10 , pp. 2003-2013
    • May, L.T.1    Avlani, V.A.2    Sexton, P.M.3    Christopoulos, A.4
  • 73
    • 80052018338 scopus 로고    scopus 로고
    • 3 Muscarinic Receptor by Amiodarone and N-ethylamiodarone: Application of the Four-Ligand Allosteric Two-state model
    • 3 Muscarinic Receptor by Amiodarone and N-ethylamiodarone: Application of the Four-Ligand Allosteric Two-state model Mol. Pharmacol. 2011, 80, 378-388 10.1124/mol.111.072991
    • (2011) Mol. Pharmacol. , vol.80 , pp. 378-388
    • Stahl, E.1    Elmslie, G.2    Ellis, J.3
  • 74
    • 84896383220 scopus 로고    scopus 로고
    • Estimation of Ligand Affinity Constants for Receptor States in Functional Studies Involving the Allosteric Modulation of G Protein-Coupled Receptors: Implications for Ligand Bias
    • Ehlert, F. J.; Griffin, M. T. Estimation of Ligand Affinity Constants for Receptor States in Functional Studies Involving the Allosteric Modulation of G Protein-Coupled Receptors: Implications for Ligand Bias J. Pharmacol. Toxicol. Methods 2014, 69, 253-279 10.1016/j.vascn.2014.01.002
    • (2014) J. Pharmacol. Toxicol. Methods , vol.69 , pp. 253-279
    • Ehlert, F.J.1    Griffin, M.T.2
  • 75
    • 84879339183 scopus 로고    scopus 로고
    • Mechanistic Analysis of the Function of Agonists and Allosteric Modulators: Reconciling Two-State and Operational Models
    • Roche, D.; Gil, D.; Giraldo, J. Mechanistic Analysis of the Function of Agonists and Allosteric Modulators: Reconciling Two-State and Operational Models Br. J. Pharmacol. 2013, 169, 1189-1202 10.1111/bph.12231
    • (2013) Br. J. Pharmacol. , vol.169 , pp. 1189-1202
    • Roche, D.1    Gil, D.2    Giraldo, J.3
  • 76
    • 0021058380 scopus 로고
    • Operational Models of Pharmacological Agonism
    • Black, J. W.; Leff, P. Operational Models of Pharmacological Agonism Proc. R. Soc. London, Ser. B 1983, 220, 141-162 10.1098/rspb.1983.0093
    • (1983) Proc. R. Soc. London, Ser. B , vol.220 , pp. 141-162
    • Black, J.W.1    Leff, P.2
  • 77
    • 34447632041 scopus 로고    scopus 로고
    • Allosteric GPCR Modulators: Taking Advantage of Permissive Receptor Pharmacology
    • Leach, K.; Sexton, P. M.; Christopoulos, A. Allosteric GPCR Modulators: Taking Advantage of Permissive Receptor Pharmacology Trends Pharmacol. Sci. 2007, 28, 382-389 10.1016/j.tips.2007.06.004
    • (2007) Trends Pharmacol. Sci. , vol.28 , pp. 382-389
    • Leach, K.1    Sexton, P.M.2    Christopoulos, A.3
  • 78
    • 84455173446 scopus 로고    scopus 로고
    • Probe Dependence in the Allosteric Modulation of a G Protein-Coupled Receptor: Implications for Detection and Validation of Allosteric Ligand Effects
    • Valant, C.; Felder, C. C.; Sexton, P. M.; Christopoulos, A. Probe Dependence in the Allosteric Modulation of a G Protein-Coupled Receptor: Implications for Detection and Validation of Allosteric Ligand Effects Mol. Pharmacol. 2012, 81, 41-52 10.1124/mol.111.074872
    • (2012) Mol. Pharmacol. , vol.81 , pp. 41-52
    • Valant, C.1    Felder, C.C.2    Sexton, P.M.3    Christopoulos, A.4
  • 79
    • 84923362213 scopus 로고    scopus 로고
    • Ligand-Biased and Probe-Dependent Modulation of Chemokine Receptor CXCR3 Signaling by Negative Allosteric Modulators
    • Bernat, V.; Brox, R.; Heinrich, M. R.; Auberson, Y. P.; Tschammer, N. Ligand-Biased and Probe-Dependent Modulation of Chemokine Receptor CXCR3 Signaling by Negative Allosteric Modulators ChemMedChem 2015, 10, 566-574 10.1002/cmdc.201402507
    • (2015) ChemMedChem , vol.10 , pp. 566-574
    • Bernat, V.1    Brox, R.2    Heinrich, M.R.3    Auberson, Y.P.4    Tschammer, N.5
  • 81
    • 84875426039 scopus 로고    scopus 로고
    • Differential Activation and Modulation of the Glucagon-Like Peptide-1 Receptor by Small Molecule Ligands
    • Wootten, D.; Savage, E. E.; Willard, F. S.; Bueno, A. B.; Sloop, K. W.; Christopoulos, A.; Sexton, P. M. Differential Activation and Modulation of the Glucagon-Like Peptide-1 Receptor by Small Molecule Ligands Mol. Pharmacol. 2013, 83, 822-834 10.1124/mol.112.084525
    • (2013) Mol. Pharmacol. , vol.83 , pp. 822-834
    • Wootten, D.1    Savage, E.E.2    Willard, F.S.3    Bueno, A.B.4    Sloop, K.W.5    Christopoulos, A.6    Sexton, P.M.7
  • 85
    • 76749091482 scopus 로고    scopus 로고
    • Allosteric Antipsychotics: M4Muscarinic Potentiators as Novel Treatments for Schizophrenia
    • Farrell, M.; Roth, B. L. Allosteric Antipsychotics: M4Muscarinic Potentiators as Novel Treatments for Schizophrenia Neuropsychopharmacology 2010, 35, 851-852 10.1038/npp.2009.206
    • (2010) Neuropsychopharmacology , vol.35 , pp. 851-852
    • Farrell, M.1    Roth, B.L.2
  • 88
    • 84904860442 scopus 로고    scopus 로고
    • A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptor
    • Morris, L. C.; Days, E. L.; Turney, M.; Mi, D.; Lindsley, C. W.; Weaver, C. D.; Niswender, K. D. A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptor J. Biomol. Screening 2014, 19, 847-858 10.1177/1087057114520971
    • (2014) J. Biomol. Screening , vol.19 , pp. 847-858
    • Morris, L.C.1    Days, E.L.2    Turney, M.3    Mi, D.4    Lindsley, C.W.5    Weaver, C.D.6    Niswender, K.D.7
  • 89
    • 84918528163 scopus 로고    scopus 로고
    • Discovery of (S)-2-Cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): A Novel, CNS Penetrant GLP-1 Positive Allosteric Modulator (PAM)
    • Morris, L. C.; Nance, K. D.; Gentry, P. R.; Days, E. L.; Weaver, C. D.; Niswender, C. M.; Thompson, A. D.; Jones, C. K.; Locuson, C. W.; Morrison, R. D. et al. Discovery of (S)-2-Cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): A Novel, CNS Penetrant GLP-1 Positive Allosteric Modulator (PAM) J. Med. Chem. 2014, 57, 10192-10197 10.1021/jm501375c
    • (2014) J. Med. Chem. , vol.57 , pp. 10192-10197
    • Morris, L.C.1    Nance, K.D.2    Gentry, P.R.3    Days, E.L.4    Weaver, C.D.5    Niswender, C.M.6    Thompson, A.D.7    Jones, C.K.8    Locuson, C.W.9    Morrison, R.D.10
  • 90
    • 84882643174 scopus 로고    scopus 로고
    • 5) Positive Allosteric Modulators (PAMs) for the Treatment of Schizophrenia: An Historical Perspective and a Review of the Patent Literature
    • 5) Positive Allosteric Modulators (PAMs) for the Treatment of Schizophrenia: An Historical Perspective and a Review of the Patent Literature Pharm. Pat. Anal. 2013, 2, 93-108 10.4155/ppa.12.82
    • (2013) Pharm. Pat. Anal. , vol.2 , pp. 93-108
    • Lindsley, C.W.1    Stauffer, S.R.2
  • 91
    • 80051710347 scopus 로고    scopus 로고
    • Recent Advances in the Design and Development of Novel Negative Allosteric Modulators of mGlu5
    • Emmitte, K. A. Recent Advances in the Design and Development of Novel Negative Allosteric Modulators of mGlu5 ACS Chem. Neurosci. 2011, 2, 411-432 10.1021/cn2000266
    • (2011) ACS Chem. Neurosci. , vol.2 , pp. 411-432
    • Emmitte, K.A.1
  • 95
    • 36448968578 scopus 로고    scopus 로고
    • Allosteric Modulation of Heterodimeric G-Protein-Coupled Receptors
    • Milligan, G.; Smith, N. J. Allosteric Modulation of Heterodimeric G-Protein-Coupled Receptors Trends Pharmacol. Sci. 2007, 28, 615-620 10.1016/j.tips.2007.11.001
    • (2007) Trends Pharmacol. Sci. , vol.28 , pp. 615-620
    • Milligan, G.1    Smith, N.J.2
  • 96
    • 0034714335 scopus 로고    scopus 로고
    • Oligomerization of μ- And δ-Opioid Receptors. Generation of Novel Functional Properties
    • George, S. R.; Fan, T.; Xie, Z.; Tse, R.; Tam, V.; Varghese, G.; O'Dowd, B. F. Oligomerization of μ- and δ-Opioid Receptors. Generation of Novel Functional Properties J. Biol. Chem. 2000, 275, 26128-26135 10.1074/jbc.M000345200
    • (2000) J. Biol. Chem. , vol.275 , pp. 26128-26135
    • George, S.R.1    Fan, T.2    Xie, Z.3    Tse, R.4    Tam, V.5    Varghese, G.6    O'Dowd, B.F.7
  • 97
    • 33846328669 scopus 로고    scopus 로고
    • D1-D2 Dopamine Receptor Heterooligomers with Unique Pharmacology are Coupled to Rapid Activation of Gq/11 in the Striatum
    • Rashid, A. J.; So, C. H.; Kong, M. M. C.; Furtak, T.; El-Ghundi, M.; Cheng, R.; O'Dowd, B. F.; George, S. D1-D2 Dopamine Receptor Heterooligomers with Unique Pharmacology are Coupled to Rapid Activation of Gq/11 in the Striatum Proc. Natl. Acad. Sci. U. S. A. 2007, 104, 654-659 10.1073/pnas.0604049104
    • (2007) Proc. Natl. Acad. Sci. U. S. A. , vol.104 , pp. 654-659
    • Rashid, A.J.1    So, C.H.2    Kong, M.M.C.3    Furtak, T.4    El-Ghundi, M.5    Cheng, R.6    O'Dowd, B.F.7    George, S.8
  • 98
    • 3342965731 scopus 로고    scopus 로고
    • Preferential Formation of MT1/MT2 Melatonin Receptor Heterodimers with Distinct Ligand Interaction Properties Compared with MT2 Homodimers
    • Ayoub, M. A.; Levoye, A.; Delagrange, P.; Jockers, R. Preferential Formation of MT1/MT2 Melatonin Receptor Heterodimers with Distinct Ligand Interaction Properties Compared with MT2 Homodimers Mol. Pharmacol. 2004, 66, 312-321 10.1124/mol.104.000398
    • (2004) Mol. Pharmacol. , vol.66 , pp. 312-321
    • Ayoub, M.A.1    Levoye, A.2    Delagrange, P.3    Jockers, R.4
  • 100
    • 0035955732 scopus 로고    scopus 로고
    • The Angiotensin II AT2 Receptor is an AT1 Receptor Antagonist
    • AbdAlla, S.; Lother, H.; Abdel-tawab, A. M.; Quitterer, U. The Angiotensin II AT2 Receptor is an AT1 Receptor Antagonist J. Biol. Chem. 2001, 276, 39721-39726 10.1074/jbc.M105253200
    • (2001) J. Biol. Chem. , vol.276 , pp. 39721-39726
    • AbdAlla, S.1    Lother, H.2    Abdel-Tawab, A.M.3    Quitterer, U.4
  • 101
    • 33746290412 scopus 로고    scopus 로고
    • The Orphan GPR50 Receptor Specifically Inhibits MT1Melatonin Receptor Function Through Heterodimerization
    • Levoye, A.; Dam, L.; Ayoub, M. A.; Guillaume, J.-L.; Couturier, C.; Delagrange, P.; Jockers, R. The Orphan GPR50 Receptor Specifically Inhibits MT1Melatonin Receptor Function Through Heterodimerization EMBO J. 2006, 25, 3012-3023 10.1038/sj.emboj.7601193
    • (2006) EMBO J. , vol.25 , pp. 3012-3023
    • Levoye, A.1    Dam, L.2    Ayoub, M.A.3    Guillaume, J.-L.4    Couturier, C.5    Delagrange, P.6    Jockers, R.7
  • 102
    • 72449193715 scopus 로고    scopus 로고
    • The Role of Dimerisation in the Cellular Trafficking of G-Protein-Coupled Receptors
    • Milligan, G. The Role of Dimerisation in the Cellular Trafficking of G-Protein-Coupled Receptors Curr. Opin. Pharmacol. 2010, 10, 23-29 10.1016/j.coph.2009.09.010
    • (2010) Curr. Opin. Pharmacol. , vol.10 , pp. 23-29
    • Milligan, G.1
  • 103
    • 80053374553 scopus 로고    scopus 로고
    • Structural Insights into RAMP Modification of Secretin Family G Protein-Coupled Receptors: Implications for Drug Development
    • Archbold, J. K.; Flanagan, J. U.; Watkins, H. A.; Gingell, J. J.; Hay, D. L. Structural Insights into RAMP Modification of Secretin Family G Protein-Coupled Receptors: Implications for Drug Development Trends Pharmacol. Sci. 2011, 32, 591-600 10.1016/j.tips.2011.05.007
    • (2011) Trends Pharmacol. Sci. , vol.32 , pp. 591-600
    • Archbold, J.K.1    Flanagan, J.U.2    Watkins, H.A.3    Gingell, J.J.4    Hay, D.L.5
  • 104
    • 84921714353 scopus 로고    scopus 로고
    • Calcitonin Gene-Related Peptide: Physiology and Pathophysiology
    • Russell, F. A.; King, R.; Smillie, S.-J.; Kodji, X.; Brain, S. D. Calcitonin Gene-Related Peptide: Physiology and Pathophysiology Physiol. Rev. 2014, 94, 1099-1142 10.1152/physrev.00034.2013
    • (2014) Physiol. Rev. , vol.94 , pp. 1099-1142
    • Russell, F.A.1    King, R.2    Smillie, S.-J.3    Kodji, X.4    Brain, S.D.5
  • 106
    • 15744369263 scopus 로고    scopus 로고
    • Novel Function for Receptor Activity-Modifying Proteins (RAMPs) in Post-Endocytic Receptor Trafficking
    • Bomberger, J. M.; Parameswaran, N.; Hall, C. S.; Aiyar, N.; Spielman, W. S. Novel Function for Receptor Activity-Modifying Proteins (RAMPs) in Post-Endocytic Receptor Trafficking J. Biol. Chem. 2005, 280, 9297-9307 10.1074/jbc.M413786200
    • (2005) J. Biol. Chem. , vol.280 , pp. 9297-9307
    • Bomberger, J.M.1    Parameswaran, N.2    Hall, C.S.3    Aiyar, N.4    Spielman, W.S.5
  • 107
    • 28444464430 scopus 로고    scopus 로고
    • GPCR Modulation by RAMPs
    • Hay, D. L.; Poyner, D. R.; Sexton, P. M. GPCR Modulation by RAMPs Pharmacol. Ther. 2006, 109, 173-197 10.1016/j.pharmthera.2005.06.015
    • (2006) Pharmacol. Ther. , vol.109 , pp. 173-197
    • Hay, D.L.1    Poyner, D.R.2    Sexton, P.M.3
  • 109
    • 79951854466 scopus 로고    scopus 로고
    • Dimers and Beyond: The Functional Puzzles of Class C GPCRs
    • Kniazeff, J.; Prezeau, L.; Rondard, P.; Pin, J.-P.; Goudet, C. Dimers and Beyond: The Functional Puzzles of Class C GPCRs Pharmacol. Ther. 2011, 130, 9-25 10.1016/j.pharmthera.2011.01.006
    • (2011) Pharmacol. Ther. , vol.130 , pp. 9-25
    • Kniazeff, J.1    Prezeau, L.2    Rondard, P.3    Pin, J.-P.4    Goudet, C.5
  • 110
    • 0029903640 scopus 로고    scopus 로고
    • Metabotropic Glutamate Receptor 5 is a Disulfide-Linked Dimer
    • Romano, C.; Yang, W. L.; O'Malley, K. L. Metabotropic Glutamate Receptor 5 is a Disulfide-Linked Dimer J. Biol. Chem. 1996, 271, 28612-28616 10.1074/jbc.271.45.28612
    • (1996) J. Biol. Chem. , vol.271 , pp. 28612-28616
    • Romano, C.1    Yang, W.L.2    O'Malley, K.L.3
  • 112
    • 0032483541 scopus 로고    scopus 로고
    • Dimerization of the Extracellular Calcium-Sensing Receptor (CaR) on the Cell Surface of CaR-Transfected HEK293 Cells
    • Bai, M.; Trivedi, S.; Brown, E. M. Dimerization of the Extracellular Calcium-Sensing Receptor (CaR) on the Cell Surface of CaR-Transfected HEK293 Cells J. Biol. Chem. 1998, 273, 23605-23610 10.1074/jbc.273.36.23605
    • (1998) J. Biol. Chem. , vol.273 , pp. 23605-23610
    • Bai, M.1    Trivedi, S.2    Brown, E.M.3
  • 115
    • 6944237210 scopus 로고    scopus 로고
    • The Ants go Marching Two by Two: Oligomeric Structure of G-Protein-Coupled Receptors
    • Javitch, J. A. The Ants go Marching Two by Two: Oligomeric Structure of G-Protein-Coupled Receptors Mol. Pharmacol. 2004, 66, 1077-1082 10.1124/mol.104.006320
    • (2004) Mol. Pharmacol. , vol.66 , pp. 1077-1082
    • Javitch, J.A.1
  • 117
    • 43249095827 scopus 로고    scopus 로고
    • B Receptors: Mechanism of Action and Therapeutic Perspective
    • B Receptors: Mechanism of Action and Therapeutic Perspective Curr. Neuropharmacol. 2007, 5, 195-201 10.2174/157015907781695919
    • (2007) Curr. Neuropharmacol. , vol.5 , pp. 195-201
    • Pin, J.P.1    Prezeau, L.2
  • 120
    • 4644308014 scopus 로고    scopus 로고
    • Different Functional Roles of T1R Subunits in the Heteromeric Taste Receptors
    • Xu, H.; Staszewski, L.; Tang, H.; Adler, E.; Zoller, M.; Li, X. Different Functional Roles of T1R Subunits in the Heteromeric Taste Receptors Proc. Natl. Acad. Sci. U. S. A. 2004, 101, 14258-14263 10.1073/pnas.0404384101
    • (2004) Proc. Natl. Acad. Sci. U. S. A. , vol.101 , pp. 14258-14263
    • Xu, H.1    Staszewski, L.2    Tang, H.3    Adler, E.4    Zoller, M.5    Li, X.6
  • 121
    • 26644458124 scopus 로고    scopus 로고
    • Identification of the Cyclamate Interaction Site Within the Transmembrane Domain of the Human Sweet Taste Receptor Subunit T1R3
    • Jiang, P.; Cui, M.; Zhao, B.; Snyder, L. A.; Benard, L. M. J.; Osman, R.; Max, M.; Margolskee, R. F. Identification of the Cyclamate Interaction Site Within the Transmembrane Domain of the Human Sweet Taste Receptor Subunit T1R3 J. Biol. Chem. 2005, 280, 34296-34305 10.1074/jbc.M505255200
    • (2005) J. Biol. Chem. , vol.280 , pp. 34296-34305
    • Jiang, P.1    Cui, M.2    Zhao, B.3    Snyder, L.A.4    Benard, L.M.J.5    Osman, R.6    Max, M.7    Margolskee, R.F.8
  • 124
    • 26444538550 scopus 로고    scopus 로고
    • Valine 738 and Lysine 735 in the Fifth Transmembrane Domain of rTas1r3Mediate Insensitivity Towards Lactisole of the Rat Sweet Taste Receptor
    • Winnig, M.; Bufe, B.; Meyerhof, W. Valine 738 and Lysine 735 in the Fifth Transmembrane Domain of rTas1r3Mediate Insensitivity Towards Lactisole of the Rat Sweet Taste Receptor BMC Neurosci. 2005, 6, 22-30 10.1186/1471-2202-6-22
    • (2005) BMC Neurosci. , vol.6 , pp. 22-30
    • Winnig, M.1    Bufe, B.2    Meyerhof, W.3
  • 125
    • 33751505567 scopus 로고    scopus 로고
    • The Heterodimeric Sweet Taste Receptor has Multiple Potential Ligand Binding Sites
    • Cui, M.; Jiang, P.; Maillet, E.; Max, M.; Margolskee, R. F.; Osman, R. The Heterodimeric Sweet Taste Receptor has Multiple Potential Ligand Binding Sites Curr. Pharm. Des. 2006, 12, 4591-4600 10.2174/138161206779010350
    • (2006) Curr. Pharm. Des. , vol.12 , pp. 4591-4600
    • Cui, M.1    Jiang, P.2    Maillet, E.3    Max, M.4    Margolskee, R.F.5    Osman, R.6
  • 126
    • 0029903640 scopus 로고    scopus 로고
    • Metabotropic Glutamate Receptor 5 is a Disulfide-Linked Dimer
    • Romano, C.; Yang, W. L.; O'Malley, K. L. Metabotropic Glutamate Receptor 5 is a Disulfide-Linked Dimer J. Biol. Chem. 1996, 271, 28612-2866 10.1074/jbc.271.45.28612
    • (1996) J. Biol. Chem. , vol.271 , pp. 28612-32866
    • Romano, C.1    Yang, W.L.2    O'Malley, K.L.3
  • 129
    • 77949516412 scopus 로고    scopus 로고
    • Metabotropic Glutamate Receptors: Physiology, Pharmacology, and Disease
    • Niswender, C. M.; Conn, P. J. Metabotropic Glutamate Receptors: Physiology, Pharmacology, and Disease Annu. Rev. Pharmacol. Toxicol. 2010, 50, 295-322 10.1146/annurev.pharmtox.011008.145533
    • (2010) Annu. Rev. Pharmacol. Toxicol. , vol.50 , pp. 295-322
    • Niswender, C.M.1    Conn, P.J.2
  • 130
    • 79251591614 scopus 로고    scopus 로고
    • A New Approach to Analyze Cell Surface Protein Complexes Reveals Specific Heterodimeric Metabotropic Glutamate Receptors
    • Doumazane, E.; Scholler, P.; Zwier, J. M.; Trinquet, E.; Rondard, P.; Pin, J.-P. A New Approach to Analyze Cell Surface Protein Complexes Reveals Specific Heterodimeric Metabotropic Glutamate Receptors FASEB J. 2011, 25, 66-77 10.1096/fj.10-163147
    • (2011) FASEB J. , vol.25 , pp. 66-77
    • Doumazane, E.1    Scholler, P.2    Zwier, J.M.3    Trinquet, E.4    Rondard, P.5    Pin, J.-P.6
  • 131
    • 84865263040 scopus 로고    scopus 로고
    • Functional and Pharmacological Characteristics of Metabotropic Glutamate Receptors 2/4 Heterodimers
    • Kammermeier, P. J. Functional and Pharmacological Characteristics of Metabotropic Glutamate Receptors 2/4 Heterodimers Mol. Pharmacol. 2012, 82, 438-447 10.1124/mol.112.078501
    • (2012) Mol. Pharmacol. , vol.82 , pp. 438-447
    • Kammermeier, P.J.1
  • 132
    • 79960604663 scopus 로고    scopus 로고
    • Structural Determinants of Allosteric Antagonism at Metabotropic Glutamate Receptor 2: Mechanistic Studies with New Potent Negative Allosteric Modulators
    • Lundstrom, L.; Bissantz, C.; Beck, J.; Wettstein, J. G.; Woltering, T. J.; Wichmann, J.; Gatti, S. Structural Determinants of Allosteric Antagonism at Metabotropic Glutamate Receptor 2: Mechanistic Studies with New Potent Negative Allosteric Modulators Br. J. Pharmacol. 2011, 164, 521-537 10.1111/j.1476-5381.2011.01409.x
    • (2011) Br. J. Pharmacol. , vol.164 , pp. 521-537
    • Lundstrom, L.1    Bissantz, C.2    Beck, J.3    Wettstein, J.G.4    Woltering, T.J.5    Wichmann, J.6    Gatti, S.7
  • 134
    • 84891438084 scopus 로고    scopus 로고
    • Selective Actions of Novel Allosteric Modulators Reveal Functional Heteromers of Metabotropic Glutamate Receptors in the CNS
    • Yin, S.; Noetzel, M. J.; Johnson, K. A.; Zamorano, R.; Jalan-Sakrikar, N.; Gregory, K. J.; Conn, P. J.; Niswender, C. M. Selective Actions of Novel Allosteric Modulators Reveal Functional Heteromers of Metabotropic Glutamate Receptors in the CNS J. Neurosci. 2014, 34, 79-94 10.1523/JNEUROSCI.1129-13.2014
    • (2014) J. Neurosci. , vol.34 , pp. 79-94
    • Yin, S.1    Noetzel, M.J.2    Johnson, K.A.3    Zamorano, R.4    Jalan-Sakrikar, N.5    Gregory, K.J.6    Conn, P.J.7    Niswender, C.M.8
  • 135
    • 77953396876 scopus 로고    scopus 로고
    • Identification and Characterization of a Potent and Selective Positive Allosteric Modulator of mGluR4
    • Presented at, Washington, DC, Poster 823.27/C40
    • Ortuno, D.; Cheng, C.; Weiss, M.; Bergeron, M.; Shanker, Y. Identification and Characterization of a Potent and Selective Positive Allosteric Modulator of mGluR4. Presented at Neuroscience 2008, Washington, DC, 2008; Poster 823.27/C40.
    • (2008) Neuroscience 2008
    • Ortuno, D.1    Cheng, C.2    Weiss, M.3    Bergeron, M.4    Shanker, Y.5
  • 136
    • 84872142960 scopus 로고    scopus 로고
    • Synergy between l -DOPA and a Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4: Implications for Parkinson's Disease Treatment and Dyskinesia
    • Bennouar, K. E.; Uberti, M. A.; Melon, C.; Bacolod, M. D.; Jimenez, H. N.; Cajina, M.; Kerkerian-Le Goff, L.; Doller, D.; Gubellini, P. Synergy between l -DOPA and a Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4: Implications for Parkinson's Disease Treatment and Dyskinesia Neuropharmacology 2013, 66, 158-169 10.1016/j.neuropharm.2012.03.022
    • (2013) Neuropharmacology , vol.66 , pp. 158-169
    • Bennouar, K.E.1    Uberti, M.A.2    Melon, C.3    Bacolod, M.D.4    Jimenez, H.N.5    Cajina, M.6    Kerkerian-Le Goff, L.7    Doller, D.8    Gubellini, P.9
  • 137
    • 84928704210 scopus 로고    scopus 로고
    • Overlapping Binding Sites Drive Allosteric Agonism and Positive Cooperativity in Type 4 Metabotropic Glutamate Receptors
    • Rovira, X.; Malhaire, F.; Scholler, P.; Rodrigo, J.; Gonzalez-Bulnes, P.; Llebaria, A.; Pin, J. P.; Giraldo, J.; Goudet, C. Overlapping Binding Sites Drive Allosteric Agonism and Positive Cooperativity in Type 4 Metabotropic Glutamate Receptors FASEB J. 2015, 29, 116-130 10.1096/fj.14-257287
    • (2015) FASEB J. , vol.29 , pp. 116-130
    • Rovira, X.1    Malhaire, F.2    Scholler, P.3    Rodrigo, J.4    Gonzalez-Bulnes, P.5    Llebaria, A.6    Pin, J.P.7    Giraldo, J.8    Goudet, C.9
  • 138
    • 19444377720 scopus 로고    scopus 로고
    • Group III Metabotropic Glutamate-Receptor-Mediated Modulation of Excitatory Transmission in Rodent Substantia Nigra Pars Compacta Dopamine Neurons
    • Valenti, O.; Mannaioni, G.; Seabrook, G. R.; Marino, M. J. Group III Metabotropic Glutamate-Receptor-Mediated Modulation of Excitatory Transmission in Rodent Substantia Nigra Pars Compacta Dopamine Neurons J. Pharmacol. Exp. Ther. 2005, 313, 1296-1304 10.1124/jpet.104.080481
    • (2005) J. Pharmacol. Exp. Ther. , vol.313 , pp. 1296-1304
    • Valenti, O.1    Mannaioni, G.2    Seabrook, G.R.3    Marino, M.J.4
  • 139
    • 0028933282 scopus 로고
    • Metabotropic Glutamate Receptor-Mediated Presynaptic Depression at Corticostriatal Synapses Involves mGluR2 or 3
    • Lovinger, D. M.; McCool, B. A. Metabotropic Glutamate Receptor-Mediated Presynaptic Depression at Corticostriatal Synapses Involves mGluR2 or 3 J. Neurophysiol. 1995, 73, 1076-1083
    • (1995) J. Neurophysiol. , vol.73 , pp. 1076-1083
    • Lovinger, D.M.1    McCool, B.A.2
  • 140
    • 0035966145 scopus 로고    scopus 로고
    • Group 2 Metabotropic Glutamate Receptors Induced Long Term Depression in Mouse Striatal Slices
    • Kahn, L.; Alonso, G.; Robbe, D.; Bockaert, J.; Manzoni, O. J. Group 2 Metabotropic Glutamate Receptors Induced Long Term Depression in Mouse Striatal Slices Neurosci. Lett. 2001, 316, 178-182 10.1016/S0304-3940(01)02397-7
    • (2001) Neurosci. Lett. , vol.316 , pp. 178-182
    • Kahn, L.1    Alonso, G.2    Robbe, D.3    Bockaert, J.4    Manzoni, O.J.5
  • 141
    • 58149527808 scopus 로고    scopus 로고
    • Enhanced Sensitivity to Group II mGlu Receptor Activation at Corticostriatal Synapses in Mice Lacking the Familial Parkinsonism-Linked genes PINK1 or Parkin
    • Martella, G.; Platania, P.; Vita, D.; Sciamanna, G.; Cuomo, D.; Tassone, A.; Tscherter, A.; Kitada, T.; Bonsi, P.; Shen, J. et al. Enhanced Sensitivity to Group II mGlu Receptor Activation at Corticostriatal Synapses in Mice Lacking the Familial Parkinsonism-Linked genes PINK1 or Parkin Exp. Neurol. 2009, 215, 388-396 10.1016/j.expneurol.2008.11.001
    • (2009) Exp. Neurol. , vol.215 , pp. 388-396
    • Martella, G.1    Platania, P.2    Vita, D.3    Sciamanna, G.4    Cuomo, D.5    Tassone, A.6    Tscherter, A.7    Kitada, T.8    Bonsi, P.9    Shen, J.10
  • 142
    • 0036895272 scopus 로고    scopus 로고
    • Striatal Metabotropic Glutamate Receptor Function Following Experimental Parkinsonism and Chronic Levodopa Treatment
    • Picconi, B.; Pisani, A.; Centonze, D.; Battaglia, G.; Storto, M.; Nicoletti, F.; Bernardi, G.; Calabresi, P. Striatal Metabotropic Glutamate Receptor Function Following Experimental Parkinsonism and Chronic Levodopa Treatment Brain 2002, 125, 2635-2645 10.1093/brain/awf269
    • (2002) Brain , vol.125 , pp. 2635-2645
    • Picconi, B.1    Pisani, A.2    Centonze, D.3    Battaglia, G.4    Storto, M.5    Nicoletti, F.6    Bernardi, G.7    Calabresi, P.8
  • 143
    • 84902242673 scopus 로고    scopus 로고
    • Distinct Effects of mGlu4 Receptor Positive Allosteric Modulators at Corticostriatal vs. Striatopallidal Synapses May Differentially Contribute to their Antiparkinsonian Action
    • Gubellini, P.; Melon, C.; Dale, E.; Doller, D.; Kerkerian-Le Goff, L. Distinct Effects of mGlu4 Receptor Positive Allosteric Modulators at Corticostriatal vs. Striatopallidal Synapses May Differentially Contribute to their Antiparkinsonian Action Neuropharmacology 2014, 85, 166-177 10.1016/j.neuropharm.2014.05.025
    • (2014) Neuropharmacology , vol.85 , pp. 166-177
    • Gubellini, P.1    Melon, C.2    Dale, E.3    Doller, D.4    Kerkerian-Le Goff, L.5
  • 145
    • 27944470972 scopus 로고    scopus 로고
    • Metabotropic Glutamate Receptors in the Basal Ganglia Motor Circuit
    • Conn, P. J.; Battaglia, G.; Marino, M. J.; Nicoletti, F. Metabotropic Glutamate Receptors in the Basal Ganglia Motor Circuit Nat. Rev. Neurosci. 2005, 6, 787-798 10.1038/nrn1763
    • (2005) Nat. Rev. Neurosci. , vol.6 , pp. 787-798
    • Conn, P.J.1    Battaglia, G.2    Marino, M.J.3    Nicoletti, F.4
  • 146
    • 84856022448 scopus 로고    scopus 로고
    • The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU0364770 Produces Efficacy Alone and in Combination with l -DOPA or an Adenosine 2A Antagonist in Preclinical Rodent Models of Parkinson's Disease
    • Jones, C. K.; Bubser, M.; Thompson, A. D.; Dickerson, J. W.; Turle-Lorenzo, N.; Amalric, M.; Blobaum, A. L.; Bridges, T. M.; Morrison, R. D.; Jadhav, S. et al. The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU0364770 Produces Efficacy Alone and in Combination with l -DOPA or an Adenosine 2A Antagonist in Preclinical Rodent Models of Parkinson's Disease J. Pharmacol. Exp. Ther. 2012, 340, 404-421 10.1124/jpet.111.187443
    • (2012) J. Pharmacol. Exp. Ther. , vol.340 , pp. 404-421
    • Jones, C.K.1    Bubser, M.2    Thompson, A.D.3    Dickerson, J.W.4    Turle-Lorenzo, N.5    Amalric, M.6    Blobaum, A.L.7    Bridges, T.M.8    Morrison, R.D.9    Jadhav, S.10
  • 147
    • 80455173693 scopus 로고    scopus 로고
    • Discovery, Synthesis, and Structure-Activity Relationship Development of a Series of N-4-(2,5-Dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): Characterization of a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu(4)) with Oral Efficacy in an Antiparkinsonian Animal Model
    • Jones, C. K.; Engers, D. W.; Thompson, A. D.; Field, J. R.; Blobaum, A. L.; Lindsley, S. R.; Zhou, Y.; Gogliotti, R. D.; Jadhav, S.; Zamorano, R. et al. Discovery, Synthesis, and Structure-Activity Relationship Development of a Series of N-4-(2,5-Dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): Characterization of a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu(4)) with Oral Efficacy in an Antiparkinsonian Animal Model J. Med. Chem. 2011, 54, 7639-7647 10.1021/jm200956q
    • (2011) J. Med. Chem. , vol.54 , pp. 7639-7647
    • Jones, C.K.1    Engers, D.W.2    Thompson, A.D.3    Field, J.R.4    Blobaum, A.L.5    Lindsley, S.R.6    Zhou, Y.7    Gogliotti, R.D.8    Jadhav, S.9    Zamorano, R.10
  • 148
  • 149
    • 84866331745 scopus 로고    scopus 로고
    • A Potent and Selective Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator Improves Movement in Rodent Models of Parkinson's Disease
    • Le Poul, E.; Boléa, C.; Girard, F.; Poli, S.; Charvin, D.; Campo, B.; Bortoli, J.; Bessif, A.; Luo, B.; Koser, A. J. et al. A Potent and Selective Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator Improves Movement in Rodent Models of Parkinson's Disease J. Pharmacol. Exp. Ther. 2012, 343, 167-177 10.1124/jpet.112.196063
    • (2012) J. Pharmacol. Exp. Ther. , vol.343 , pp. 167-177
    • Le Poul, E.1    Boléa, C.2    Girard, F.3    Poli, S.4    Charvin, D.5    Campo, B.6    Bortoli, J.7    Bessif, A.8    Luo, B.9    Koser, A.J.10
  • 150
    • 3142619404 scopus 로고    scopus 로고
    • Therapeutic Doses of l -Dopa Reverse Hypersensitivity of Corticostriatal D2-Dopamine Receptors and Glutamatergic Overactivity in Experimental Parkinsonism
    • Picconi, B.; Centonze, D.; Rossi, D.; Bernardi, G.; Calabresi, P. Therapeutic Doses of l -Dopa Reverse Hypersensitivity of Corticostriatal D2-Dopamine Receptors and Glutamatergic Overactivity in Experimental Parkinsonism Brain 2004, 127, 1661-1669 10.1093/brain/awh190
    • (2004) Brain , vol.127 , pp. 1661-1669
    • Picconi, B.1    Centonze, D.2    Rossi, D.3    Bernardi, G.4    Calabresi, P.5
  • 151
    • 20444380333 scopus 로고    scopus 로고
    • Subthalamic Nucleus Lesion Reverses Motor Abnormalities and Striatal Glutamatergic Overactivity in Experimental Parkinsonism
    • Centonze, D.; Gubellini, P.; Rossi, S.; Picconi, B.; Pisani, A.; Bernardi, G.; Calabresi, P.; Baunez, C. Subthalamic Nucleus Lesion Reverses Motor Abnormalities and Striatal Glutamatergic Overactivity in Experimental Parkinsonism Neuroscience 2005, 133, 831-840 10.1016/j.neuroscience.2005.03.006
    • (2005) Neuroscience , vol.133 , pp. 831-840
    • Centonze, D.1    Gubellini, P.2    Rossi, S.3    Picconi, B.4    Pisani, A.5    Bernardi, G.6    Calabresi, P.7    Baunez, C.8
  • 152
    • 77953290203 scopus 로고    scopus 로고
    • Cortical Regulation of Striatal Medium Spiny Neuron Dendritic Remodeling in Parkinsonism: Modulation of Glutamate Release Reverses Dopamine Depletion-Induced Dendritic Spine Loss
    • Garcia, B. G.; Neely, M. D.; Deutch, A. Y. Cortical Regulation of Striatal Medium Spiny Neuron Dendritic Remodeling in Parkinsonism: Modulation of Glutamate Release Reverses Dopamine Depletion-Induced Dendritic Spine Loss Cereb. Cortex 2010, 20, 2423-32 10.1093/cercor/bhp317
    • (2010) Cereb. Cortex , vol.20 , pp. 2423-2432
    • Garcia, B.G.1    Neely, M.D.2    Deutch, A.Y.3
  • 166
    • 0037363728 scopus 로고    scopus 로고
    • Positive Allosteric Modulation of the Human Metabotropic Glutamate Receptor 4 (hmGluR4) by SIB-1893 and MPEP
    • Mathiesen, J. M.; Svendsen, N.; Brauner-Osborne, H.; Thomsen, C.; Ramirez, M. T. Positive Allosteric Modulation of the Human Metabotropic Glutamate Receptor 4 (hmGluR4) by SIB-1893 and MPEP Br. J. Pharmacol. 2003, 138, 1026-1030 10.1038/sj.bjp.0705159
    • (2003) Br. J. Pharmacol. , vol.138 , pp. 1026-1030
    • Mathiesen, J.M.1    Svendsen, N.2    Brauner-Osborne, H.3    Thomsen, C.4    Ramirez, M.T.5
  • 168
    • 0029876140 scopus 로고    scopus 로고
    • A Novel Class of Antagonists for Metabotropic Glutamate Receptors, 7-(Hydroxyimino)cyclopropa[b]chromen-1a-carboxylates
    • Annoura, H.; Fukunaga, A.; Uesugi, M.; Tatsuoka, T.; Horikawa, Y. A Novel Class of Antagonists for Metabotropic Glutamate Receptors, 7-(Hydroxyimino)cyclopropa[b]chromen-1a-carboxylates Bioorg. Med. Chem. Lett. 1996, 6, 763-766 10.1016/0960-894X(96)00104-7
    • (1996) Bioorg. Med. Chem. Lett. , vol.6 , pp. 763-766
    • Annoura, H.1    Fukunaga, A.2    Uesugi, M.3    Tatsuoka, T.4    Horikawa, Y.5
  • 170
    • 1642454572 scopus 로고    scopus 로고
    • Thiochrome Enhances Acetylcholine Affinity at Muscarinic M4 Receptors: Receptor Subtype Selectivity via Cooperativity Rather than Affinity
    • Lazareno, S.; Dolezal, V.; Popham, A.; Birdsall, N. J. Thiochrome Enhances Acetylcholine Affinity at Muscarinic M4 Receptors: Receptor Subtype Selectivity via Cooperativity Rather than Affinity Mol. Pharmacol. 2004, 65, 257-266 10.1124/mol.65.1.257
    • (2004) Mol. Pharmacol. , vol.65 , pp. 257-266
    • Lazareno, S.1    Dolezal, V.2    Popham, A.3    Birdsall, N.J.4
  • 171
    • 68749094966 scopus 로고    scopus 로고
    • Identification of a Novel Transmembrane Domain Involved in the Negative Modulation of mGluR1 Using a Newly Discovered Allosteric mGluR1 Antagonist, 3-Cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one
    • Fukuda, J.; Suzuki, G.; Kimura, T.; Nagatomi, Y.; Ito, S.; Kawamoto, H.; Ozaki, S.; Ohta, H. Identification of a Novel Transmembrane Domain Involved in the Negative Modulation of mGluR1 Using a Newly Discovered Allosteric mGluR1 Antagonist, 3-Cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one Neuropharmacology 2009, 57, 438-445 10.1016/j.neuropharm.2009.06.017
    • (2009) Neuropharmacology , vol.57 , pp. 438-445
    • Fukuda, J.1    Suzuki, G.2    Kimura, T.3    Nagatomi, Y.4    Ito, S.5    Kawamoto, H.6    Ozaki, S.7    Ohta, H.8
  • 172
    • 29344436808 scopus 로고    scopus 로고
    • Determination of Key Amino Acids Implicated in the Actions of Allosteric Modulation by 3,3′-Difluorobenzaldazine on Rat mGlu5 Receptors
    • Muhlemann, A.; Ward, N. A.; Kratochwil, N.; Diener, C.; Fischer, C.; Stucki, A.; Jaeschke, G.; Malherbe, P.; Porter, R. H. Determination of Key Amino Acids Implicated in the Actions of Allosteric Modulation by 3,3′-Difluorobenzaldazine on Rat mGlu5 Receptors Eur. J. Pharmacol. 2006, 529, 95-104 10.1016/j.ejphar.2005.11.008
    • (2006) Eur. J. Pharmacol. , vol.529 , pp. 95-104
    • Muhlemann, A.1    Ward, N.A.2    Kratochwil, N.3    Diener, C.4    Fischer, C.5    Stucki, A.6    Jaeschke, G.7    Malherbe, P.8    Porter, R.H.9
  • 173
    • 84899020574 scopus 로고    scopus 로고
    • Identification of Specific Ligand-Receptor Interactions that Govern Binding and Cooperativity of Diverse Modulators to a Common Metabotropic Glutamate Receptor 5 Allosteric Site
    • Gregory, K. J.; Nguyen, E. D.; Malosh, C.; Mendenhall, J. L.; Zic, J. Z.; Bates, B. S.; Noetzel, M. J.; Squire, E. F.; Turner, E. M.; Rook, J. M. et al. Identification of Specific Ligand-Receptor Interactions that Govern Binding and Cooperativity of Diverse Modulators to a Common Metabotropic Glutamate Receptor 5 Allosteric Site ACS Chem. Neurosci. 2014, 5, 282-295 10.1021/cn400225x
    • (2014) ACS Chem. Neurosci. , vol.5 , pp. 282-295
    • Gregory, K.J.1    Nguyen, E.D.2    Malosh, C.3    Mendenhall, J.L.4    Zic, J.Z.5    Bates, B.S.6    Noetzel, M.J.7    Squire, E.F.8    Turner, E.M.9    Rook, J.M.10
  • 175
    • 84886566347 scopus 로고    scopus 로고
    • Exploration of Allosteric Agonism Structure-Activity Relationships Within an Acetylene Series of Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulators (PAMs): Discovery of 5-((3-Fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254)
    • Turlington, M.; Noetzel, M. J.; Chun, A.; Zhou, Y.; Gogliotti, R. D.; Nguyen, E. D.; Gregory, K. J.; Vinson, P. N.; Rook, J. M.; Gogi, K. K. et al. Exploration of Allosteric Agonism Structure-Activity Relationships Within an Acetylene Series of Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulators (PAMs): Discovery of 5-((3-Fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254) J. Med. Chem. 2013, 56, 7976-7996 10.1021/jm401028t
    • (2013) J. Med. Chem. , vol.56 , pp. 7976-7996
    • Turlington, M.1    Noetzel, M.J.2    Chun, A.3    Zhou, Y.4    Gogliotti, R.D.5    Nguyen, E.D.6    Gregory, K.J.7    Vinson, P.N.8    Rook, J.M.9    Gogi, K.K.10
  • 179
    • 77949516412 scopus 로고    scopus 로고
    • Metabotropic Glutamate Receptors: Physiology, Pharmacology, and Disease
    • Niswender, C. M.; Conn, P. J. Metabotropic Glutamate Receptors: Physiology, Pharmacology, and Disease Annu. Rev. Pharmacol. Toxicol. 2010, 50, 295-322 10.1146/annurev.pharmtox.011008.145533
    • (2010) Annu. Rev. Pharmacol. Toxicol. , vol.50 , pp. 295-322
    • Niswender, C.M.1    Conn, P.J.2
  • 180
    • 0032834028 scopus 로고    scopus 로고
    • Pharmacological Agents Acting at Subtypes of Metabotropic Glutamate Receptors
    • Schoepp, D. D.; Jane, D. E.; Monn, J. A. Pharmacological Agents Acting at Subtypes of Metabotropic Glutamate Receptors Neuropharmacology 1999, 38, 1431-1476 10.1016/S0028-3908(99)00092-1
    • (1999) Neuropharmacology , vol.38 , pp. 1431-1476
    • Schoepp, D.D.1    Jane, D.E.2    Monn, J.A.3
  • 181
    • 0030995878 scopus 로고    scopus 로고
    • Pharmacology and Functions of Metabotropic Glutamate Receptors
    • Conn, P. J.; Pin, J.-P. Pharmacology and Functions of Metabotropic Glutamate Receptors Annu. Rev. Pharmacol. Toxicol. 1997, 37, 205-237 10.1146/annurev.pharmtox.37.1.205
    • (1997) Annu. Rev. Pharmacol. Toxicol. , vol.37 , pp. 205-237
    • Conn, P.J.1    Pin, J.-P.2
  • 182
    • 80051728277 scopus 로고    scopus 로고
    • Progress Toward Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5 (mGlu5)
    • Stauffer, S. R. Progress Toward Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5 (mGlu5) ACS Chem. Neurosci. 2011, 2, 450-470 10.1021/cn2000519
    • (2011) ACS Chem. Neurosci. , vol.2 , pp. 450-470
    • Stauffer, S.R.1
  • 183
    • 80051740508 scopus 로고    scopus 로고
    • Recent Advances in the Medicinal Chemistry of the Metabotropic Glutamate Receptor 1 (mGlu1)
    • Owen, D. R. Recent Advances in the Medicinal Chemistry of the Metabotropic Glutamate Receptor 1 (mGlu1) ACS Chem. Neurosci. 2011, 2, 394-401 10.1021/cn2000124
    • (2011) ACS Chem. Neurosci. , vol.2 , pp. 394-401
    • Owen, D.R.1
  • 184
    • 79953899942 scopus 로고    scopus 로고
    • Allosteric Modulation of Family C G-Protein-Coupled Receptors: From Molecular Insights to Therapeutic Perspectives
    • Urwyler, S. Allosteric Modulation of Family C G-Protein-Coupled Receptors: From Molecular Insights to Therapeutic Perspectives Pharmacol. Rev. 2011, 63, 59-126 10.1124/pr.109.002501
    • (2011) Pharmacol. Rev. , vol.63 , pp. 59-126
    • Urwyler, S.1
  • 185
    • 0035818605 scopus 로고    scopus 로고
    • Positive Allosteric Modulators of Metabotropic Glutamate 1 Receptor: Characterization, Mechanism of Action and Binding Site
    • Knoflach, F.; Mutel, V.; Jolidon, S.; Kew, J. N.; Malherbe, P.; Vieira, E.; Wichmann, J.; Kemp, J. A. Positive Allosteric Modulators of Metabotropic Glutamate 1 Receptor: Characterization, Mechanism of Action and Binding Site Proc. Natl. Acad. Sci. U. S. A. 2001, 98, 13402-13407 10.1073/pnas.231358298
    • (2001) Proc. Natl. Acad. Sci. U. S. A. , vol.98 , pp. 13402-13407
    • Knoflach, F.1    Mutel, V.2    Jolidon, S.3    Kew, J.N.4    Malherbe, P.5    Vieira, E.6    Wichmann, J.7    Kemp, J.A.8
  • 186
    • 24344475655 scopus 로고    scopus 로고
    • 9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl and (2H-tertazol-5-yl)-amides as Potent, Orally Available mGlu1 Enhancers
    • Vieira, E.; Huwyler, J.; Jolidon, S.; Knoflach, F.; Mutel, V.; Wichmann, J. 9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl and (2H-tertazol-5-yl)-amides as Potent, Orally Available mGlu1 Enhancers Bioorg. Med. Chem. Lett. 2005, 15, 4628-4631 10.1016/j.bmcl.2005.05.135
    • (2005) Bioorg. Med. Chem. Lett. , vol.15 , pp. 4628-4631
    • Vieira, E.1    Huwyler, J.2    Jolidon, S.3    Knoflach, F.4    Mutel, V.5    Wichmann, J.6
  • 187
    • 61349180283 scopus 로고    scopus 로고
    • Fluorinated 9H-Xanthene-9-carboxylic Acid Oxazol-2-yl Amides as Potent, Orally Available mGlu1 Enhancers
    • Vieira, E.; Huwyler, J.; Jolidon, S.; Knoflach, F.; Mutel, V.; Wichmann, J. Fluorinated 9H-Xanthene-9-carboxylic Acid Oxazol-2-yl Amides as Potent, Orally Available mGlu1 Enhancers Bioorg. Med. Chem. Lett. 2009, 19, 1666-1669 10.1016/j.bmcl.2009.01.108
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 1666-1669
    • Vieira, E.1    Huwyler, J.2    Jolidon, S.3    Knoflach, F.4    Mutel, V.5    Wichmann, J.6
  • 188
    • 33746265808 scopus 로고    scopus 로고
    • A Novel Class of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Interact with a Site Distinct from that of Negative Allosteric Modulators
    • Hemstapat, K.; de Paulis, T.; Chen, Y.; Brady, A. E.; Grover, V. K.; Alagille, D.; Tamagnan, G. D.; Conn, P. J. A Novel Class of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Interact with a Site Distinct From that of Negative Allosteric Modulators Mol. Pharmacol. 2006, 70, 616-626 10.1124/mol.105.021857
    • (2006) Mol. Pharmacol. , vol.70 , pp. 616-626
    • Hemstapat, K.1    De Paulis, T.2    Chen, Y.3    Brady, A.E.4    Grover, V.K.5    Alagille, D.6    Tamagnan, G.D.7    Conn, P.J.8
  • 189
    • 49949089659 scopus 로고    scopus 로고
    • Switch in the Expression of mGlu1 and mGlu5Metabotropic Glutamate Receptors in the Cerebellum of Mice Developing Experimental Autoimmune Encephalomyelitis and in Autoptic Cerebellear Samples from Patients with Multiple Sclerosis
    • Fazio, F.; Notartomaso, S.; Aronica, E.; Storto, M.; Battaglia, G.; Vieira, E.; Gatti, S.; Bruno, V.; Biagioni, F.; Gradini, R. et al. Switch in the Expression of mGlu1 and mGlu5Metabotropic Glutamate Receptors in the Cerebellum of Mice Developing Experimental Autoimmune Encephalomyelitis and in Autoptic Cerebellear Samples From Patients with Multiple Sclerosis Neuropharmacology 2008, 55, 491-499 10.1016/j.neuropharm.2008.06.066
    • (2008) Neuropharmacology , vol.55 , pp. 491-499
    • Fazio, F.1    Notartomaso, S.2    Aronica, E.3    Storto, M.4    Battaglia, G.5    Vieira, E.6    Gatti, S.7    Bruno, V.8    Biagioni, F.9    Gradini, R.10
  • 192
    • 84887750408 scopus 로고    scopus 로고
    • Pharmacological Enhancement of mGlu1Metabotropic Glutamate Receptors Causes a Prolonged Symptomatic Benefit in a Mouse Model of Spinocerebellar Ataxia Type 1
    • Notartomaso, S.; Zappulla, C.; Biagioni, F.; Cannella, M.; Bucci, D.; Mascio, G.; Scarselli, P.; Fazio, F.; Weisz, F.; Lionetto, L. et al. Pharmacological Enhancement of mGlu1Metabotropic Glutamate Receptors Causes a Prolonged Symptomatic Benefit in a Mouse Model of Spinocerebellar Ataxia Type 1 Mol. Brain 2013, 6, 48-56 10.1186/1756-6606-6-48
    • (2013) Mol. Brain , vol.6 , pp. 48-56
    • Notartomaso, S.1    Zappulla, C.2    Biagioni, F.3    Cannella, M.4    Bucci, D.5    Mascio, G.6    Scarselli, P.7    Fazio, F.8    Weisz, F.9    Lionetto, L.10
  • 195
    • 77953661232 scopus 로고    scopus 로고
    • Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4
    • Williams, R.; Zhou, Y.; Niswender, C. M.; Luo, Q.; Conn, P. J.; Lindsley, C. W.; Hopkins, C. R. Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4 ACS Chem. Neurosci. 2010, 1, 411-419 10.1021/cn9000318
    • (2010) ACS Chem. Neurosci. , vol.1 , pp. 411-419
    • Williams, R.1    Zhou, Y.2    Niswender, C.M.3    Luo, Q.4    Conn, P.J.5    Lindsley, C.W.6    Hopkins, C.R.7
  • 196
    • 84945918469 scopus 로고    scopus 로고
    • Lead Optimization of the VU0486321 Series of mGlu1 PAMs. Part 1: SAR of Modifications to the Central Aryl Core
    • Garcia-Barrantes, P. M.; Cho, H. P.; Blobaum, A. L.; Niswender, C. M.; Conn, P. J.; Lindsley, C. W. Lead Optimization of the VU0486321 Series of mGlu1 PAMs. Part 1: SAR of Modifications to the Central Aryl Core Bioorg. Med. Chem. Lett. 2015, 25, 5107-5110 10.1016/j.bmcl.2015.10.013
    • (2015) Bioorg. Med. Chem. Lett. , vol.25 , pp. 5107-5110
    • Garcia-Barrantes, P.M.1    Cho, H.P.2    Blobaum, A.L.3    Niswender, C.M.4    Conn, P.J.5    Lindsley, C.W.6
  • 197
    • 0032834028 scopus 로고    scopus 로고
    • Pharmacological Agents Acting at Subtypes of Metabotropic Glutamate Receptors
    • Schoepp, D. D.; Jane, D. E.; Monn, J. A. Pharmacological Agents Acting at Subtypes of Metabotropic Glutamate Receptors Neuropharmacology 1999, 38, 1431-1476 10.1016/S0028-3908(99)00092-1
    • (1999) Neuropharmacology , vol.38 , pp. 1431-1476
    • Schoepp, D.D.1    Jane, D.E.2    Monn, J.A.3
  • 198
    • 0030995878 scopus 로고    scopus 로고
    • Pharmacology and Functions of Metabotropic Glutamate Receptors
    • Conn, P. J.; Pin, J.-P. Pharmacology and Functions of Metabotropic Glutamate Receptors Annu. Rev. Pharmacol. Toxicol. 1997, 37, 205-237 10.1146/annurev.pharmtox.37.1.205
    • (1997) Annu. Rev. Pharmacol. Toxicol. , vol.37 , pp. 205-237
    • Conn, P.J.1    Pin, J.-P.2
  • 200
    • 84872166978 scopus 로고    scopus 로고
    • MGlu2/3 and mGlu5 Receptors: Potential Targets for Novel Antidepressants
    • Chaki, S.; Ago, Y.; Palucha-Paniewiera, A.; Matrisciano, F.; Pilc, A. mGlu2/3 and mGlu5 Receptors: Potential Targets for Novel Antidepressants Neuropharmacology 2013, 66, 40-52 10.1016/j.neuropharm.2012.05.022
    • (2013) Neuropharmacology , vol.66 , pp. 40-52
    • Chaki, S.1    Ago, Y.2    Palucha-Paniewiera, A.3    Matrisciano, F.4    Pilc, A.5
  • 201
    • 34347241277 scopus 로고    scopus 로고
    • Metabotropic Glutamate Receptor Ligands as Possible Anxiolytic and Antidepressant Drugs
    • Palucha, A.; Pilc, A. Metabotropic Glutamate Receptor Ligands as Possible Anxiolytic and Antidepressant Drugs Pharmacol. Ther. 2007, 115, 116-147 10.1016/j.pharmthera.2007.04.007
    • (2007) Pharmacol. Ther. , vol.115 , pp. 116-147
    • Palucha, A.1    Pilc, A.2
  • 202
    • 15644369847 scopus 로고    scopus 로고
    • Design, Synthesis, and Pharmacological Characterization of (+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY354740): A Potent, Selective, and Orally Active Group 2 Metabotropic Glutamate Receptor Agonist Possessing Anticonvulsant and Anxiolytic Properties
    • Monn, J. A.; Valli, M. J.; Massey, S. M.; Wright, R. A.; Salhoff, C. R.; Johnson, B. G.; Howe, T.; Alt, C. A.; Rhodes, G. A.; Robey, R. L. et al. Design, Synthesis, and Pharmacological Characterization of (+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY354740): A Potent, Selective, and Orally Active Group 2 Metabotropic Glutamate Receptor Agonist Possessing Anticonvulsant and Anxiolytic Properties J. Med. Chem. 1997, 40, 528-537 10.1021/jm9606756
    • (1997) J. Med. Chem. , vol.40 , pp. 528-537
    • Monn, J.A.1    Valli, M.J.2    Massey, S.M.3    Wright, R.A.4    Salhoff, C.R.5    Johnson, B.G.6    Howe, T.7    Alt, C.A.8    Rhodes, G.A.9    Robey, R.L.10
  • 203
    • 0033602516 scopus 로고    scopus 로고
    • Synthesis, Pharmacological Characterization, and Molecular Modeling of Heterobicyclic Amino Acids Related to (+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY354740): Identification of Two New Potent, Selective, and Systemically Active Agonists for Group II Metabotropic Glutamate Receptors
    • Monn, J. A.; Valli, M. J.; Massey, S. M.; Hansen, M. M.; Kress, T. J.; Wepsiec, J. P.; Harkness, A. R.; Grutsch, J. L., Jr.; Wright, R. A.; Johnson, B. G. et al. Synthesis, Pharmacological Characterization, and Molecular Modeling of Heterobicyclic Amino Acids Related to (+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY354740): Identification of Two New Potent, Selective, and Systemically Active Agonists for Group II Metabotropic Glutamate Receptors J. Med. Chem. 1999, 42, 1027-1040 10.1021/jm980616n
    • (1999) J. Med. Chem. , vol.42 , pp. 1027-1040
    • Monn, J.A.1    Valli, M.J.2    Massey, S.M.3    Hansen, M.M.4    Kress, T.J.5    Wepsiec, J.P.6    Harkness, A.R.7    Grutsch, Jr.J.L.8    Wright, R.A.9    Johnson, B.G.10
  • 205
    • 0035996365 scopus 로고    scopus 로고
    • The Anxiolytic Action of mGlu2/3 Receptor Agonist, LY354740, in the Fear-Potentiated Startle Model in Rats is Mechanistically Distinct from Diazepam
    • Tizzano, J. P.; Griffey, K. I.; Schoepp, D. D. The Anxiolytic Action of mGlu2/3 Receptor Agonist, LY354740, in the Fear-Potentiated Startle Model in Rats is Mechanistically Distinct from Diazepam Pharmacol., Biochem. Behav. 2002, 73, 367-374 10.1016/S0091-3057(02)00850-X
    • (2002) Pharmacol., Biochem. Behav. , vol.73 , pp. 367-374
    • Tizzano, J.P.1    Griffey, K.I.2    Schoepp, D.D.3
  • 206
    • 0344980107 scopus 로고    scopus 로고
    • Potential Anti-Anxiety, Anti-Addictive Effects of LY 354740, a Selective Group II Glutamate Metabotropic Receptors Agonist in Animal Models
    • Kłodzińska, A.; Chojnacka-Wójcik, E.; Pałucha, A.; Brański, P.; Popik, P.; Pilc, A. Potential Anti-Anxiety, Anti-Addictive Effects of LY 354740, a Selective Group II Glutamate Metabotropic Receptors Agonist in Animal Models Neuropharmacology 1999, 38, 1831-1839 10.1016/S0028-3908(99)00066-0
    • (1999) Neuropharmacology , vol.38 , pp. 1831-1839
    • Kłodzińska, A.1    Chojnacka-Wójcik, E.2    Pałucha, A.3    Brański, P.4    Popik, P.5    Pilc, A.6
  • 207
    • 0031933951 scopus 로고    scopus 로고
    • Anxiolytic and Side-Effect Profile of LY354740: A Potent, Highly Selective, Orally Active Agonist for Group II Metabotropic Glutamate Receptors
    • Helton, D. R.; Tizzano, J. P.; Monn, J. A.; Schoepp, D. D.; Kallman, M. J. Anxiolytic and Side-Effect Profile of LY354740: A Potent, Highly Selective, Orally Active Agonist for Group II Metabotropic Glutamate Receptors J. Pharmacol. Exp. Ther. 1998, 284, 651-660
    • (1998) J. Pharmacol. Exp. Ther. , vol.284 , pp. 651-660
    • Helton, D.R.1    Tizzano, J.P.2    Monn, J.A.3    Schoepp, D.D.4    Kallman, M.J.5
  • 208
    • 33745966819 scopus 로고    scopus 로고
    • Pharmacological Stimulation of Group II Metabotropic Glutamate Receptors Reduces Cocaine Self-Administration and Cocaine-Induced Reinstatement of Drug Seeking in Squirrel Monkeys
    • Adewale, A. S.; Platt, D. M.; Spealman, R. D. Pharmacological Stimulation of Group II Metabotropic Glutamate Receptors Reduces Cocaine Self-Administration and Cocaine-Induced Reinstatement of Drug Seeking in Squirrel Monkeys J. Pharmacol. Exp. Ther. 2006, 318, 922-931 10.1124/jpet.106.105387
    • (2006) J. Pharmacol. Exp. Ther. , vol.318 , pp. 922-931
    • Adewale, A.S.1    Platt, D.M.2    Spealman, R.D.3
  • 209
    • 33646565030 scopus 로고    scopus 로고
    • The Group II Metabotropic Glutamate Receptor Agonist, LY379268, Inhibits both Cocaine- and Food-Seeking Behavior in Rats
    • Peters, J.; Kalivas, P. W. The Group II Metabotropic Glutamate Receptor Agonist, LY379268, Inhibits both Cocaine- and Food-Seeking Behavior in Rats Psychopharmacology 2006, 186, 143-149 10.1007/s00213-006-0372-9
    • (2006) Psychopharmacology , vol.186 , pp. 143-149
    • Peters, J.1    Kalivas, P.W.2
  • 210
    • 2442672865 scopus 로고    scopus 로고
    • Preferential Effects of the Metabotropic Glutamate 2/3 Receptor Agonist LY379268 on Conditioned Reinstatement Versus Primary Reinforcement: Comparison between Cocaine and a Potent Conventional Reinforce
    • Baptista, M. A. S.; Martin-Fardon, R.; Weiss, F. Preferential Effects of the Metabotropic Glutamate 2/3 Receptor Agonist LY379268 on Conditioned Reinstatement Versus Primary Reinforcement: Comparison Between Cocaine and a Potent Conventional Reinforce J. Neurosci. 2004, 24, 4723-4727 10.1523/JNEUROSCI.0176-04.2004
    • (2004) J. Neurosci. , vol.24 , pp. 4723-4727
    • Baptista, M.A.S.1    Martin-Fardon, R.2    Weiss, F.3
  • 211
    • 34547686245 scopus 로고    scopus 로고
    • The Use of Knock-Out Mice Unravels Distinct Roles for mGlu2 and mGlu3Metabotropic Glutamate Receptors in Mechanisms of Neurodegeneration/Neuroprotection
    • Corti, C.; Battaglia, G.; Molinaro, G.; Riozzi, B.; Pittaluga, A.; Corsi, M.; Mugnaini, M.; Nicoletti, F.; Bruno, V. The Use of Knock-Out Mice Unravels Distinct Roles for mGlu2 and mGlu3Metabotropic Glutamate Receptors in Mechanisms of Neurodegeneration/Neuroprotection J. Neurosci. 2007, 27, 8297-8308 10.1523/JNEUROSCI.1889-07.2007
    • (2007) J. Neurosci. , vol.27 , pp. 8297-8308
    • Corti, C.1    Battaglia, G.2    Molinaro, G.3    Riozzi, B.4    Pittaluga, A.5    Corsi, M.6    Mugnaini, M.7    Nicoletti, F.8    Bruno, V.9
  • 214
    • 0032822044 scopus 로고    scopus 로고
    • LY379268, a Potent and Selective Group II Metabotropic Glutamate Receptor Agonist, is Neuroprotective in Gerbil Global, but not Focal, Cerebral Ischemia
    • Bond, A.; Ragumoorthy, N.; Monn, J. A.; Hicks, C. A.; Ward, M. A.; Lodge, D.; O'Neill, M. J. LY379268, a Potent and Selective Group II Metabotropic Glutamate Receptor Agonist, is Neuroprotective in Gerbil Global, but not Focal, Cerebral Ischemia Neurosci. Lett. 1999, 273, 191-194 10.1016/S0304-3940(99)00663-1
    • (1999) Neurosci. Lett. , vol.273 , pp. 191-194
    • Bond, A.1    Ragumoorthy, N.2    Monn, J.A.3    Hicks, C.A.4    Ward, M.A.5    Lodge, D.6    O'Neill, M.J.7
  • 215
    • 25444470248 scopus 로고    scopus 로고
    • An Efficient Synthesis of LY544344·HCl: A Prodrug of mGluR2 Agonist LY354740
    • Coffey, D. S.; Hawk, M. K.; Pedersen, S. W.; Vaid, R. K. An Efficient Synthesis of LY544344·HCl: A Prodrug of mGluR2 Agonist LY354740 Tetrahedron Lett. 2005, 46, 7299-7302 10.1016/j.tetlet.2005.08.144
    • (2005) Tetrahedron Lett. , vol.46 , pp. 7299-7302
    • Coffey, D.S.1    Hawk, M.K.2    Pedersen, S.W.3    Vaid, R.K.4
  • 216
    • 31144440181 scopus 로고    scopus 로고
    • Improved Bioavailability of the mGlu2/3 Receptor Agonist LY354740 using a Prodrug Strategy: In Vivo Pharmacology of LY544344
    • Rorick-Kehn, L. M.; Perkins, E. J.; Knitowski, K. M.; Hart, J. C.; Johnson, B. G.; Schoepp, D. D.; McKinzie, D. L. Improved Bioavailability of the mGlu2/3 Receptor Agonist LY354740 using a Prodrug Strategy: In Vivo Pharmacology of LY544344 J. Pharmacol. Exp. Ther. 2005, 316, 905-913 10.1124/jpet.105.091926
    • (2005) J. Pharmacol. Exp. Ther. , vol.316 , pp. 905-913
    • Rorick-Kehn, L.M.1    Perkins, E.J.2    Knitowski, K.M.3    Hart, J.C.4    Johnson, B.G.5    Schoepp, D.D.6    McKinzie, D.L.7
  • 217
    • 43649087034 scopus 로고    scopus 로고
    • Efficacy and Tolerability of an mGlu2/3 Agonist in the Treatment of Generalized Anxiety Disorder
    • Dunayevich, E.; Erickson, J.; Levine, L.; Landbloom, R.; Schoepp, D. D.; Tollefson, G. D. Efficacy and Tolerability of an mGlu2/3 Agonist in the Treatment of Generalized Anxiety Disorder Neuropsychopharmacology 2008, 33, 1603-1610 10.1038/sj.npp.1301531
    • (2008) Neuropsychopharmacology , vol.33 , pp. 1603-1610
    • Dunayevich, E.1    Erickson, J.2    Levine, L.3    Landbloom, R.4    Schoepp, D.D.5    Tollefson, G.D.6
  • 218
    • 17744390351 scopus 로고    scopus 로고
    • Effects of a Metabotropic Glutamate2/3 Receptor Agonist (LY544344/LY354740) on Panic Anxiety Induced by Cholecystokinin Tetrapeptide in Healthy Humans: Preliminary Results
    • Kellner, M.; Muhtz, C.; Stark, K.; Yassouridis, A.; Arlt, J.; Wiedemann, K. Effects of a Metabotropic Glutamate2/3 Receptor Agonist (LY544344/LY354740) on Panic Anxiety Induced by Cholecystokinin Tetrapeptide in Healthy Humans: Preliminary Results Psychopharmacology 2005, 179, 310-315 10.1007/s00213-004-2025-1
    • (2005) Psychopharmacology , vol.179 , pp. 310-315
    • Kellner, M.1    Muhtz, C.2    Stark, K.3    Yassouridis, A.4    Arlt, J.5    Wiedemann, K.6
  • 219
    • 26944475559 scopus 로고    scopus 로고
    • Metabotropic Glutamate II Receptor Agonists in Panic Disorder: A Double Blind Clinical Trial with LY354740
    • Bergink, V.; Westenberg, H. G. M. Metabotropic Glutamate II Receptor Agonists in Panic Disorder: A Double Blind Clinical Trial with LY354740 Int. Clin. Psychopharmacol. 2005, 20, 291-293 10.1097/00004850-200511000-00001
    • (2005) Int. Clin. Psychopharmacol. , vol.20 , pp. 291-293
    • Bergink, V.1    Westenberg, H.G.M.2
  • 220
    • 0041488670 scopus 로고    scopus 로고
    • Anxiolytic Effects of a Novel Group II Metabotropic Glutamate Receptor Agonist (LY354740) in the Fear-Potentiated Startle Paradigm in Humans
    • Grillon, C.; Cordova, J.; Levine, L. R.; Morgan, C. A., III. Anxiolytic Effects of a Novel Group II Metabotropic Glutamate Receptor Agonist (LY354740) in the Fear-Potentiated Startle Paradigm in Humans Psychopharmacology 2003, 168, 446-454 10.1007/s00213-003-1444-8
    • (2003) Psychopharmacology , vol.168 , pp. 446-454
    • Grillon, C.1    Cordova, J.2    Levine, L.R.3    Iii, A.M.C.4
  • 221
    • 0141644133 scopus 로고    scopus 로고
    • LY354740, and mGlu2/3 Receptor Agonist as a Novel Approach to Treat Anxiety/Stress
    • Schoepp, D. D.; Wright, R. A.; Levine, L. R.; Gaydos, B.; Potter, W. Z. LY354740, and mGlu2/3 Receptor Agonist as a Novel Approach to Treat Anxiety/Stress Stress 2003, 6, 189-197 10.1080/1025389031000146773
    • (2003) Stress , vol.6 , pp. 189-197
    • Schoepp, D.D.1    Wright, R.A.2    Levine, L.R.3    Gaydos, B.4    Potter, W.Z.5
  • 222
    • 84856072333 scopus 로고    scopus 로고
    • Metabotropic Glutamate Receptors as Therapeutic Targets for Schizophrenia
    • Vinson, P. N.; Conn, P. J. Metabotropic Glutamate Receptors as Therapeutic Targets for Schizophrenia Neuropharmacology 2012, 62, 1461-1472 10.1016/j.neuropharm.2011.05.005
    • (2012) Neuropharmacology , vol.62 , pp. 1461-1472
    • Vinson, P.N.1    Conn, P.J.2
  • 223
    • 84856097892 scopus 로고    scopus 로고
    • Group II Metabotropic Glutamate Receptor Agonists and Positive Allosteric Modulators as Novel Treatments for Schizophrenia
    • Fell, M. J.; McKinzie, D. L.; Monn, J. A.; Svensson, K. A. Group II Metabotropic Glutamate Receptor Agonists and Positive Allosteric Modulators as Novel Treatments for Schizophrenia Neuropharmacology 2012, 62, 1473-1483 10.1016/j.neuropharm.2011.06.007
    • (2012) Neuropharmacology , vol.62 , pp. 1473-1483
    • Fell, M.J.1    McKinzie, D.L.2    Monn, J.A.3    Svensson, K.A.4
  • 224
    • 58149119377 scopus 로고    scopus 로고
    • Activation of Metabotropic Glutamate Receptors as a Novel Approach for the Treatment of Schizophrenia
    • Conn, P. J.; Lindsley, C. W.; Jones, C. K. Activation of Metabotropic Glutamate Receptors as a Novel Approach for the Treatment of Schizophrenia Trends Pharmacol. Sci. 2009, 30, 25-31 10.1016/j.tips.2008.10.006
    • (2009) Trends Pharmacol. Sci. , vol.30 , pp. 25-31
    • Conn, P.J.1    Lindsley, C.W.2    Jones, C.K.3
  • 225
    • 77953620136 scopus 로고    scopus 로고
    • Group II Metabotropic Glutamate Receptor Agonists as a Potential Drug for Schizophrenia
    • Chaki, S. Group II Metabotropic Glutamate Receptor Agonists as a Potential Drug for Schizophrenia Eur. J. Pharmacol. 2010, 639, 59-66 10.1016/j.ejphar.2009.12.041
    • (2010) Eur. J. Pharmacol. , vol.639 , pp. 59-66
    • Chaki, S.1
  • 226
    • 33947415606 scopus 로고    scopus 로고
    • Pharmacological and Pharmacokinetic Properties of a Structurally Novel, Potent, and Selective Mmetabotropic Glutamate 2/3 Receptor Agonist: In Vitro Characterization of Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039)
    • Rorick-Kehn, L. M.; Johnson, B. G.; Burkey, J. L.; Wright, R. A.; Calligaro, D. O.; Marek, G. J.; Nisenbaum, E. S.; Catlow, J. T.; Kingston, A. E.; Giera, D. D. et al. Pharmacological and Pharmacokinetic Properties of a Structurally Novel, Potent, and Selective Mmetabotropic Glutamate 2/3 Receptor Agonist: In Vitro Characterization of Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039) J. Pharmacol. Exp. Ther. 2007, 321, 308-317 10.1124/jpet.106.110809
    • (2007) J. Pharmacol. Exp. Ther. , vol.321 , pp. 308-317
    • Rorick-Kehn, L.M.1    Johnson, B.G.2    Burkey, J.L.3    Wright, R.A.4    Calligaro, D.O.5    Marek, G.J.6    Nisenbaum, E.S.7    Catlow, J.T.8    Kingston, A.E.9    Giera, D.D.10
  • 227
    • 77954095737 scopus 로고    scopus 로고
    • LY-2140023, a Prodrug of the Group II Metabotropic Glutamate Receptor Agonist LY-404039 for the Potential Treatment of Schizophrenia
    • Mezler, M.; Geneste, H.; Gault, L.; Marek, G. J. LY-2140023, a Prodrug of the Group II Metabotropic Glutamate Receptor Agonist LY-404039 for the Potential Treatment of Schizophrenia Curr. Opin. Invest. Drugs 2010, 11, 833-845
    • (2010) Curr. Opin. Invest. Drugs , vol.11 , pp. 833-845
    • Mezler, M.1    Geneste, H.2    Gault, L.3    Marek, G.J.4
  • 229
    • 84907976568 scopus 로고    scopus 로고
    • Pomaglumetad Methionil (LY2140023 Monohydrate) and Aripiprazole in Patients with Schizophrenia: A Phase 3, Multicenter, Double-Blind Comparison
    • Adams, D. H.; Zhang, L.; Millen, B. A.; Kinon, B. J.; Gomez, J.-C. Pomaglumetad Methionil (LY2140023 Monohydrate) and Aripiprazole in Patients with Schizophrenia: A Phase 3, Multicenter, Double-Blind Comparison Schizophr. Res. Treat. 2014, 2014, 758212 10.1155/2014/758212
    • (2014) Schizophr. Res. Treat. , vol.2014 , pp. 758212
    • Adams, D.H.1    Zhang, L.2    Millen, B.A.3    Kinon, B.J.4    Gomez, J.-C.5
  • 231
    • 84886304673 scopus 로고    scopus 로고
    • Pomaglumetad Methionil: No Significant Difference as an Adjunctive Treatment for Patients with Prominent Negative Symptoms of Schizophrenia Compared to Placebo
    • Stauffer, V. L.; Millen, B. A.; Andersen, S.; Kinon, B. J.; LaGrandeur, L.; Lindenmayer, J. P.; Gomez, J. C. Pomaglumetad Methionil: No Significant Difference as an Adjunctive Treatment for Patients with Prominent Negative Symptoms of Schizophrenia Compared to Placebo Schizophr. Res. 2013, 150, 434-441 10.1016/j.schres.2013.08.020
    • (2013) Schizophr. Res. , vol.150 , pp. 434-441
    • Stauffer, V.L.1    Millen, B.A.2    Andersen, S.3    Kinon, B.J.4    LaGrandeur, L.5    Lindenmayer, J.P.6    Gomez, J.C.7
  • 232
    • 84878009124 scopus 로고    scopus 로고
    • A Long-Term, Phase 2, Multicenter, Randomized, Open-Label, Comparative Safety Study of Pomaglumetad Methionil (LY2140023 Monohydrate) Versus Atypical Antipsychotic Standard of Care in Patients with Schizophrenia
    • Adams, D. H.; Kinon, B. J.; Baygani, S.; Millen, B. A.; Velona, I.; Kollack-Walker, S.; Walling, D. P. A Long-Term, Phase 2, Multicenter, Randomized, Open-Label, Comparative Safety Study of Pomaglumetad Methionil (LY2140023 Monohydrate) Versus Atypical Antipsychotic Standard of Care in Patients with Schizophrenia BMC Psychiatry 2013, 13 (143) 143-152 10.1186/1471-244X-13-143
    • (2013) BMC Psychiatry , vol.13 , Issue.143 , pp. 143-152
    • Adams, D.H.1    Kinon, B.J.2    Baygani, S.3    Millen, B.A.4    Velona, I.5    Kollack-Walker, S.6    Walling, D.P.7
  • 233
    • 84872130954 scopus 로고    scopus 로고
    • Clinical Development of Pomaglumetad Methionil: A Non-Dopaminergic Treatment for Schizophrenia
    • Kinon, B. J.; Gómez, J. C. Clinical Development of Pomaglumetad Methionil: A Non-Dopaminergic Treatment for Schizophrenia Neuropharmacology 2013, 66, 82-86 10.1016/j.neuropharm.2012.06.002
    • (2013) Neuropharmacology , vol.66 , pp. 82-86
    • Kinon, B.J.1    Gómez, J.C.2
  • 234
    • 79955594301 scopus 로고    scopus 로고
    • HBBI Study Group. A Multicenter, In-patient, Phase 2, Double-Blind, Placebo-Controlled Dose-Ranging Study of LY2140023 Monohydrate in Patients with DSM-IV Schizophrenia
    • Kinon, B. J.; Zhang, L.; Millen, B. A.; Osuntokun, O. O.; Williams, J. E.; Kollack-Walker, S.; Jackson, K.; Kryzhanovskaya, L.; Jarkova, N. HBBI Study Group. A Multicenter, In-patient, Phase 2, Double-Blind, Placebo-Controlled Dose-Ranging Study of LY2140023 Monohydrate in Patients with DSM-IV Schizophrenia J. Clin. Psychopharmacol. 2011, 31, 349-355 10.1097/JCP.0b013e318218dcd5
    • (2011) J. Clin. Psychopharmacol. , vol.31 , pp. 349-355
    • Kinon, B.J.1    Zhang, L.2    Millen, B.A.3    Osuntokun, O.O.4    Williams, J.E.5    Kollack-Walker, S.6    Jackson, K.7    Kryzhanovskaya, L.8    Jarkova, N.9
  • 236
    • 84919429588 scopus 로고    scopus 로고
    • Novel Metabotropic Glutamate Receptor 2/3 Antagonists and Their Therapeutic Applications: A Patent Review (2005 - Present)
    • Célanire, S.; Sebhat, I.; Wichmann, J.; Mayer, S.; Schann, S.; Gatti, S. Novel Metabotropic Glutamate Receptor 2/3 Antagonists and Their Therapeutic Applications: A Patent Review (2005-Present) Expert Opin. Ther. Patents 2015, 25, 69-90 10.1517/13543776.2014.983899
    • (2015) Expert Opin. Ther. Patents , vol.25 , pp. 69-90
    • Célanire, S.1    Sebhat, I.2    Wichmann, J.3    Mayer, S.4    Schann, S.5    Gatti, S.6
  • 237
    • 14444286701 scopus 로고    scopus 로고
    • 2-Substituted (2SR)-2-Amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as Potent and Selective Antagonists of Group II Metabotropic Glutamate Receptors. 2. Effects of Aromatic Substitution, Pharmacological Characterization, and Bioavailability
    • Ornstein, P. L.; Bleisch, T. J.; Arnold, M. B.; Kennedy, J. H.; Wright, R. A.; Johnson, B. G.; Tizzano, J. P.; Helton, D. R.; Kallman, M. J.; Schoepp, D. D.; Hérin, M. 2-Substituted (2SR)-2-Amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as Potent and Selective Antagonists of Group II Metabotropic Glutamate Receptors. 2. Effects of Aromatic Substitution, Pharmacological Characterization, and Bioavailability J. Med. Chem. 1998, 41, 358-378 10.1021/jm970498o
    • (1998) J. Med. Chem. , vol.41 , pp. 358-378
    • Ornstein, P.L.1    Bleisch, T.J.2    Arnold, M.B.3    Kennedy, J.H.4    Wright, R.A.5    Johnson, B.G.6    Tizzano, J.P.7    Helton, D.R.8    Kallman, M.J.9    Schoepp, D.D.10    Hérin, M.11
  • 239
    • 49949084013 scopus 로고    scopus 로고
    • Behavioral Characterization of the mGlu group II/III Receptor Antagonist, LY-341495, in Animal Models of Anxiety and Depression
    • Bespalov, A. Y.; van Gaalen, M. M.; Sukhotina, I. A.; Wicke, K.; Mezler, M.; Schoemaker, H.; Gross, G. Behavioral Characterization of the mGlu group II/III Receptor Antagonist, LY-341495, in Animal Models of Anxiety and Depression Eur. J. Pharmacol. 2008, 592, 96-102 10.1016/j.ejphar.2008.06.089
    • (2008) Eur. J. Pharmacol. , vol.592 , pp. 96-102
    • Bespalov, A.Y.1    Van Gaalen, M.M.2    Sukhotina, I.A.3    Wicke, K.4    Mezler, M.5    Schoemaker, H.6    Gross, G.7
  • 240
    • 4644372048 scopus 로고    scopus 로고
    • Anxiolytic-Like Activity of MGS0039, a Potent Group II Metabotropic Glutamate Receptor Antagonist, in a Marble-Burying Behavior Test
    • Shimazaki, T.; Iijima, M.; Chaki, S. Anxiolytic-Like Activity of MGS0039, a Potent Group II Metabotropic Glutamate Receptor Antagonist, in a Marble-Burying Behavior Test Eur. J. Pharmacol. 2004, 501, 121-125 10.1016/j.ejphar.2004.08.016
    • (2004) Eur. J. Pharmacol. , vol.501 , pp. 121-125
    • Shimazaki, T.1    Iijima, M.2    Chaki, S.3
  • 241
    • 33744957683 scopus 로고    scopus 로고
    • An mGluR2/3 Antagonist, MGS0039, Exerts Antidepressant and Anxiolytic Effects in Behavioral Models in Rats
    • Yoshimizu, T.; Shimazaki, T.; Ito, A.; Chaki, S. An mGluR2/3 Antagonist, MGS0039, Exerts Antidepressant and Anxiolytic Effects in Behavioral Models in Rats Psychopharmacology 2006, 186, 587-593 10.1007/s00213-006-0390-7
    • (2006) Psychopharmacology , vol.186 , pp. 587-593
    • Yoshimizu, T.1    Shimazaki, T.2    Ito, A.3    Chaki, S.4
  • 245
    • 0842288995 scopus 로고    scopus 로고
    • Increased Cell Proliferation in the Adult Mouse Hippocampus Following Chronic Administration of Group II Metabotropic Glutamate Receptor Antagonist, MGS0039
    • Yoshimizu, T.; Chaki, S. Increased Cell Proliferation in the Adult Mouse Hippocampus Following Chronic Administration of Group II Metabotropic Glutamate Receptor Antagonist, MGS0039 Biochem. Biophys. Res. Commun. 2004, 315, 493-496 10.1016/j.bbrc.2004.01.073
    • (2004) Biochem. Biophys. Res. Commun. , vol.315 , pp. 493-496
    • Yoshimizu, T.1    Chaki, S.2
  • 246
    • 84882758341 scopus 로고    scopus 로고
    • MGlu2/3 Agonist-Induced Hyperthermia: An in Vivo Assay for Detection of mGlu2/3 Receptor Antagonism and its Relation to Antidepressant-Like Efficacy in Mice
    • Gleason, S. D.; Li, X.; Smith, I. A.; Ephlin, J. D.; Wang, X. S.; Heinz, B. A.; Carter, J. H.; Baez, M.; Yu, J. et al. mGlu2/3 Agonist-Induced Hyperthermia: An in Vivo Assay for Detection of mGlu2/3 Receptor Antagonism and its Relation to Antidepressant-Like Efficacy in Mice CNS Neurol. Disord.: Drug Targets 2013, 12, 554-566 10.2174/18715273113129990079
    • (2013) CNS Neurol. Disord.: Drug Targets , vol.12 , pp. 554-566
    • Gleason, S.D.1    Li, X.2    Smith, I.A.3    Ephlin, J.D.4    Wang, X.S.5    Heinz, B.A.6    Carter, J.H.7    Baez, M.8    Yu, J.9
  • 247
    • 84868559249 scopus 로고    scopus 로고
    • Role of BDNF/TrkB Signaling in Antidepressant-Like Effects of a Group II Metabotropic Glutamate Receptor Antagonist in Animal Models of Depression
    • Koike, H.; Fukumoto, K.; Iijima, M.; Chaki, S. Role of BDNF/TrkB Signaling in Antidepressant-Like Effects of a Group II Metabotropic Glutamate Receptor Antagonist in Animal Models of Depression Behav. Brain Res. 2013, 238, 48-52 10.1016/j.bbr.2012.10.023
    • (2013) Behav. Brain Res. , vol.238 , pp. 48-52
    • Koike, H.1    Fukumoto, K.2    Iijima, M.3    Chaki, S.4
  • 248
    • 80053601060 scopus 로고    scopus 로고
    • Involvement of the Mammalian Target of Rapamycin Signaling in the Antidepressant-Like Effect of Group II Metabotropic Glutamate Receptor Antagonists
    • Koike, H.; Iijima, M.; Chaki, S. Involvement of the Mammalian Target of Rapamycin Signaling in the Antidepressant-Like Effect of Group II Metabotropic Glutamate Receptor Antagonists Neuropharmacology 2011, 61, 1419-1423 10.1016/j.neuropharm.2011.08.034
    • (2011) Neuropharmacology , vol.61 , pp. 1419-1423
    • Koike, H.1    Iijima, M.2    Chaki, S.3
  • 249
    • 17044396861 scopus 로고    scopus 로고
    • AMPA Receptor Stimulation Mediates the Antidepressant-Like Effect of a Group II Metabotropic Glutamate Receptor Antagonist
    • Karasawa, J.; Shimazaki, T.; Kawashima, N.; Chaki, S. AMPA Receptor Stimulation Mediates the Antidepressant-Like Effect of a Group II Metabotropic Glutamate Receptor Antagonist Brain Res. 2005, 1042, 92-98 10.1016/j.brainres.2005.02.032
    • (2005) Brain Res. , vol.1042 , pp. 92-98
    • Karasawa, J.1    Shimazaki, T.2    Kawashima, N.3    Chaki, S.4
  • 250
    • 84875553685 scopus 로고    scopus 로고
    • Effect of an mGlu2/3 Receptor Antagonist on Depressive Behavior Induced by Withdrawal from Chronic Treatment with Methamphetamine
    • Iijima, M.; Koike, H.; Chaki, S. Effect of an mGlu2/3 Receptor Antagonist on Depressive Behavior Induced by Withdrawal From Chronic Treatment with Methamphetamine Behav. Brain Res. 2013, 246, 24-28 10.1016/j.bbr.2013.02.039
    • (2013) Behav. Brain Res. , vol.246 , pp. 24-28
    • Iijima, M.1    Koike, H.2    Chaki, S.3
  • 251
    • 33845211109 scopus 로고    scopus 로고
    • Metabotropic Glutamate Receptor Antagonists: Novel Therapeutics for Nicotine Dependence and Depression?
    • Markou, A. Metabotropic Glutamate Receptor Antagonists: Novel Therapeutics for Nicotine Dependence and Depression? Biol. Psychiatry 2007, 61, 17-22 10.1016/j.biopsych.2006.03.053
    • (2007) Biol. Psychiatry , vol.61 , pp. 17-22
    • Markou, A.1
  • 252
    • 84870889349 scopus 로고    scopus 로고
    • Metabotropic Glutamate 2/3 Receptor Antagonists Improve Behavioral and Prefrontal Dopaminergic Alterations in the Chronic Corticosterone-Induced Depression Model in Mice
    • Ago, Y.; Yano, K.; Araki, R.; Hiramatsu, N.; Kita, Y.; Kawasaki, T.; Onoe, H.; Chaki, S.; Nakazato, A.; Hashimoto, H.; Baba, A.; Takuma, K.; Matsuda, T. Metabotropic Glutamate 2/3 Receptor Antagonists Improve Behavioral and Prefrontal Dopaminergic Alterations in the Chronic Corticosterone-Induced Depression Model in Mice Neuropharmacology 2013, 65, 29-38 10.1016/j.neuropharm.2012.09.008
    • (2013) Neuropharmacology , vol.65 , pp. 29-38
    • Ago, Y.1    Yano, K.2    Araki, R.3    Hiramatsu, N.4    Kita, Y.5    Kawasaki, T.6    Onoe, H.7    Chaki, S.8    Nakazato, A.9    Hashimoto, H.10    Baba, A.11    Takuma, K.12    Matsuda, T.13
  • 253
    • 84902661636 scopus 로고    scopus 로고
    • MGluR2/3 Blockade Produces Rapid and Long-Lasting Reversal of Anhedonia Caused by Chronic Stress Exposure
    • Dwyer, J. M.; Lepack, A. E.; Duman, R. S. mGluR2/3 Blockade Produces Rapid and Long-Lasting Reversal of Anhedonia Caused by Chronic Stress Exposure J. Mol. Psychiatry 2013, 1, 15 10.1186/2049-9256-1-15
    • (2013) J. Mol. Psychiatry , vol.1 , pp. 15
    • Dwyer, J.M.1    Lepack, A.E.2    Duman, R.S.3
  • 254
    • 84876562945 scopus 로고    scopus 로고
    • MGluR2 Positive Allosteric Modulators: A Patent Review (2009 - Present)
    • Trabanco, A. A.; Cid, J. M. mGluR2 Positive Allosteric Modulators: A Patent Review (2009-present) Expert Opin. Ther. Pat. 2013, 23, 629-647 10.1517/13543776.2013.777043
    • (2013) Expert Opin. Ther. Pat. , vol.23 , pp. 629-647
    • Trabanco, A.A.1    Cid, J.M.2
  • 255
    • 80051770211 scopus 로고    scopus 로고
    • Recent Progress in the Synthesis and Characterization of Group II Metabotropic Glutamate Receptor Allosteric Modulators
    • Sheffler, D. J.; Pinkerton, A. B.; Dahl, R.; Markou, A.; Cosford, N. D. P. Recent Progress in the Synthesis and Characterization of Group II Metabotropic Glutamate Receptor Allosteric Modulators ACS Chem. Neurosci. 2011, 2, 382-393 10.1021/cn200008d
    • (2011) ACS Chem. Neurosci. , vol.2 , pp. 382-393
    • Sheffler, D.J.1    Pinkerton, A.B.2    Dahl, R.3    Markou, A.4    Cosford, N.D.P.5
  • 256
    • 38949207272 scopus 로고    scopus 로고
    • The mGlu2 but not the mGlu3 Receptor Mediates the Actions of the mGluR2/3 Agonist, LY379268, in Mouse Models Predictive of Antipsychotic Activity
    • Woolley, M. L.; Pemberton, D. J.; Bate, S.; Corti, C.; Jones, D. N. C. The mGlu2 but not the mGlu3 Receptor Mediates the Actions of the mGluR2/3 Agonist, LY379268, in Mouse Models Predictive of Antipsychotic Activity Psychopharmacology 2008, 196, 431-440 10.1007/s00213-007-0974-x
    • (2008) Psychopharmacology , vol.196 , pp. 431-440
    • Woolley, M.L.1    Pemberton, D.J.2    Bate, S.3    Corti, C.4    Jones, D.N.C.5
  • 257
    • 45749139623 scopus 로고    scopus 로고
    • Evidence for the Role of Metabotropic Glutamate (mGlu)2 not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of the mGlu2/3 Receptor Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic Acid (LY404039)
    • Fell, M. J.; Svensson, K. A.; Johnson, B. G.; Schoepp, D. D. Evidence for the Role of Metabotropic Glutamate (mGlu)2 not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of the mGlu2/3 Receptor Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic Acid (LY404039) J. Pharmacol. Exp. Ther. 2008, 326, 209-217 10.1124/jpet.108.136861
    • (2008) J. Pharmacol. Exp. Ther. , vol.326 , pp. 209-217
    • Fell, M.J.1    Svensson, K.A.2    Johnson, B.G.3    Schoepp, D.D.4
  • 258
    • 0038155299 scopus 로고    scopus 로고
    • Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity of N-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethylamine
    • Johnson, M. P.; Baez, M.; Jagdmann, G. E., Jr.; Britton, T. C.; Large, T. H.; Callagaro, D. O.; Tizzano, J. P.; Monn, J. A.; Schoepp, D. D. Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity of N-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethylamine J. Med. Chem. 2003, 46, 3189-3192 10.1021/jm034015u
    • (2003) J. Med. Chem. , vol.46 , pp. 3189-3192
    • Johnson, M.P.1    Baez, M.2    Jagdmann, Jr.G.E.3    Britton, T.C.4    Large, T.H.5    Callagaro, D.O.6    Tizzano, J.P.7    Monn, J.A.8    Schoepp, D.D.9
  • 259
    • 27744597869 scopus 로고    scopus 로고
    • A Selective Allosteric Potentiator of Metabotropic Glutamate (mGlu) 2 Receptors has Effects Similar to an Orthosteric mGlu2/3 Receptor Agonist in Mouse Models Predictive of Antipsychotic Activity
    • Galici, R.; Echemendia, N. G.; Rodriguez, A. L.; Conn, P. J. A Selective Allosteric Potentiator of Metabotropic Glutamate (mGlu) 2 Receptors has Effects Similar to an Orthosteric mGlu2/3 Receptor Agonist in Mouse Models Predictive of Antipsychotic Activity J. Pharmacol. Exp. Ther. 2005, 315, 1181-1187 10.1124/jpet.105.091074
    • (2005) J. Pharmacol. Exp. Ther. , vol.315 , pp. 1181-1187
    • Galici, R.1    Echemendia, N.G.2    Rodriguez, A.L.3    Conn, P.J.4
  • 260
    • 33745227414 scopus 로고    scopus 로고
    • Biphenyl-indanone A, a Positive Allosteric Modulator of the Metabotropic Glutamate Receptor Subtype 2, Has Antipsychotic- and Anxiolytic-Like Effects in Mice
    • Galici, R.; Jones, C. K.; Hempstapat, K.; Nong, Y.; Echemendia, N. G.; Williams, L. C.; de Paulis, T.; Conn, P. J. Biphenyl-indanone A, a Positive Allosteric Modulator of the Metabotropic Glutamate Receptor Subtype 2, Has Antipsychotic- and Anxiolytic-Like Effects in Mice J. Pharmacol. Exp. Ther. 2006, 318, 173-185 10.1124/jpet.106.102046
    • (2006) J. Pharmacol. Exp. Ther. , vol.318 , pp. 173-185
    • Galici, R.1    Jones, C.K.2    Hempstapat, K.3    Nong, Y.4    Echemendia, N.G.5    Williams, L.C.6    De Paulis, T.7    Conn, P.J.8
  • 261
    • 84938550306 scopus 로고    scopus 로고
    • Positive Allosteric Modulators of Metabotropic Glutamate 2 Receptors in Schizophrenia Treatment
    • Ellaithy, A.; Younkin, J.; González-Maeso, J.; Logothetis, D. E. Positive Allosteric Modulators of Metabotropic Glutamate 2 Receptors in Schizophrenia Treatment Trends Neurosci. 2015, 38, 506-516 10.1016/j.tins.2015.06.002
    • (2015) Trends Neurosci. , vol.38 , pp. 506-516
    • Ellaithy, A.1    Younkin, J.2    González-Maeso, J.3    Logothetis, D.E.4
  • 262
    • 77955670662 scopus 로고    scopus 로고
    • MGluR2-Positive Allosteric Modulators: Therapeutic Potential for Treating Cocaine Abuse?
    • Barrett, J. E. mGluR2-Positive Allosteric Modulators: Therapeutic Potential for Treating Cocaine Abuse? Neuropsychopharmacology 2010, 35, 2007-2008 10.1038/npp.2010.93
    • (2010) Neuropsychopharmacology , vol.35 , pp. 2007-2008
    • Barrett, J.E.1
  • 263
    • 57649112566 scopus 로고    scopus 로고
    • Promise of mGluR2/3 Activators in Psychiatry
    • Conn, P. J.; Jones, C. K. Promise of mGluR2/3 Activators in Psychiatry Neuropsychopharmacology 2009, 34, 248-249 10.1038/npp.2008.156
    • (2009) Neuropsychopharmacology , vol.34 , pp. 248-249
    • Conn, P.J.1    Jones, C.K.2
  • 264
    • 84923360833 scopus 로고    scopus 로고
    • Perspectives on the mGluR2/3 Agonists as a Therapeutic Target for Schizophrenia: Still Promising or a Dead End?
    • Li, M.-L.; Hu, X.-Q.; Li, F.; Gao, W.-J. Perspectives on the mGluR2/3 Agonists as a Therapeutic Target for Schizophrenia: Still Promising or a Dead End? Prog. Neuro-Psychopharmacol. Biol. Psychiatry 2015, 60, 66-76 10.1016/j.pnpbp.2015.02.012
    • (2015) Prog. Neuro-Psychopharmacol. Biol. Psychiatry , vol.60 , pp. 66-76
    • Li, M.-L.1    Hu, X.-Q.2    Li, F.3    Gao, W.-J.4
  • 265
    • 84870020714 scopus 로고    scopus 로고
    • Orally Active Metabotropic Glutamate Subtype 2 Receptor Positive Allosteric Modulators: Structure-Activity Relationships and Assessment in a Rat Model of Nicotine Dependence
    • Sidique, S.; Dhanya, R.-P.; Sheffler, D. J.; Nickols, H. H.; Yang, L.; Dahl, R.; Mangravita-Novo, A.; Smith, L. H.; D'Souza, M. S. et al. Orally Active Metabotropic Glutamate Subtype 2 Receptor Positive Allosteric Modulators: Structure-Activity Relationships and Assessment in a Rat Model of Nicotine Dependence J. Med. Chem. 2012, 55, 9434-9445 10.1021/jm3005306
    • (2012) J. Med. Chem. , vol.55 , pp. 9434-9445
    • Sidique, S.1    Dhanya, R.-P.2    Sheffler, D.J.3    Nickols, H.H.4    Yang, L.5    Dahl, R.6    Mangravita-Novo, A.7    Smith, L.H.8    D'Souza, M.S.9
  • 266
    • 84901269216 scopus 로고    scopus 로고
    • Design and Synthesis of Systemically Active Metabotropic Glutamate Subtype-2 and -3 (mGlu2/3) Receptor Positive Allosteric Modulators (PAMs): Pharmacological Characterization and Assessment in a Rat Model of Cocaine Dependence
    • Dhanya, R.-P.; Sheffler, D. J.; Dahl, R.; Davis, M.; Lee, P. S.; Yang, L.; Nickols, H. H.; Cho, H. P.; Smith, L. H.; D'Souza, M. S. et al. Design and Synthesis of Systemically Active Metabotropic Glutamate Subtype-2 and -3 (mGlu2/3) Receptor Positive Allosteric Modulators (PAMs): Pharmacological Characterization and Assessment in a Rat Model of Cocaine Dependence J. Med. Chem. 2014, 57, 4154-4172 10.1021/jm5000563
    • (2014) J. Med. Chem. , vol.57 , pp. 4154-4172
    • Dhanya, R.-P.1    Sheffler, D.J.2    Dahl, R.3    Davis, M.4    Lee, P.S.5    Yang, L.6    Nickols, H.H.7    Cho, H.P.8    Smith, L.H.9    D'Souza, M.S.10
  • 267
    • 17144417749 scopus 로고    scopus 로고
    • 3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)-phenoxy]butoxy}phenyl)propanoic Acid: A Brain Penetrant Allosteric Potentiator at the Metabotropic Glutamate Receptor 2 (mGluR2)
    • Cube, R. V.; Vernier, J. M.; Hutchinson, J. H.; Gardner, M. F.; James, J. K.; Rowe, B. A.; Schaffhauser, H.; Daggett, L.; Pinkerton, A. B. 3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)-phenoxy]butoxy}phenyl)propanoic Acid: A Brain Penetrant Allosteric Potentiator at the Metabotropic Glutamate Receptor 2 (mGluR2) Bioorg. Med. Chem. Lett. 2005, 15, 2389-2393 10.1016/j.bmcl.2005.02.078
    • (2005) Bioorg. Med. Chem. Lett. , vol.15 , pp. 2389-2393
    • Cube, R.V.1    Vernier, J.M.2    Hutchinson, J.H.3    Gardner, M.F.4    James, J.K.5    Rowe, B.A.6    Schaffhauser, H.7    Daggett, L.8    Pinkerton, A.B.9
  • 268
    • 77955717226 scopus 로고    scopus 로고
    • The mGluR2 Positive Allosteric Modulator BINA Decreases Cocaine Self-Administration and Cue-Induced Cocaine-Seeking and Counteracts Cocaine-Induced Enhancement of Brain Reward Function in Rats
    • Jin, X.; Semenova, S.; Yang, L.; Ardecky, R.; Sheffler, D. J.; Dahl, R.; Conn, P. J.; Cosford, N. D.; Markou, A. The mGluR2 Positive Allosteric Modulator BINA Decreases Cocaine Self-Administration and Cue-Induced Cocaine-Seeking and Counteracts Cocaine-Induced Enhancement of Brain Reward Function in Rats Neuropsychopharmacology 2010, 35, 2021-2036 10.1038/npp.2010.82
    • (2010) Neuropsychopharmacology , vol.35 , pp. 2021-2036
    • Jin, X.1    Semenova, S.2    Yang, L.3    Ardecky, R.4    Sheffler, D.J.5    Dahl, R.6    Conn, P.J.7    Cosford, N.D.8    Markou, A.9
  • 269
  • 273
    • 84867770282 scopus 로고    scopus 로고
    • Discovery of 3-Cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): A Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor
    • Cid, J. M.; Tresadern, G.; Vega, J. A.; de Lucas, A. I.; Matesanz, E.; Iturrino, L.; Linares, M. L.; Garcia, A.; Andrés, J. I.; Macdonald, G. J. et al. Discovery of 3-Cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): A Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor J. Med. Chem. 2012, 55, 8770-8789 10.1021/jm3010724
    • (2012) J. Med. Chem. , vol.55 , pp. 8770-8789
    • Cid, J.M.1    Tresadern, G.2    Vega, J.A.3    De Lucas, A.I.4    Matesanz, E.5    Iturrino, L.6    Linares, M.L.7    Garcia, A.8    Andrés, J.I.9    Macdonald, G.J.10
  • 275
    • 84867805389 scopus 로고    scopus 로고
    • Synthesis, Evaluation, and Radiolabeling of New Potent Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2 as Potential Tracers for Positron Emission Tomography Imaging
    • Andrés, J. I.; Alcázar, J.; Cid, J. M.; De Angelis, M.; Iturrino, L.; Langlois, X.; Lavreysen, H.; Trabanco, A. A.; Celen, S.; Bormans, G. Synthesis, Evaluation, and Radiolabeling of New Potent Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2 as Potential Tracers for Positron Emission Tomography Imaging J. Med. Chem. 2012, 55, 8685-8699 10.1021/jm300912k
    • (2012) J. Med. Chem. , vol.55 , pp. 8685-8699
    • Andrés, J.I.1    Alcázar, J.2    Cid, J.M.3    De Angelis, M.4    Iturrino, L.5    Langlois, X.6    Lavreysen, H.7    Trabanco, A.A.8    Celen, S.9    Bormans, G.10
  • 276
    • 84858052780 scopus 로고    scopus 로고
    • Discovery of 1,4-Disubstituted 3-Cyano-2-pyridones: A New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor
    • Cid, J. M.; Duvey, G.; Tresadern, G.; Nhem, V.; Furnari, R.; Cluzeau, P.; Vega, J. A.; de Lucas, A. I.; Matesanz, E.; Alonso, J. M. et al. Discovery of 1,4-Disubstituted 3-Cyano-2-pyridones: A New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor J. Med. Chem. 2012, 55, 2388-2405 10.1021/jm2016864
    • (2012) J. Med. Chem. , vol.55 , pp. 2388-2405
    • Cid, J.M.1    Duvey, G.2    Tresadern, G.3    Nhem, V.4    Furnari, R.5    Cluzeau, P.6    Vega, J.A.7    De Lucas, A.I.8    Matesanz, E.9    Alonso, J.M.10
  • 277
    • 84885573617 scopus 로고    scopus 로고
    • (Press Release). Addex Pharmaceuticals, Nov 5, available at (accessed Sep 1, 2015)
    • Addex Reports Top-line Data from a Successful Phase 2a Clinical Study with ADX71149 in Schizophrenia Patients (Press Release). Addex Pharmaceuticals, Nov 5, 2012; available at http://www.addextherapeutics.com/investors/press-releases/news-details/article/addex-reports-top-line-data-from-a-successful-phase-2a-clinical-study-with-adx71149-in-schizophrenia/ (accessed Sep 1, 2015).
    • (2012) Addex Reports Top-line Data from A Successful Phase 2a Clinical Study with ADX71149 in Schizophrenia Patients
  • 278
    • 84905406625 scopus 로고    scopus 로고
    • Discovery of 1-Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor
    • Cid, J. M.; Tresadern, G.; Duvey, G.; Lütjens, R.; Finn, T.; Rocher, J. P.; Poli, S.; Vega, J. A.; de Lucas, A. I.; Matesanz, E. et al. Discovery of 1-Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor J. Med. Chem. 2014, 57, 6495-6512 10.1021/jm500496m
    • (2014) J. Med. Chem. , vol.57 , pp. 6495-6512
    • Cid, J.M.1    Tresadern, G.2    Duvey, G.3    Lütjens, R.4    Finn, T.5    Rocher, J.P.6    Poli, S.7    Vega, J.A.8    De Lucas, A.I.9    Matesanz, E.10
  • 283
    • 84974580395 scopus 로고    scopus 로고
    • The structure of AZD8529 can be found at PubChem (CID 25125217): (accessed Sep 2)
    • The structure of AZD8529 can be found at PubChem (CID 25125217): http://pubchem.ncbi.nlm.nih.gov/compound/25125217 (accessed Sep 2, 2015).
    • (2015)
  • 284
    • 84941026458 scopus 로고    scopus 로고
    • The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys
    • Justinova, Z.; Panlilio, L. V.; Secci, M. E.; Redhi, G. H.; Schindler, C. W.; Cross, A. J.; Mrzljak, L.; Medd, A.; Shaham, Y.; Goldberg, S. R. The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys Biol. Psychiatry 2015, 78, 452-462 10.1016/j.biopsych.2015.01.014
    • (2015) Biol. Psychiatry , vol.78 , pp. 452-462
    • Justinova, Z.1    Panlilio, L.V.2    Secci, M.E.3    Redhi, G.H.4    Schindler, C.W.5    Cross, A.J.6    Mrzljak, L.7    Medd, A.8    Shaham, Y.9    Goldberg, S.R.10
  • 288
    • 84929207618 scopus 로고    scopus 로고
    • Deletion of Metabotropic Glutamate Receptors 2 and 3 (mGlu2 & mGlu3) in Mice Disrupts Sleep and Wheel-Running Activity, and Increases the Sensitivity of the Circadian System to Light
    • Pritchett, D.; Jagannath, A.; Brown, L. A.; Tam, S. K. E.; Hasan, S.; Gatti, S.; Harrison, P. J.; Bannerman, D. M.; Foster, R. G.; Peirson, S. N. Deletion of Metabotropic Glutamate Receptors 2 and 3 (mGlu2 & mGlu3) in Mice Disrupts Sleep and Wheel-Running Activity, and Increases the Sensitivity of the Circadian System to Light PLoS One 2015, 10, e0125523 10.1371/journal.pone.0125523
    • (2015) PLoS One , vol.10 , pp. e0125523
    • Pritchett, D.1    Jagannath, A.2    Brown, L.A.3    Tam, S.K.E.4    Hasan, S.5    Gatti, S.6    Harrison, P.J.7    Bannerman, D.M.8    Foster, R.G.9    Peirson, S.N.10
  • 289
    • 78149284597 scopus 로고    scopus 로고
    • Synthesis and Characterization of 1,3-d = Dihydro-benzo[b][1,4]diazepin-2-one Derivatives: Part 4. in Vivo Active Potent and Selective Non-Competitive Metabotropic Glutamate Receptor 2/3 Antagonists
    • Woltering, T. J.; Wichmann, J.; Goetschi, E.; Knoflach, F.; Ballard, T. M.; Huwyler, J.; Gatti, S. Synthesis and Characterization of 1,3-d = Dihydro-benzo[b][1,4]diazepin-2-one Derivatives: Part 4. In Vivo Active Potent and Selective Non-Competitive Metabotropic Glutamate Receptor 2/3 Antagonists Bioorg. Med. Chem. Lett. 2010, 20, 6969-6974 10.1016/j.bmcl.2010.09.125
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 6969-6974
    • Woltering, T.J.1    Wichmann, J.2    Goetschi, E.3    Knoflach, F.4    Ballard, T.M.5    Huwyler, J.6    Gatti, S.7
  • 291
    • 84866401521 scopus 로고    scopus 로고
    • Cognitive Impairment in Major Depression and the mGlu2 Receptor as a Therapeutic Target
    • Goeldner, C.; Ballard, T. M.; Knoflach, F.; Wichmann, J.; Gatti, S.; Umbricht, D. Cognitive Impairment in Major Depression and the mGlu2 Receptor as a Therapeutic Target Neuropharmacology 2013, 64, 337-346 10.1016/j.neuropharm.2012.08.001
    • (2013) Neuropharmacology , vol.64 , pp. 337-346
    • Goeldner, C.1    Ballard, T.M.2    Knoflach, F.3    Wichmann, J.4    Gatti, S.5    Umbricht, D.6
  • 293
    • 84942254112 scopus 로고    scopus 로고
    • International Nonproprietary Names
    • For the structure of decoglurant, see: In; World Health Organization: Geneva, Switzerland, Vol
    • For the structure of decoglurant, see: International Nonproprietary Names. In WHO Drug Information; World Health Organization: Geneva, Switzerland, 2013; Vol. 27, No. 2, p 150.
    • (2013) WHO Drug Information , vol.27 , Issue.2 , pp. 150
  • 295
    • 84875192840 scopus 로고    scopus 로고
    • 5 Negative Allosteric Modulators: A Patent Review
    • 5 Negative Allosteric Modulators: A Patent Review Expert Opin. Ther. Pat. 2013, 23, 393-408 10.1517/13543776.2013.760544
    • (2013) Expert Opin. Ther. Pat. , vol.23 , pp. 393-408
    • Emmitte, K.A.1
  • 297
    • 84919435956 scopus 로고    scopus 로고
    • Molecular Switch Strategy Delivers Distinct Group II mGluR Allosteric Modulator Families
    • Presented at the, Indianapolis, IN, Sep 8-12, Article No. 268
    • Schann, S.; Manteau, B.; Franchet, C.; Frauli, M.; Mayer, S. Molecular Switch Strategy Delivers Distinct Group II mGluR Allosteric Modulator Families. Presented at the 246th ACS National Meeting and Exposition, Indianapolis, IN, Sep 8-12, 2013; Article No. 268.
    • (2013) 246th ACS National Meeting and Exposition
    • Schann, S.1    Manteau, B.2    Franchet, C.3    Frauli, M.4    Mayer, S.5
  • 299
    • 84921782484 scopus 로고    scopus 로고
    • Metabotropic Glutamate Receptor 3 Activation is Required for Long-Term Depression in Medial Prefrontal Cortex and Fear Extinction
    • Walker, A. G.; Wenthur, C. J.; Xiang, Z.; Rook, J. M.; Emmitte, K. A.; Niswender, C. M.; Lindsley, C. W.; Conn, P. J. Metabotropic Glutamate Receptor 3 Activation is Required for Long-Term Depression in Medial Prefrontal Cortex and Fear Extinction Proc. Natl. Acad. Sci. U. S. A. 2015, 112, 1196-1201 10.1073/pnas.1416196112
    • (2015) Proc. Natl. Acad. Sci. U. S. A. , vol.112 , pp. 1196-1201
    • Walker, A.G.1    Wenthur, C.J.2    Xiang, Z.3    Rook, J.M.4    Emmitte, K.A.5    Niswender, C.M.6    Lindsley, C.W.7    Conn, P.J.8
  • 300
    • 84942279943 scopus 로고    scopus 로고
    • Discovery of VU0650786: A Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents
    • Engers, J. L.; Rodriguez, A. L.; Konkol, L. C.; Morrison, R. D.; Thompson, A. D.; Byers, F. W.; Blobaum, A. L.; Chang, S.; Venable, D. F.; Loch, M. T. et al. Discovery of VU0650786: A Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents J. Med. Chem. 2015, 58, 7485-7500 10.1021/acs.jmedchem.5b01005
    • (2015) J. Med. Chem. , vol.58 , pp. 7485-7500
    • Engers, J.L.1    Rodriguez, A.L.2    Konkol, L.C.3    Morrison, R.D.4    Thompson, A.D.5    Byers, F.W.6    Blobaum, A.L.7    Chang, S.8    Venable, D.F.9    Loch, M.T.10
  • 301
    • 84894071937 scopus 로고    scopus 로고
    • Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator
    • Zhang, L.; Balan, G.; Barreiro, G.; Boscoe, B. P.; Chenard, L. K.; Cianfrogna, J.; Claffey, M. M.; Chen, L.; Coffman, K. J.; Drozda, S. E. et al. Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator J. Med. Chem. 2014, 57, 861-877 10.1021/jm401622k
    • (2014) J. Med. Chem. , vol.57 , pp. 861-877
    • Zhang, L.1    Balan, G.2    Barreiro, G.3    Boscoe, B.P.4    Chenard, L.K.5    Cianfrogna, J.6    Claffey, M.M.7    Chen, L.8    Coffman, K.J.9    Drozda, S.E.10
  • 302
    • 84940105369 scopus 로고    scopus 로고
    • Identification of Glutathione Conjugates of Acetylene-Containing Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5
    • Zhuo, X.; Huang, X. S.; Degnan, A. P.; Snyder, L. B.; Yang, F.; Huang, H.; Shu, Y.-Z.; Johnson, B. M. Identification of Glutathione Conjugates of Acetylene-Containing Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Drug Metab. Dispos. 2015, 43, 578-589 10.1124/dmd.114.061879
    • (2015) Drug Metab. Dispos. , vol.43 , pp. 578-589
    • Zhuo, X.1    Huang, X.S.2    Degnan, A.P.3    Snyder, L.B.4    Yang, F.5    Huang, H.6    Shu, Y.-Z.7    Johnson, B.M.8
  • 305
    • 84948807651 scopus 로고    scopus 로고
    • Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2
    • Felts, A. S.; Rodriguez, A. L.; Smith, K. A.; Engers, J. L.; Morrison, R. D.; Byers, F. W.; Blobaum, A. L.; Locuson, C. W.; Chang, S.; Venable, D. F. et al. Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2 J. Med. Chem. 2015, 58, 9027-9040 10.1021/acs.jmedchem.5b01371
    • (2015) J. Med. Chem. , vol.58 , pp. 9027-9040
    • Felts, A.S.1    Rodriguez, A.L.2    Smith, K.A.3    Engers, J.L.4    Morrison, R.D.5    Byers, F.W.6    Blobaum, A.L.7    Locuson, C.W.8    Chang, S.9    Venable, D.F.10
  • 306
    • 84864472836 scopus 로고    scopus 로고
    • 4 Receptor Provides Functional Neuroprotection in the 6-Hydroxydopamine Rat Model of Parkinson's Disease
    • 4 Receptor Provides Functional Neuroprotection in the 6-Hydroxydopamine Rat Model of Parkinson's Disease Br. J. Pharmacol. 2012, 166, 2317-2330 10.1111/j.1476-5381.2012.01943.x
    • (2012) Br. J. Pharmacol. , vol.166 , pp. 2317-2330
    • Betts, M.J.1    O'Neill, M.J.2    Duty, S.3
  • 309
    • 84905057310 scopus 로고    scopus 로고
    • Characterization of the Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 ADX88178 in Rodent Models of Neuropsychiatric Disorders
    • Kalinichev, M.; Le Poul, E.; Bolea, C.; Girard, F.; Campo, B.; Fonsi, M.; Royer-Urios, I.; Browne, S. E.; Uslaner, J. M.; Davis, M. J. et al. Characterization of the Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 ADX88178 in Rodent Models of Neuropsychiatric Disorders J. Pharmacol. Exp. Ther. 2014, 350, 495-505 10.1124/jpet.114.214437
    • (2014) J. Pharmacol. Exp. Ther. , vol.350 , pp. 495-505
    • Kalinichev, M.1    Le Poul, E.2    Bolea, C.3    Girard, F.4    Campo, B.5    Fonsi, M.6    Royer-Urios, I.7    Browne, S.E.8    Uslaner, J.M.9    Davis, M.J.10
  • 314
    • 84947203145 scopus 로고    scopus 로고
    • Identification and Optimisation of a Series of Tetrahydrobenzotriazoles as Metabotropic Glutamate Receptor 5-Selective Positive Allosteric Modulators that Improve Performance in a Preclinical Model of Cognition
    • Ellard, J. M.; Madin, A.; Philps, O.; Hopkin, M.; Henderson, S.; Birch, L.; O'Connor, D.; Arai, T.; Takase, K.; Morgan, L. et al. Identification and Optimisation of a Series of Tetrahydrobenzotriazoles as Metabotropic Glutamate Receptor 5-Selective Positive Allosteric Modulators that Improve Performance in a Preclinical Model of Cognition Bioorg. Med. Chem. Lett. 2015, 25, 5792-5796 10.1016/j.bmcl.2015.10.050
    • (2015) Bioorg. Med. Chem. Lett. , vol.25 , pp. 5792-5796
    • Ellard, J.M.1    Madin, A.2    Philps, O.3    Hopkin, M.4    Henderson, S.5    Birch, L.6    O'Connor, D.7    Arai, T.8    Takase, K.9    Morgan, L.10
  • 315
    • 80052509542 scopus 로고    scopus 로고
    • A New Lead from Genetic Studies in Depressed Siblings: Assessing Studies of Chromosome 3
    • Hamilton, S. P. A New Lead From Genetic Studies in Depressed Siblings: Assessing Studies of Chromosome 3 Am. J. Psychiatry 2011, 168, 783-789 10.1176/appi.ajp.2011.11060835
    • (2011) Am. J. Psychiatry , vol.168 , pp. 783-789
    • Hamilton, S.P.1
  • 318
    • 57349087268 scopus 로고    scopus 로고
    • Genome-Wide Association Study of Response to Methylphenidate in 187 Children with Attention-Deficit/Hyperactivity Disorder
    • Mick, E.; Neale, B.; Middleton, F. A.; McGough, J. J.; Faraone, S. V. Genome-Wide Association Study of Response to Methylphenidate in 187 Children with Attention-Deficit/Hyperactivity Disorder Am. J. Med. Genet., Part B 2008, 147B, 1412 10.1002/ajmg.b.30865
    • (2008) Am. J. Med. Genet., Part B , vol.147 , pp. 1412
    • Mick, E.1    Neale, B.2    Middleton, F.A.3    McGough, J.J.4    Faraone, S.V.5
  • 319
    • 84872339618 scopus 로고    scopus 로고
    • Role of Metabotropic Glutamate Receptor 7 in Autism Spectrum Disorders: A Pilot Study
    • Yang, Y.; Pan, C. Role of Metabotropic Glutamate Receptor 7 in Autism Spectrum Disorders: A Pilot Study Life Sci. 2013, 92, 149-153 10.1016/j.lfs.2012.11.010
    • (2013) Life Sci. , vol.92 , pp. 149-153
    • Yang, Y.1    Pan, C.2
  • 320
    • 84901274038 scopus 로고    scopus 로고
    • The Metabotropic Glutamate Receptor Subtype 7 rs3792452 Polymorphism is Associated with the Response to Methylphenidate in Children with Attention-Deficit/Hyperactivity Disorder
    • Park, S.; Kim, B. N.; Cho, S. C.; Kim, J. W.; Kim, J. I.; Shin, M. S.; Yoo, H. J.; Han, D. H.; Cheong, J. H. The Metabotropic Glutamate Receptor Subtype 7 rs3792452 Polymorphism is Associated with the Response to Methylphenidate in Children with Attention-Deficit/Hyperactivity Disorder J. Child Adolesc. Psychopharmacol. 2014, 24, 223-227 10.1089/cap.2013.0079
    • (2014) J. Child Adolesc. Psychopharmacol. , vol.24 , pp. 223-227
    • Park, S.1    Kim, B.N.2    Cho, S.C.3    Kim, J.W.4    Kim, J.I.5    Shin, M.S.6    Yoo, H.J.7    Han, D.H.8    Cheong, J.H.9
  • 323
    • 64649098447 scopus 로고    scopus 로고
    • Association Study of Polymorphisms in the Group III Metabotropic Glutamate Receptor Genes, GRM4 and GRM7, with Schizophrenia
    • Shibata, H.; Tani, A.; Chikuhara, T.; Kikuta, R.; Sakai, M.; Ninomiya, H.; Tashiro, N.; Iwata, N.; Ozaki, N.; Fukumaki, Y. Association Study of Polymorphisms in the Group III Metabotropic Glutamate Receptor Genes, GRM4 and GRM7, with Schizophrenia Psychiatry Res. 2009, 167, 88-96 10.1016/j.psychres.2007.12.002
    • (2009) Psychiatry Res. , vol.167 , pp. 88-96
    • Shibata, H.1    Tani, A.2    Chikuhara, T.3    Kikuta, R.4    Sakai, M.5    Ninomiya, H.6    Tashiro, N.7    Iwata, N.8    Ozaki, N.9    Fukumaki, Y.10
  • 325
    • 84923218060 scopus 로고    scopus 로고
    • Evidence for Schizophrenia Susceptibility Alleles in the Indian Population: An Association of Neurodevelopmental Genes in Case-Control and Familial Samples
    • Jajodia, A.; Kaur, H.; Kumari, K.; Gupta, M.; Baghel, R.; Srivastava, A.; Sood, M.; Chadda, R. K.; Jain, S.; Kukreti, R. Evidence for Schizophrenia Susceptibility Alleles in the Indian Population: An Association of Neurodevelopmental Genes in Case-Control and Familial Samples Schizophr. Res. 2015, 162, 112-117 10.1016/j.schres.2014.12.031
    • (2015) Schizophr. Res. , vol.162 , pp. 112-117
    • Jajodia, A.1    Kaur, H.2    Kumari, K.3    Gupta, M.4    Baghel, R.5    Srivastava, A.6    Sood, M.7    Chadda, R.K.8    Jain, S.9    Kukreti, R.10
  • 326
    • 84901610692 scopus 로고    scopus 로고
    • Allelic Association, DNA Resequencing and Copy Number Variation at the Metabotropic Glutamate Receptor GRM7 Gene Locus in Bipolar Disorder
    • Kandaswamy, R.; McQuillin, A.; Curtis, D.; Gurling, H. Allelic Association, DNA Resequencing and Copy Number Variation at the Metabotropic Glutamate Receptor GRM7 Gene Locus in Bipolar Disorder Am. J. Med. Genet., Part B 2014, 165, 365-372 10.1002/ajmg.b.32239
    • (2014) Am. J. Med. Genet., Part B , vol.165 , pp. 365-372
    • Kandaswamy, R.1    McQuillin, A.2    Curtis, D.3    Gurling, H.4
  • 330
  • 332
    • 84918494690 scopus 로고    scopus 로고
    • Identification of Positive Allosteric Modulators VU0155094 (ML397) and VU0422288 (ML396) Reveals New Insights into the Biology of Metabotropic Glutamate Receptor 7
    • Jalan-Sakrikar, N.; Field, J. R.; Klar, R.; Mattmann, M. E.; Gregory, K. J.; Zamorano, R.; Engers, D. W.; Bollinger, S. R.; Weaver, C. D.; Days, E. L. et al. Identification of Positive Allosteric Modulators VU0155094 (ML397) and VU0422288 (ML396) Reveals New Insights Into the Biology of Metabotropic Glutamate Receptor 7 ACS Chem. Neurosci. 2014, 5, 1221-1237 10.1021/cn500153z
    • (2014) ACS Chem. Neurosci. , vol.5 , pp. 1221-1237
    • Jalan-Sakrikar, N.1    Field, J.R.2    Klar, R.3    Mattmann, M.E.4    Gregory, K.J.5    Zamorano, R.6    Engers, D.W.7    Bollinger, S.R.8    Weaver, C.D.9    Days, E.L.10
  • 333
    • 40849116128 scopus 로고    scopus 로고
    • Group III mGluR Regulation of Synaptic Transmission at the SC-CA1 Synapse is Developmentally Regulated
    • Ayala, J. E.; Niswender, C. M.; Luo, Q.; Banko, J. L.; Conn, P. J. Group III mGluR Regulation of Synaptic Transmission at the SC-CA1 Synapse is Developmentally Regulated Neuropharmacology 2008, 54, 804 10.1016/j.neuropharm.2007.12.009
    • (2008) Neuropharmacology , vol.54 , pp. 804
    • Ayala, J.E.1    Niswender, C.M.2    Luo, Q.3    Banko, J.L.4    Conn, P.J.5
  • 334
    • 0026344031 scopus 로고
    • Agonists at Metabotropic Glutamate Receptors Presynaptically Inhibit EPSCs in Neonatal Rat Hippocampus
    • Baskys, A.; Malenka, R. C. Agonists at Metabotropic Glutamate Receptors Presynaptically Inhibit EPSCs in Neonatal Rat Hippocampus J. Physiol. 1991, 444, 687-701 10.1113/jphysiol.1991.sp018901
    • (1991) J. Physiol. , vol.444 , pp. 687-701
    • Baskys, A.1    Malenka, R.C.2
  • 335
    • 84929380172 scopus 로고    scopus 로고
    • Activation of Metabotropic Glutamate Receptor 7 is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the hippocampus
    • Klar, R.; Walker, A. G.; Ghose, D.; Grueter, B. A.; Engers, D. W.; Hopkins, C. R.; Lindsley, C. W.; Xiang, Z.; Conn, P. J.; Niswender, C. M. Activation of Metabotropic Glutamate Receptor 7 is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the hippocampus J. Neurosci. 2015, 35, 7600-7615 10.1523/JNEUROSCI.4543-14.2015
    • (2015) J. Neurosci. , vol.35 , pp. 7600-7615
    • Klar, R.1    Walker, A.G.2    Ghose, D.3    Grueter, B.A.4    Engers, D.W.5    Hopkins, C.R.6    Lindsley, C.W.7    Xiang, Z.8    Conn, P.J.9    Niswender, C.M.10
  • 336
    • 84899024860 scopus 로고    scopus 로고
    • Blocking Metabotropic Glutamate Receptor Subtype 7 (mGlu7) via the Venus Flytrap Domain (VFTD) Inhibits Amygdala Plasticity, Stress, and Anxiety-Related Behavior
    • Gee, C. E.; Peterlik, D.; Neuhäuser, C.; Bouhelal, R.; Kaupmann, K.; Laue, G.; Uschold-Schmidt, N.; Feuerbach, D.; Zimmermann, K.; Ofner, S. et al. Blocking Metabotropic Glutamate Receptor Subtype 7 (mGlu7) via the Venus Flytrap Domain (VFTD) Inhibits Amygdala Plasticity, Stress, and Anxiety-Related Behavior J. Biol. Chem. 2014, 289, 10975-10987 10.1074/jbc.M113.542654
    • (2014) J. Biol. Chem. , vol.289 , pp. 10975-10987
    • Gee, C.E.1    Peterlik, D.2    Neuhäuser, C.3    Bouhelal, R.4    Kaupmann, K.5    Laue, G.6    Uschold-Schmidt, N.7    Feuerbach, D.8    Zimmermann, K.9    Ofner, S.10
  • 337
    • 34548848868 scopus 로고    scopus 로고
    • In Vitro Pharmacological Characterization of Novel Isoxazolopyridone Derivatives as Allosteric Metabotropic Glutamate Receptor 7 Antagonists
    • Suzuki, G.; Tsukamoto, N.; Fushiki, H.; Kawagishi, A.; Nakamura, M.; Kurihara, H.; Mitsuya, M.; Ohkubo, M.; Ohta, H. In Vitro Pharmacological Characterization of Novel Isoxazolopyridone Derivatives as Allosteric Metabotropic Glutamate Receptor 7 Antagonists J. Pharmacol. Exp. Ther. 2007, 323, 147-156 10.1124/jpet.107.124701
    • (2007) J. Pharmacol. Exp. Ther. , vol.323 , pp. 147-156
    • Suzuki, G.1    Tsukamoto, N.2    Fushiki, H.3    Kawagishi, A.4    Nakamura, M.5    Kurihara, H.6    Mitsuya, M.7    Ohkubo, M.8    Ohta, H.9
  • 338
    • 72249103001 scopus 로고    scopus 로고
    • Isoxazolopyridone Derivatives as Allosteric Metabotropic Glutamate Receptor 7 Antagonists
    • Nakamura, M.; Kurihara, H.; Suzuki, G.; Mitsuya, M.; Ohkubo, M.; Ohta, H. Isoxazolopyridone Derivatives as Allosteric Metabotropic Glutamate Receptor 7 Antagonists Bioorg. Med. Chem. Lett. 2010, 20, 726-729 10.1016/j.bmcl.2009.11.070
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 726-729
    • Nakamura, M.1    Kurihara, H.2    Suzuki, G.3    Mitsuya, M.4    Ohkubo, M.5    Ohta, H.6
  • 339
    • 84881248520 scopus 로고    scopus 로고
    • Synthesis and Evaluation of [11C]MMPIP as a Potential Radioligand for Imaging of Metabotropic Glutamate 7 Receptor in the Brain
    • Yamasaki, T.; Kumata, K.; Yui, J.; Fujinaga, M.; Furutsuka, K.; Hatori, A.; Xie, L.; Ogawa, M.; Nengaki, N. et al. Synthesis and Evaluation of [11C]MMPIP as a Potential Radioligand for Imaging of Metabotropic Glutamate 7 Receptor in the Brain EJNMMI Res. 2013, 3, 54 10.1186/2191-219X-3-54
    • (2013) EJNMMI Res. , vol.3 , pp. 54
    • Yamasaki, T.1    Kumata, K.2    Yui, J.3    Fujinaga, M.4    Furutsuka, K.5    Hatori, A.6    Xie, L.7    Ogawa, M.8    Nengaki, N.9
  • 342
    • 0008218273 scopus 로고
    • Properties of Opiate Receptor Bindign in Rat Brain
    • Pert, C. B.; Snyder, S. H. Properties of Opiate Receptor Bindign in Rat Brain Proc. Natl. Acad. Sci. U. S. A. 1973, 70, 2243-2247 10.1073/pnas.70.8.2243
    • (1973) Proc. Natl. Acad. Sci. U. S. A. , vol.70 , pp. 2243-2247
    • Pert, C.B.1    Snyder, S.H.2
  • 343
    • 0024847889 scopus 로고
    • Site-Directed Mutagenesis of M1 Muscarinic Acetylcholine Receptors: Conserved Aspartic Acids Play Important Roles in Receptor Function
    • Fraser, C. M.; Wang, C.-D.; Robinson, D. A.; Gocayne, J. D.; Venter, J. C. Site-Directed Mutagenesis of M1 Muscarinic Acetylcholine Receptors: Conserved Aspartic Acids Play Important Roles in Receptor Function Mol. Pharmacol. 1989, 36, 840-847
    • (1989) Mol. Pharmacol. , vol.36 , pp. 840-847
    • Fraser, C.M.1    Wang, C.-D.2    Robinson, D.A.3    Gocayne, J.D.4    Venter, J.C.5
  • 345
    • 84935507594 scopus 로고    scopus 로고
    • Characterization of Imidazopyridine Compounds as Negative Allosteric Modulators of Proton-Sensign GPR4 in Extracellular Acidification-Induced Responses
    • Tobo, A.; Tobo, M.; Nakakura, T.; Ebara, M.; Tomura, H.; Mogi, C.; Im, D.-S.; Murata, N.; Kuwabara, A.; Ito, S. et al. Characterization of Imidazopyridine Compounds as Negative Allosteric Modulators of Proton-Sensign GPR4 in Extracellular Acidification-Induced Responses PLoS One 2015, 10, e0129334 10.1371/journal.pone.0129334
    • (2015) PLoS One , vol.10 , pp. e0129334
    • Tobo, A.1    Tobo, M.2    Nakakura, T.3    Ebara, M.4    Tomura, H.5    Mogi, C.6    Im, D.-S.7    Murata, N.8    Kuwabara, A.9    Ito, S.10


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.