-
1
-
-
77949516412
-
Metabotropic glutamate receptors: Physiology, pharmacology, and disease
-
Niswender, C. M.; Conn, J. P. Metabotropic glutamate receptors: physiology, pharmacology, and disease Annu. Rev. Pharmacol. Toxicol. 2010, 50, 295-322
-
(2010)
Annu. Rev. Pharmacol. Toxicol.
, vol.50
, pp. 295-322
-
-
Niswender, C.M.1
Conn, J.P.2
-
2
-
-
38949115944
-
Mood disorders: Regulation by metabotropic glutamate receptors
-
Pilc, A.; Chaki, S.; Nowak, G.; Witkin, J. M. Mood disorders: regulation by metabotropic glutamate receptors Biochem. Pharmacol. 2008, 75, 997-1006
-
(2008)
Biochem. Pharmacol.
, vol.75
, pp. 997-1006
-
-
Pilc, A.1
Chaki, S.2
Nowak, G.3
Witkin, J.M.4
-
3
-
-
76849116197
-
Group 1 mGluR-dependent synaptic long-term depression: Mechanisms and implications for circuitry and disease
-
Lüscher, C.; Huber, K. M. Group 1 mGluR-dependent synaptic long-term depression: mechanisms and implications for circuitry and disease Neuron 2010, 65, 445-459
-
(2010)
Neuron
, vol.65
, pp. 445-459
-
-
Lüscher, C.1
Huber, K.M.2
-
4
-
-
84856072333
-
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
-
(2012)
Neuropharmacology
, vol.62
, pp. 1461-1472
-
-
Vinson, P.N.1
Conn, P.J.2
-
5
-
-
84857238962
-
Metabotropic glutamate receptors and the control of chronic pain
-
Chiechio, S.; Nicoletti, F. Metabotropic glutamate receptors and the control of chronic pain Curr. Opin. Pharmacol. 2012, 12, 28-34
-
(2012)
Curr. Opin. Pharmacol.
, vol.12
, pp. 28-34
-
-
Chiechio, S.1
Nicoletti, F.2
-
6
-
-
70349782435
-
Metabotropic glutamate receptor ligands as potential therapeutics for addiction
-
Foster, O. M. Metabotropic glutamate receptor ligands as potential therapeutics for addiction Curr. Drug Abuse Rev. 2009, 2, 83-98
-
(2009)
Curr. Drug Abuse Rev.
, vol.2
, pp. 83-98
-
-
Foster, O.M.1
-
7
-
-
75849152052
-
Glutamate receptors as therapeutic targets for Parkinsons disease
-
Johnson, K. A.; Conn, P. J.; Niswender, C. M. Glutamate receptors as therapeutic targets for Parkinsons disease CNS Neurol. Disord.: Drug Targets 2009, 8, 475-491
-
(2009)
CNS Neurol. Disord.: Drug Targets
, vol.8
, pp. 475-491
-
-
Johnson, K.A.1
Conn, P.J.2
Niswender, C.M.3
-
8
-
-
0033851295
-
L -Glutamate as a central neurotransmitter: Looking back
-
Watkins, J. C. l -Glutamate as a central neurotransmitter: looking back Biochem. Soc. Trans. 2000, 28, 297-310
-
(2000)
Biochem. Soc. Trans.
, vol.28
, pp. 297-310
-
-
Watkins, J.C.1
-
9
-
-
17744387125
-
Ionotropic and metabotropic glutamate receptor structure and pharmacology
-
Kew, J. N. C.; Kemp, J. A. Ionotropic and metabotropic glutamate receptor structure and pharmacology Psyhopharmacology 2005, 179, 4-29
-
(2005)
Psyhopharmacology
, vol.179
, pp. 4-29
-
-
Kew, J.N.C.1
Kemp, J.A.2
-
10
-
-
80053057994
-
Interdomain movements in metabotropic glutamate receptor activation
-
Huang, S.; Cao, J.; Jiang, M.; Labesse, G.; Liu, J.; Pin, J.-P.; Rondard, P. Interdomain movements in metabotropic glutamate receptor activation Proc. Natl. Acad. Sci. U.S.A. 2011, 108, 15480-15485
-
(2011)
Proc. Natl. Acad. Sci. U.S.A.
, vol.108
, pp. 15480-15485
-
-
Huang, S.1
Cao, J.2
Jiang, M.3
Labesse, G.4
Liu, J.5
Pin, J.-P.6
Rondard, P.7
-
11
-
-
0038662595
-
Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors
-
Pin, J. P.; Galvez, T.; Prezeau, L. Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors Pharmacol. Ther. 2003, 98, 325-354
-
(2003)
Pharmacol. Ther.
, vol.98
, pp. 325-354
-
-
Pin, J.P.1
Galvez, T.2
Prezeau, L.3
-
12
-
-
33845973375
-
Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors
-
Brauner-Osborne, H.; Wellendorph, P.; Jensen, A. A. Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors Curr. Drug Targets 2007, 8, 169-184
-
(2007)
Curr. Drug Targets
, vol.8
, pp. 169-184
-
-
Brauner-Osborne, H.1
Wellendorph, P.2
Jensen, A.A.3
-
13
-
-
0033844601
-
Regulation of neurotransmitter release by metabotropic glutamate receptors
-
Cartmell, J.; Schoepp, D. D. Regulation of neurotransmitter release by metabotropic glutamate receptors J. Neurochem. 2000, 75, 889-907
-
(2000)
J. Neurochem.
, vol.75
, pp. 889-907
-
-
Cartmell, J.1
Schoepp, D.D.2
-
14
-
-
0027190384
-
Distribution of the messenger RNA for metabotropic glutamate receptor, mGlu2, in the central nervous system of the rat
-
Ohishi, H.; Shigemoto, R.; Nakanishi, S.; Mizuno, N. Distribution of the messenger RNA for metabotropic glutamate receptor, mGlu2, in the central nervous system of the rat Neuroscience 1993, 53, 1009-1018
-
(1993)
Neuroscience
, vol.53
, pp. 1009-1018
-
-
Ohishi, H.1
Shigemoto, R.2
Nakanishi, S.3
Mizuno, N.4
-
15
-
-
18444373887
-
35S]GTPγS binding
-
35S]GTPγS binding J. Comp. Neurol. 2005, 487, 15-27
-
(2005)
J. Comp. Neurol.
, vol.487
, pp. 15-27
-
-
Richards, G.1
Messer, J.2
Malherbe, P.3
Pink, R.4
Brockhaus, M.5
Stadler, H.6
Wichmann, J.7
Schaffhauser, H.J.8
Mutel, V.9
-
16
-
-
39149083048
-
Distribution of metabotropic glutamate 2 and 3 receptors in the rat forebrain: Implication in emotional responses and central disinhibition
-
Gu, G.; Lorrain, D. S.; Wei, H.; Cole, R. L.; Zhang, X.; Daggett, L. P.; Schaffhauser, H. J.; Bristow, L. J.; Lechner, S. M. Distribution of metabotropic glutamate 2 and 3 receptors in the rat forebrain: implication in emotional responses and central disinhibition Brain Res. 2008, 1197, 47-62
-
(2008)
Brain Res.
, vol.1197
, pp. 47-62
-
-
Gu, G.1
Lorrain, D.S.2
Wei, H.3
Cole, R.L.4
Zhang, X.5
Daggett, L.P.6
Schaffhauser, H.J.7
Bristow, L.J.8
Lechner, S.M.9
-
17
-
-
67649981850
-
Differential expression of metabotropic glutamate receptors 2 and 3 in schizophrenia: A mechanism for antipsychotic drug action?
-
Ghose, S.; Gleason, K. A.; Potts, B. W.; Lewis-Amezcua, K.; Tamminga, C. A. Differential expression of metabotropic glutamate receptors 2 and 3 in schizophrenia: a mechanism for antipsychotic drug action? Am. J. Psychiatry 2009, 166, 812-820
-
(2009)
Am. J. Psychiatry
, vol.166
, pp. 812-820
-
-
Ghose, S.1
Gleason, K.A.2
Potts, B.W.3
Lewis-Amezcua, K.4
Tamminga, C.A.5
-
18
-
-
79953311403
-
Targeting of metabotropic glutamate receptors for the treatment of schizophrenia
-
Shigeyuki, C.; Hirohiko, H. Targeting of metabotropic glutamate receptors for the treatment of schizophrenia Curr. Pharm. Des. 2011, 17, 94-102
-
(2011)
Curr. Pharm. Des.
, vol.17
, pp. 94-102
-
-
Shigeyuki, C.1
Hirohiko, H.2
-
19
-
-
15644369847
-
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 roperties
-
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.; Griffey, K. R.; Tizzano, J. P.; Kallman, M. J.; Helton, D. R.; Schoepp, D. D. 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 roperties J. Med. Chem. 1997, 40, 528-537
-
(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
Griffey, K.R.11
Tizzano, J.P.12
Kallman, M.J.13
Helton, D.R.14
Schoepp, D.D.15
-
20
-
-
14044258729
-
Glutamate receptors as novel targets for anxiety and stress disorders
-
Swanson, C. J.; Bures, M.; Johnson, M. P.; Linden, A. M.; Monn, J. A.; Schoepp, D. D. Glutamate receptors as novel targets for anxiety and stress disorders Nat. Rev. Drug Discovery 2005, 4, 131-144
-
(2005)
Nat. Rev. Drug Discovery
, vol.4
, pp. 131-144
-
-
Swanson, C.J.1
Bures, M.2
Johnson, M.P.3
Linden, A.M.4
Monn, J.A.5
Schoepp, D.D.6
-
21
-
-
84856097892
-
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
-
(2012)
Neuropharmacology
, vol.62
, pp. 1473-1483
-
-
Fell, M.J.1
McKinzie, D.L.2
Monn, J.A.3
Svensson, K.A.4
-
22
-
-
34948858402
-
Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: A randomized phase 2 clinical trial
-
Patil, S. T.; Zhang, L.; Martenyi, F.; Lowe, S. L.; Jackson, K. A.; Andreev, B. V.; Avedisova, A. S.; Bardenstein, L. M.; Gurovich, I. Y.; Morozova, M. A.; Mosolov, S. N.; Neznanov, N. G.; Reznik, A. M.; Smulevich, A. B.; Tochilov, V. A.; Johnson, B. G.; Monn, J. A.; Schoepp, D. D. Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized phase 2 clinical trial Nat. Med. 2007, 13, 1102-1107
-
(2007)
Nat. Med.
, vol.13
, pp. 1102-1107
-
-
Patil, S.T.1
Zhang, L.2
Martenyi, F.3
Lowe, S.L.4
Jackson, K.A.5
Andreev, B.V.6
Avedisova, A.S.7
Bardenstein, L.M.8
Gurovich, I.Y.9
Morozova, M.A.10
Mosolov, S.N.11
Neznanov, N.G.12
Reznik, A.M.13
Smulevich, A.B.14
Tochilov, V.A.15
Johnson, B.G.16
Monn, J.A.17
Schoepp, D.D.18
-
23
-
-
84873986434
-
-
During the preparation of this manuscript Eli Lilly and Company announced in a press release (August 29, 2012) the decision to stop the clinical studies investigating LY2140023 for the treatment of patients suffering from schizophrenia. The press release mentioned that the decision was made after a recently conducted independent futility analysis concluded that HBBN, the second of Lillys two pivotal studies, was unlikely to be positive in its primary efficacy endpoint if enrolled to completion. The decision was not based on any safety signals.
-
During the preparation of this manuscript Eli Lilly and Company announced in a press release (August 29, 2012) the decision to stop the clinical studies investigating LY2140023 for the treatment of patients suffering from schizophrenia. The press release mentioned that the decision was made after a recently conducted independent futility analysis concluded that HBBN, the second of Lillys two pivotal studies, was unlikely to be positive in its primary efficacy endpoint if enrolled to completion. The decision was not based on any safety signals. https://investor.lilly.com/releaseDetail.cfm?ReleaseID=703018.
-
-
-
-
24
-
-
0034757740
-
B receptors open new routes for the development of drugs targeting family 3 G-protein-coupled receptors
-
B receptors open new routes for the development of drugs targeting family 3 G-protein-coupled receptors Mol. Pharmacol. 2001, 60, 881-884
-
(2001)
Mol. Pharmacol.
, vol.60
, pp. 881-884
-
-
Pin, J.P.1
Parmentier, M.-L.2
Prezeau, L.3
-
26
-
-
79953899942
-
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
-
(2011)
Pharmacol. Rev.
, vol.63
, pp. 59-126
-
-
Urwyler, S.1
-
27
-
-
78751545477
-
Progress in the development of positive allosteric modulators of the metabotropic glutamate receptor 2
-
Trabanco, A. A.; Cid, J. M.; Lavreysen, H.; Macdonald, G. J.; Tresadern, G. Progress in the development of positive allosteric modulators of the metabotropic glutamate receptor 2 Curr. Med. Chem. 2011, 18, 47-68
-
(2011)
Curr. Med. Chem.
, vol.18
, pp. 47-68
-
-
Trabanco, A.A.1
Cid, J.M.2
Lavreysen, H.3
MacDonald, G.J.4
Tresadern, G.5
-
28
-
-
78751643006
-
New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): Identification and synthesis of N -propyl-8-chloro-6-substituted isoquinolones
-
Trabanco, A. A.; Duvey, G.; Cid, J. M.; Macdonald, G. J.; Cluzeau, P.; Nhem, V.; Furnari, R.; Behaj, N.; Poulain, G.; Finn, T.; Lavreysen, H.; Poli, S.; Raux, A.; Thollon, Y.; Poirier, N.; DAddona, D.; Andres, J. I.; Lutjens, R.; Le Poul, E.; Imogai, H.; Rocher, J.-P. New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): identification and synthesis of N -propyl-8-chloro-6-substituted isoquinolones Bioorg. Med. Chem. Lett. 2011, 21, 971-976
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 971-976
-
-
Trabanco, A.A.1
Duvey, G.2
Cid, J.M.3
MacDonald, G.J.4
Cluzeau, P.5
Nhem, V.6
Furnari, R.7
Behaj, N.8
Poulain, G.9
Finn, T.10
Lavreysen, H.11
Poli, S.12
Raux, A.13
Thollon, Y.14
Poirier, N.15
Daddona, D.16
Andres, J.I.17
Lutjens, R.18
Le Poul, E.19
Imogai, H.20
Rocher, J.-P.21
more..
-
29
-
-
79952493408
-
New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): Identification and synthesis of N -propyl-5-substituted isoquinolones
-
Trabanco, A. A.; Duvey, G.; Cid, J. M.; Macdonald, G. J.; Cluzeau, P.; Nhem, V.; Furnari, R.; Behaj, N.; Poulain, G.; Finn, T.; Poli, S.; Lavreysen, H.; Raux, A.; Thollon, Y.; Poirier, N.; DAddona, D.; Andrés, J. I.; Lutjens, R.; Le Poul, E.; Imogai, H.; Rocher, J.-P. New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): identification and synthesis of N -propyl-5-substituted isoquinolones Med. Chem. Commum. 2011, 2, 132-139
-
(2011)
Med. Chem. Commum.
, vol.2
, pp. 132-139
-
-
Trabanco, A.A.1
Duvey, G.2
Cid, J.M.3
MacDonald, G.J.4
Cluzeau, P.5
Nhem, V.6
Furnari, R.7
Behaj, N.8
Poulain, G.9
Finn, T.10
Poli, S.11
Lavreysen, H.12
Raux, A.13
Thollon, Y.14
Poirier, N.15
Daddona, D.16
Andrés, J.I.17
Lutjens, R.18
Le Poul, E.19
Imogai, H.20
Rocher, J.-P.21
more..
-
30
-
-
78650315615
-
Discovery of 1,5-disubstituted pyridones: A new class of positive allosteric modulators of the metabotropic glutamate 2 receptor
-
Cid, J. M.; Duvey, G.; Cluzeau, P.; Nhem, V.; Macary, K.; Raux, A.; Poirier, N.; Muller, J.; Bolea, C.; Finn, T.; Urios, I.; Epping-Jordan, M.; Chamelot, E.; Derouet, F.; Girard, F.; Macdonald, G. J.; Vega, J. A.; de Lucas, A. I.; Matesanz, E.; Lavreysen, H.; Linares, M. L.; Oehlrich, D.; Oyarzábal, J.; Tresadern, G.; Trabanco, A. A.; Andrés, J. I.; Le Poul, E.; Imogai, H.; Lutjens, R.; Rocher, J.-P. Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor ACS Chem. Neurosci. 2010, 1, 788-795
-
(2010)
ACS Chem. Neurosci.
, vol.1
, pp. 788-795
-
-
Cid, J.M.1
Duvey, G.2
Cluzeau, P.3
Nhem, V.4
MacAry, K.5
Raux, A.6
Poirier, N.7
Muller, J.8
Bolea, C.9
Finn, T.10
Urios, I.11
Epping-Jordan, M.12
Chamelot, E.13
Derouet, F.14
Girard, F.15
MacDonald, G.J.16
Vega, J.A.17
De Lucas, A.I.18
Matesanz, E.19
Lavreysen, H.20
Linares, M.L.21
Oehlrich, D.22
Oyarzábal, J.23
Tresadern, G.24
Trabanco, A.A.25
Andrés, J.I.26
Le Poul, E.27
Imogai, H.28
Lutjens, R.29
Rocher, J.-P.30
more..
-
31
-
-
84873992076
-
-
WO2006030032 A1.
-
Imogai, H. J.; Cid-Nuñez, J. M.; Duvey, G. A. J.; Bolea, C. M.; Nhem, V.; Finn, T. P.; Le Poul, E. C.; Rocher, J.-P. F. C.; Lutjens, R. J. Novel Pyridinone Derivatives and Their Preparation, Pharmaceutical Compositions, and Use as Positive Allosteric Modulators of mGluR2-Receptors for Treatment of Various Neurological and Psychiatric Disorders. WO2006030032 A1, 2006.
-
(2006)
Novel Pyridinone Derivatives and Their Preparation, Pharmaceutical Compositions, and Use As Positive Allosteric Modulators of mGluR2-Receptors for Treatment of Various Neurological and Psychiatric Disorders
-
-
Imogai, H.J.1
Cid-Nuñez, J.M.2
Duvey, G.A.J.3
Bolea, C.M.4
Nhem, V.5
Finn, T.P.6
Le Poul, E.C.7
Rocher, J.-P.F.C.8
Lutjens, R.J.9
-
32
-
-
84858052780
-
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.; Funary, R.; Cluzeau, P.; Vega, J. A.; de Lucas, A. I.; Matesanz, E.; Alonso, J. M.; Linares, M. L.; Andrés, J. I.; Poli, S.; Lutjens, R.; Imogai, H.; Rocher, J.-P.; Macdonald, G. J.; Oehlrich, D.; Lavreysen, H.; Ahnaou, A.; Drinkenburg, W.; Mackie, C.; Trabanco, A. A. 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
-
(2012)
J. Med. Chem.
, vol.55
, pp. 2388-2405
-
-
Cid, J.M.1
Duvey, G.2
Tresadern, G.3
Nhem, V.4
Funary, R.5
Cluzeau, P.6
Vega, J.A.7
De Lucas, A.I.8
Matesanz, E.9
Alonso, J.M.10
Linares, M.L.11
Andrés, J.I.12
Poli, S.13
Lutjens, R.14
Imogai, H.15
Rocher, J.-P.16
MacDonald, G.J.17
Oehlrich, D.18
Lavreysen, H.19
Ahnaou, A.20
Drinkenburg, W.21
MacKie, C.22
Trabanco, A.A.23
more..
-
33
-
-
78751517953
-
-
WO 2008107481 A1.
-
Cid-Nuñez, J. M.; Trabanco-Suárez, A. A.; Macdonald, G. J.; Duvey, G. A. J.; Lutjens, R. J. Preparation of 3-Cyano-4-(4-tetrahydropyran- phenyl)pyridin-2-one Derivatives as Positive mGluR2 Receptor Modulators. WO 2008107481 A1, 2008.
-
(2008)
Preparation of 3-Cyano-4-(4-tetrahydropyran-phenyl)pyridin-2-one Derivatives As Positive mGluR2 Receptor Modulators
-
-
Cid-Nuñez, J.M.1
Trabanco-Suárez, A.A.2
MacDonald, G.J.3
Duvey, G.A.J.4
Lutjens, R.J.5
-
34
-
-
84882912527
-
-
WO2007104783 A2.
-
Imogai, H. I.; Cid-Nuñez, J. M.; Andrés-Gil, J. I.; Trabanco-Suárez, A. A.; Oyarzábal-Santamarina, J.; Dautzenberg, F. M.; Macdonald, G. J.; Pullan, S. E.; Lutjens, R. J.; Duvey, G. A. J.; Nhem, V.; Finn, T. P.; Melikyan, G. 1,4-Disubstituted 3-Cyanopyridone Derivatives and Their Use as Positive Allosteric Modulators of mGlu2-Receptors and Their Preparation. WO2007104783 A2, 2007.
-
(2007)
1,4-Disubstituted 3-Cyanopyridone Derivatives and Their Use As Positive Allosteric Modulators of mGlu2-Receptors and Their Preparation
-
-
Imogai, H.I.1
Cid-Nuñez, J.M.2
Andrés-Gil, J.I.3
Trabanco-Suárez, A.A.4
Oyarzábal-Santamarina, J.5
Dautzenberg, F.M.6
MacDonald, G.J.7
Pullan, S.E.8
Lutjens, R.J.9
Duvey, G.A.J.10
Nhem, V.11
Finn, T.P.12
Melikyan, G.13
-
35
-
-
72149094340
-
Scaffold hopping from pyridones to imidazo[1,2- a ]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor
-
Tresadern, G.; Cid, J. M; Macdonald, G. J.; Vega, J. A.; de Lucas, A. I.; García, A.; Matesanz, E.; Linares, M. L.; Oehlrich, D.; Lavreysen, H.; Biesmans, I.; Trabanco, A. A. Scaffold hopping from pyridones to imidazo[1,2- a ]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor Bioorg. Med. Chem. Lett. 2010, 20, 175-179
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 175-179
-
-
Tresadern, G.1
Cid, J.M.2
MacDonald, G.J.3
Vega, J.A.4
De Lucas, A.I.5
García, A.6
Matesanz, E.7
Linares, M.L.8
Oehlrich, D.9
Lavreysen, H.10
Biesmans, I.11
Trabanco, A.A.12
-
36
-
-
84858735001
-
Imidazo[1,2- a ]pyridines: Orally active positive allosteric modulators of the metabotropic glutamate 2 receptor
-
Trabanco, A. A; Tresadern, G.; Macdonald, G. J.; Vega, J. A.; de Lucas, A. I.; Matesanz, E.; Garcia, A.; Linares, M. L.; Alonso de Diego, S. A.; Alonso, J. M.; Oehlrich, D.; Ahnaou, A.; Drinkenburg, W.; Mackie, C.; Andres, J. I.; Lavreysen, H.; Cid, J. M. Imidazo[1,2- a ]pyridines: orally active positive allosteric modulators of the metabotropic glutamate 2 receptor J. Med. Chem. 2012, 55, 2688-2701
-
(2012)
J. Med. Chem.
, vol.55
, pp. 2688-2701
-
-
Trabanco, A.A.1
Tresadern, G.2
MacDonald, G.J.3
Vega, J.A.4
De Lucas, A.I.5
Matesanz, E.6
Garcia, A.7
Linares, M.L.8
Alonso De Diego, S.A.9
Alonso, J.M.10
Oehlrich, D.11
Ahnaou, A.12
Drinkenburg, W.13
MacKie, C.14
Andres, J.I.15
Lavreysen, H.16
Cid, J.M.17
-
39
-
-
84925946285
-
-
WO2010130424 A1.
-
Cid-Nuñez, J. M.; Oehlrich, D.; Trabanco-Suárez, A. A.; Tresadern, G. J.; Vega-Ramiro, J. A.; Macdonald, G. J. 1,2,4-Triazolo[4,3- a ]pyridine Derivatives and Their Use for the Treatment or Prevention of Neurological Disorders. WO2010130424 A1, 2010.
-
(2010)
1,2,4-Triazolo[4,3- A ]Pyridine Derivatives and Their Use for the Treatment or Prevention of Neurological Disorders
-
-
Cid-Nuñez, J.M.1
Oehlrich, D.2
Trabanco-Suárez, A.A.3
Tresadern, G.J.4
Vega-Ramiro, J.A.5
MacDonald, G.J.6
-
40
-
-
84873997810
-
-
WO2010130423 A1.
-
Cid-Nuñez, J. M.; De Lucas-Olivares, A. I.; Trabanco-Suárez, A. A.; Macdonald, G. J. 7-Aryl-1,2,4-triazolo[4,3- a ]pyridine Derivatives and Their Use as Positive Allosteric Modulators of mGluR2 Receptors. WO2010130423 A1, 2010.
-
(2010)
7-Aryl-1,2,4-triazolo[4,3- A ]Pyridine Derivatives and Their Use As Positive Allosteric Modulators of mGluR2 Receptors
-
-
Cid-Nuñez, J.M.1
De Lucas-Olivares, A.I.2
Trabanco-Suárez, A.A.3
MacDonald, G.J.4
-
41
-
-
84873997810
-
-
WO2010130422 A1.
-
Cid-Nuñez, J. M.; De Lucas-Olivares, A. I.; Trabanco-Suárez, A. A.; Macdonald, G. J. 1,2,4-Triazolo[4,3- a ]pyridine Derivatives and Their Use as Positive Allosteric Modulators of mGluR2 Receptors. WO2010130422 A1, 2010.
-
(2010)
1,2,4-Triazolo[4,3- A ]Pyridine Derivatives and Their Use As Positive Allosteric Modulators of mGluR2 Receptors
-
-
Cid-Nuñez, J.M.1
De Lucas-Olivares, A.I.2
Trabanco-Suárez, A.A.3
MacDonald, G.J.4
-
42
-
-
39749181550
-
Generation of a set of simple, interpretable ADMET rules of thumb
-
Gleeson, M. P. Generation of a set of simple, interpretable ADMET rules of thumb J. Med. Chem. 2008, 51, 817-834
-
(2008)
J. Med. Chem.
, vol.51
, pp. 817-834
-
-
Gleeson, M.P.1
-
43
-
-
35748934487
-
The influence of drug-like concepts on decision-making in medicinal chemistry
-
Leeson, P. D.; Springthorpe, B. The influence of drug-like concepts on decision-making in medicinal chemistry Nat. Rev. Drug Discovery 2007, 6, 881-890
-
(2007)
Nat. Rev. Drug Discovery
, vol.6
, pp. 881-890
-
-
Leeson, P.D.1
Springthorpe, B.2
-
44
-
-
61649109015
-
The influence of lead discovery strategies on the properties of drug candidates
-
Keseru, G. M.; Makara, G. M. The influence of lead discovery strategies on the properties of drug candidates Nat. Rev. Drug Discovery 2009, 8, 203-212
-
(2009)
Nat. Rev. Drug Discovery
, vol.8
, pp. 203-212
-
-
Keseru, G.M.1
Makara, G.M.2
-
45
-
-
84856846240
-
Impact of lipophilic efficiency on compound quality
-
Tarcsay, A.; Nyiri, K.; Keseru, G. M. Impact of lipophilic efficiency on compound quality J. Med. Chem. 2012, 55, 1252-1260
-
(2012)
J. Med. Chem.
, vol.55
, pp. 1252-1260
-
-
Tarcsay, A.1
Nyiri, K.2
Keseru, G.M.3
-
46
-
-
33845467113
-
Changes in extracellular glutamate levels in rat orbitofrontal cortex during sleep and wakefulness
-
Lopez-Rodriguez, F.; Medina-Ceja, L.; Wilson, C. L.; Jhung, D.; Morales-Villagram, A. Changes in extracellular glutamate levels in rat orbitofrontal cortex during sleep and wakefulness Arch. Med. Res. 2007, 38, 52-55
-
(2007)
Arch. Med. Res.
, vol.38
, pp. 52-55
-
-
Lopez-Rodriguez, F.1
Medina-Ceja, L.2
Wilson, C.L.3
Jhung, D.4
Morales-Villagram, A.5
-
47
-
-
58249128334
-
Modulation of group II metabotropic glutamate receptor (mGlu2) elicits common changes in rat and mice sleep-wake architecture
-
Ahnaou, A.; Dautzenberg, F. M.; Geys, H.; Imogai, H.; Gibelin, A.; Moechars, D.; Steckler, T.; Drinkenburg, W. H. I. M. Modulation of group II metabotropic glutamate receptor (mGlu2) elicits common changes in rat and mice sleep-wake architecture Eur. J. Pharmacol. 2009, 603, 62-72
-
(2009)
Eur. J. Pharmacol.
, vol.603
, pp. 62-72
-
-
Ahnaou, A.1
Dautzenberg, F.M.2
Geys, H.3
Imogai, H.4
Gibelin, A.5
Moechars, D.6
Steckler, T.7
Drinkenburg, W.H.I.M.8
-
48
-
-
13244277592
-
The metabotropic glutamate (mGLU)2/3 receptor antagonist LY341495 [2 S -2-amino-2-(1 S,2 S -2-carboxycyclopropyl-1-yl)-3-(xanth-9-yl)propanoic acid] stimulates waking and fast electroencephalogram power and blocks the effects of the mGLU2/3 receptor agonist LY379268 [(-)-2-oxa-4-aminobicyclo[3.1.0]hexane-4, 6-dicarboxylate] in rats
-
Feinberg, I.; Schoepp, D. D.; Hsieh, K.-C.; Darchia, N.; Campbell, I. G. The metabotropic glutamate (mGLU)2/3 receptor antagonist LY341495 [2 S -2-amino-2-(1 S,2 S -2-carboxycyclopropyl-1-yl)-3-(xanth-9-yl)propanoic acid] stimulates waking and fast electroencephalogram power and blocks the effects of the mGLU2/3 receptor agonist LY379268 [(-)-2-oxa-4-aminobicyclo[3.1.0]hexane-4, 6-dicarboxylate] in rats J. Pharmacol. Exp. Ther. 2005, 312, 826-833
-
(2005)
J. Pharmacol. Exp. Ther.
, vol.312
, pp. 826-833
-
-
Feinberg, I.1
Schoepp, D.D.2
Hsieh, K.-C.3
Darchia, N.4
Campbell, I.G.5
-
49
-
-
78650769933
-
N -(4-((2-(Trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl) benzyl)-1-methyl-1 H -imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: In vivo profiling suggests a link between behavioral and central nervous system neurochemical changes
-
Fell, M. J.; Witkin, J. M.; Falcone, J. F.; Katner, J. S.; Perry, K. W.; Hart, J.; Rorick-Kehn, L.; Overshiner, C. D.; Rasmussen, K.; Chaney, S. F.; Benvenga, M. J.; Deanna, X. L.; Marlow, L.; Thompson, L. K.; Luecke, S. K.; Wafford, K. A.; Seidel, W. F.; Edgar, D. M.; Quets, A. T.; Felder, C. C.; Wang, X.; Heinz, B. A.; Nikolayev, A.; Kuo, M.-S.; Mayhugh, D.; Khilevich, A.; Zhang, D.; Ebert, P. J.; Eckstein, J. A.; Ackermann, B. L.; Swanson, S. P.; Catlow, J. T.; Dean, R. A.; Jackson, K.; Tauscher-Wisniewski, S.; Marek, G. J.; Schkeryantz, J. M.; Svensson, K. A. N -(4-((2-(Trifluoromethyl)-3-hydroxy-4- (isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1 H -imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: in vivo profiling suggests a link between behavioral and central nervous system neurochemical changes J. Pharmacol. Exp. Ther. 2011, 336, 165-177
-
(2011)
J. Pharmacol. Exp. Ther.
, vol.336
, pp. 165-177
-
-
Fell, M.J.1
Witkin, J.M.2
Falcone, J.F.3
Katner, J.S.4
Perry, K.W.5
Hart, J.6
Rorick-Kehn, L.7
Overshiner, C.D.8
Rasmussen, K.9
Chaney, S.F.10
Benvenga, M.J.11
Deanna, X.L.12
Marlow, L.13
Thompson, L.K.14
Luecke, S.K.15
Wafford, K.A.16
Seidel, W.F.17
Edgar, D.M.18
Quets, A.T.19
Felder, C.C.20
Wang, X.21
Heinz, B.A.22
Nikolayev, A.23
Kuo, M.-S.24
Mayhugh, D.25
Khilevich, A.26
Zhang, D.27
Ebert, P.J.28
Eckstein, J.A.29
Ackermann, B.L.30
Swanson, S.P.31
Catlow, J.T.32
Dean, R.A.33
Jackson, K.34
Tauscher-Wisniewski, S.35
Marek, G.J.36
Schkeryantz, J.M.37
Svensson, K.A.38
more..
-
50
-
-
80054109355
-
Comparative analysis of the neurophysiological profile of group II metabotropic glutamate receptor activators and diazepam: Effects on hippocampal and cortical EEG patterns in rats
-
Siok, C. J.; Cogan, S. M.; Shifflett, L. B.; Doran, A. C.; Kocsis, B.; Hajós, M. Comparative analysis of the neurophysiological profile of group II metabotropic glutamate receptor activators and diazepam: effects on hippocampal and cortical EEG patterns in rats Neuropharmacology 2012, 62, 226-236
-
(2012)
Neuropharmacology
, vol.62
, pp. 226-236
-
-
Siok, C.J.1
Cogan, S.M.2
Shifflett, L.B.3
Doran, A.C.4
Kocsis, B.5
Hajós, M.6
-
51
-
-
0031023562
-
Blockade of phencyclidine-induced hyperlocomotion by olanzapine, clozapine and serotonin receptor subtype selective antagonists in mice
-
Gleason, S. D.; Shannon, H. E. Blockade of phencyclidine-induced hyperlocomotion by olanzapine, clozapine and serotonin receptor subtype selective antagonists in mice Psychopharmacology 1997, 129, 79-84
-
(1997)
Psychopharmacology
, vol.129
, pp. 79-84
-
-
Gleason, S.D.1
Shannon, H.E.2
-
53
-
-
0005544365
-
Statistical Methods in Bioassay. Estimation of Relative Potency from Quantal Responses
-
In; Kotz, S. Jonhson, N. L. Wiley: New York.
-
Tsutakawa, R. K. Statistical Methods in Bioassay. Estimation of Relative Potency from Quantal Responses. In Encyclopaedia of Statistical Science; Kotz, S.; Jonhson, N. L., Eds.; Wiley: New York, 1982.
-
(1982)
Encyclopaedia of Statistical Science
-
-
Tsutakawa, R.K.1
-
54
-
-
84862500869
-
-
An internal report on the method is available upon request: Internal Report N123705/1; Department of Global Medical and Scientific Information, Johnson & Johnson Pharmaceutical Research and Development, a Division of Janssen Pharmaceutica, Turnhoutseweg 30, B-2340 Beerse, Belgium.
-
50) and Its Confidence Interval, Assuming a Linear Log Dose-Response Function. Internal Report N123705/1; Department of Global Medical and Scientific Information, Johnson & Johnson Pharmaceutical Research and Development, a Division of Janssen Pharmaceutica, Turnhoutseweg 30, B-2340 Beerse, Belgium, 1997.
-
(1997)
50) and Its Confidence Interval, Assuming A Linear Log Dose-Response Function
-
-
Lewi, P.J.1
Niemegeers, C.J.E.2
Gypen, L.M.J.3
|