-
1
-
-
0036882079
-
3H]methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl] pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: In vitro and in vivo characterization
-
DOI 10.1124/jpet.102.040618
-
3H]Methoxymethyl-3- [(2-methyl-1,3-thiazol-4-yl) ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization. J Pharmacol Exp Ther 303:1044-1051. (Pubitemid 35424388)
-
(2002)
Journal of Pharmacology and Experimental Therapeutics
, vol.303
, Issue.3
, pp. 1044-1051
-
-
Anderson, J.J.1
Rao, S.P.2
Rowe, B.3
Giracello, D.R.4
Holtz, G.5
Chapman, D.F.6
Tehrani, L.7
Bradbury, M.J.8
Cosford, N.D.P.9
Varney, M.A.10
-
2
-
-
0032993405
-
Expression and signaling of group I metabotropic glutamate receptors in astrocytes and microglia
-
DOI 10.1046/j.1471-4159.1999.721671.x
-
Biber K, Laurie DJ, Berthele A, Sommer B, Tölle TR, Gebicke-Harter PJ, van Calker D, and Boddeke HW (1999) Expression and signaling of group I metabotropic glutamate receptors in astrocytes and microglia. J Neurochem 72:1671-1680. (Pubitemid 29140843)
-
(1999)
Journal of Neurochemistry
, vol.72
, Issue.4
, pp. 1671-1680
-
-
Biber, K.1
Laurie, D.J.2
Berthele, A.3
Sommer, B.4
Tolle, T.R.5
Gebicke-Harter, P.-J.6
Van Calker, D.7
Boddeke, H.W.G.M.8
-
3
-
-
49949106977
-
Distinct roles of group I mGlu receptors in striatal function
-
Bonsi P, Platania P, Martella G, Madeo G, Vita D, Tassone A, Bernardi G, and Pisani A (2008) Distinct roles of group I mGlu receptors in striatal function. Neuropharmacology 55:392-395.
-
(2008)
Neuropharmacology
, vol.55
, pp. 392-395
-
-
Bonsi, P.1
Platania, P.2
Martella, G.3
Madeo, G.4
Vita, D.5
Tassone, A.6
Bernardi, G.7
Pisani, A.8
-
5
-
-
40849124248
-
N-{4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl} -2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors
-
DOI 10.1124/mol.107.040097
-
Chen Y, Goudet C, Pin JP, and Conn PJ (2008) N-{4-Chloro-2-[(1,3-dioxo-1, 3-dihydro-2H-isoindol-2-yl) methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors. Mol Pharmacol 73:909-918. (Pubitemid 351397895)
-
(2008)
Molecular Pharmacology
, vol.73
, Issue.3
, pp. 909-918
-
-
Chen, Y.1
Goudet, C.2
Pin, J.-P.3
Conn, P.J.4
-
6
-
-
34247477329
-
Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses
-
DOI 10.1124/mol.106.032425
-
Chen Y, Nong Y, Goudet C, Hemstapat K, de Paulis T, Pin JP, and Conn PJ (2007) Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol Pharmacol 71:1389-1398. (Pubitemid 46661543)
-
(2007)
Molecular Pharmacology
, vol.71
, Issue.5
, pp. 1389-1398
-
-
Chen, Y.1
Nong, Y.2
Goudet, C.3
Hemstapat, K.4
De Paulis, T.5
Pin, J.-P.6
Conn, P.J.7
-
8
-
-
58149193205
-
Allosteric modulators of GPCRs: A novel approach for the treatment of CNS disorders
-
Conn PJ, Christopoulos A, and Lindsley CW (2009) Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov 8:41-54.
-
(2009)
Nat. Rev. Drug Discov.
, vol.8
, pp. 41-54
-
-
Conn, P.J.1
Christopoulos, A.2
Lindsley, C.W.3
-
10
-
-
40949090052
-
Role for metabotropic glutamate receptor 5 (mGluR5) in the pathogenesis of fragile X syndrome
-
DOI 10.1113/jphysiol.2008.150722
-
Dölen G and Bear MF (2008) Role for metabotropic glutamate receptor 5 (mGluR5) in the pathogenesis of fragile X syndrome. J Physiol 586:1503-1508. (Pubitemid 351404955)
-
(2008)
Journal of Physiology
, vol.586
, Issue.6
, pp. 1503-1508
-
-
Dolen, G.1
Bear, M.F.2
-
11
-
-
0023958554
-
Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods
-
Ehlert FJ (1988) Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods. Mol Pharmacol 33:187-194.
-
(1988)
Mol. Pharmacol.
, vol.33
, pp. 187-194
-
-
Ehlert, F.J.1
-
12
-
-
0032853255
-
2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist
-
DOI 10.1016/S0028-3908(99)00082-9, PII S0028390899000829
-
Gasparini F, Lingenhöhl K, Stoehr N, Flor PJ, Heinrich M, Vranesic I, Biollaz M, Allgeier H, Heckendorn R, Urwyler S, et al. (1999) 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology 38:1493-1503. (Pubitemid 29457731)
-
(1999)
Neuropharmacology
, vol.38
, Issue.10
, pp. 1493-1503
-
-
Gasparini, F.1
Lingenhohl, K.2
Stoehr, N.3
Flor, P.J.4
Heinrich, M.5
Vranesic, I.6
Biollaz, M.7
Allgeier, H.8
Heckendorn, R.9
Urwyler, S.10
Varney, M.A.11
Johnson, E.C.12
Hess, S.D.13
Rao, S.P.14
Sacaan, A.I.15
Santori, E.M.16
Velicelebi, G.17
Kuhn, R.18
-
13
-
-
33846901907
-
Metabotropic glutamate receptors: intracellular signaling pathways
-
DOI 10.1016/j.coph.2006.08.008, PII S1471489206001706, Neurosciences
-
Gerber U, Gee CE, and Benquet P (2007) Metabotropic glutamate receptors: intracellular signaling pathways. Curr Opin Pharmacol 7:56-61. (Pubitemid 46238032)
-
(2007)
Current Opinion in Pharmacology
, vol.7
, Issue.1
, pp. 56-61
-
-
Gerber, U.1
Gee, C.E.2
Benquet, P.3
-
14
-
-
0346458626
-
Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors
-
DOI 10.1073/pnas.0304699101
-
Goudet C, Gaven F, Kniazeff J, Vol C, Liu J, Cohen-Gonsaud M, Acher F, Prezeau L, and Pin JP (2004) Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors. Proc Natl Acad Sci USA 101:378-383. (Pubitemid 38084258)
-
(2004)
Proceedings of the National Academy of Sciences of the United States of America
, vol.101
, Issue.1
, pp. 378-383
-
-
Goudett, C.1
Gaven, F.2
Kniazeff, J.3
Vol, C.4
Liu, J.5
Cohen-Gonsaud, M.6
Acher, F.7
Prezeau, L.8
Pin, J.P.9
-
15
-
-
0035504328
-
Structural, signalling and regulatory properties of the group I metabotropic glutamate receptors: Prototypic family C G-protein-coupled receptors
-
DOI 10.1042/0264-6021:3590465
-
Hermans e and Challiss RA (2001) Structural, signalling and regulatory properties of the group I metabotropic glutamate receptors: prototypic family C G-protein-coupled receptors. Biochem J 359:465-484. (Pubitemid 33063371)
-
(2001)
Biochemical Journal
, vol.359
, Issue.3
, pp. 465-484
-
-
Hermans, E.1
Challiss, R.A.J.2
-
16
-
-
0029795629
-
Control of calcium oscillations by phosphorylation of metabotropic glutamate receptors
-
DOI 10.1038/383089a0
-
Kawabata S, Tsutsumi R, Kohara A, Yamaguchi T, Nakanishi S, and Okada M (1996) Control of calcium oscillations by phosphorylation of metabotropic glutamate receptors. Nature 383:89-92. (Pubitemid 26296467)
-
(1996)
Nature
, vol.383
, Issue.6595
, pp. 89-92
-
-
Kawabata, S.1
Tsutsumi, R.2
Kohara, A.3
Yamaguchi, T.4
Nakanishi, S.5
Okada, M.6
-
17
-
-
27844519281
-
New concepts in drug discovery: Collateral efficacy and permissive antagonism
-
DOI 10.1038/nrd1875, PII N1875
-
Kenakin T (2005) New concepts in drug discovery: collateral efficacy and permissive antagonism. Nat Rev Drug Discov 4:919-927. (Pubitemid 41637694)
-
(2005)
Nature Reviews Drug Discovery
, vol.4
, Issue.11
, pp. 919-927
-
-
Kenakin, T.1
-
18
-
-
77952354490
-
Seven transmembrane receptors as shapeshifting proteins: The impact of allosteric modulation and functional selectivity on new drug discovery
-
Kenakin T and Miller LJ (2010) Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol Rev 62:265-304.
-
(2010)
Pharmacol. Rev.
, vol.62
, pp. 265-304
-
-
Kenakin, T.1
Miller, L.J.2
-
20
-
-
20144381462
-
A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models
-
DOI 10.1124/jpet.104.079244
-
Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, et al. (2005) A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. J Pharmacol Exp Ther 313:199-206. (Pubitemid 40411343)
-
(2005)
Journal of Pharmacology and Experimental Therapeutics
, vol.313
, Issue.1
, pp. 199-206
-
-
Kinney, G.G.1
O'Brien, J.A.2
Lemaire, W.3
Burno, M.4
Bickel, D.J.5
Clements, M.K.6
Chen, T.-B.7
Wisnoski, D.D.8
Lindsley, C.W.9
Tiller, P.R.10
Smith, S.11
Jacobson, M.A.12
Sur, C.13
Duggan, M.E.14
Pettibone, D.J.15
Conn, P.J.16
Williams Jr., D.L.17
-
21
-
-
33747181100
-
Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox
-
DOI 10.1016/j.tips.2006.07.009, PII S0165614706001805
-
Langmead CJ and Christopoulos A (2006) Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox. Trends Pharmacol Sci 27:475-481. (Pubitemid 44233695)
-
(2006)
Trends in Pharmacological Sciences
, vol.27
, Issue.9
, pp. 475-481
-
-
Langmead, C.J.1
Christopoulos, A.2
-
22
-
-
0029126526
-
Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors
-
Lazareno S and Birdsall NJ (1995) Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors. Mol Pharmacol 48:362-378.
-
(1995)
Mol. Pharmacol.
, vol.48
, pp. 362-378
-
-
Lazareno, S.1
Birdsall, N.J.2
-
23
-
-
34447632041
-
Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology
-
DOI 10.1016/j.tips.2007.06.004, PII S0165614707001496, Allosterism and Collateral Efficacy
-
Leach K, Sexton PM, and Christopoulos A (2007) Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. Trends Pharmacol Sci 28:382-389. (Pubitemid 47087967)
-
(2007)
Trends in Pharmacological Sciences
, vol.28
, Issue.8
, pp. 382-389
-
-
Leach, K.1
Sexton, P.M.2
Christopoulos, A.3
-
24
-
-
57349174038
-
ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol- 5-yl]-piperidin-1-yl}-methanone]: A novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and precognitive activities
-
Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, Atkinson PJ, Popiolek M, Wantuch C, Khawaja X, et al. (2008) ADX47273 [S-(4-fluoro-phenyl)- {3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and precognitive activities. J Pharmacol Exp Ther 327:827-839.
-
(2008)
J. Pharmacol. Exp. Ther.
, vol.327
, pp. 827-839
-
-
Liu, F.1
Grauer, S.2
Kelley, C.3
Navarra, R.4
Graf, R.5
Zhang, G.6
Atkinson, P.J.7
Popiolek, M.8
Wantuch, C.9
Khawaja, X.10
-
25
-
-
30844432624
-
Glutamate-based therapeutic approaches: Allosteric modulators of metabotropic glutamate receptors
-
DOI 10.1016/j.coph.2005.09.006, PII S1471489205001839
-
Marino MJ and Conn PJ (2006) Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors. Curr Opin Pharmacol 6:98-102. (Pubitemid 43103825)
-
(2006)
Current Opinion in Pharmacology
, vol.6
, Issue.1 SPEC. ISS.
, pp. 98-102
-
-
Marino, M.J.1
Conn, P.J.2
-
26
-
-
0029133369
-
The expression of two splice variants of metabotropic glutamate receptor subtype 5 in the rat brain and neuronal cells during development
-
Minakami R, Iida K, Hirakawa N, and Sugiyama H (1995) The expression of two splice variants of metabotropic glutamate receptor subtype 5 in the rat brain and neuronal cells during development. J Neurochem 65:1536-1542.
-
(1995)
J. Neurochem.
, vol.65
, pp. 1536-1542
-
-
Minakami, R.1
Iida, K.2
Hirakawa, N.3
Sugiyama, H.4
-
28
-
-
29344436808
-
Determination of key amino acids implicated in the actions of allosteric modulation by 3,3'-difluorobenzaldazine on rat mGlu5 receptors
-
Mühlemann A, Ward NA, Kratochwil N, Diener C, Fischer C, Stucki A, Jaeschke G, Malherbe P, and Porter RH (2006) Determination of key amino acids implicated in the actions of allosteric modulation by 3,3'-difluorobenzaldazine on rat mGlu5 receptors. Eur J Pharmacol 529:95-104.
-
(2006)
Eur. J. Pharmacol.
, vol.529
, pp. 95-104
-
-
Mühlemann, 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
-
29
-
-
0033773290
-
3H]quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections
-
3H]quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections. J Neurochem 75:2590-2601.
-
(2000)
J. Neurochem.
, vol.75
, pp. 2590-2601
-
-
Mutel, V.1
Ellis, G.J.2
Adam, G.3
Chaboz, S.4
Nilly, A.5
Messer, J.6
Bleuel, Z.7
Metzler, V.8
Malherbe, P.9
Schlaeger, E.J.10
-
30
-
-
0030886438
-
The metabotropic glutamate receptor mGluR5 induces calcium oscillations in cultured astrocytes via protein kinase C phosphorylation
-
Nakahara K, Okada M, and Nakanishi S (1997) The metabotropic glutamate receptor mGluR5 induces calcium oscillations in cultured astrocytes via protein kinase C phosphorylation. J Neurochem 69:1467-1475. (Pubitemid 27406947)
-
(1997)
Journal of Neurochemistry
, vol.69
, Issue.4
, pp. 1467-1475
-
-
Nakahara, K.1
Okada, M.2
Nakanishi, S.3
-
31
-
-
0037184051
-
2+ and inositol 1,4,5-trisphosphate oscillation frequency. Receptor density versus agonist concentration
-
2+ and inositol 1,4,5-trisphosphate oscillation frequency. Receptor density versus agonist concentration. J Biol Chem 277:35947-35960.
-
(2002)
J. Biol. Chem.
, vol.277
, pp. 35947-35960
-
-
Nash, M.S.1
Schell, M.J.2
Atkinson, P.J.3
Johnston, N.R.4
Nahorski, S.R.5
Challiss, R.A.6
-
32
-
-
0035960037
-
Intracellular signalling: Receptor-specific messenger oscillations
-
DOI 10.1038/35096643
-
Nash MS, Young KW, Challiss RA, and Nahorski SR (2001) Intracellular signalling. Receptor-specific messenger oscillations. Nature 413:381-382. (Pubitemid 32928584)
-
(2001)
Nature
, vol.413
, Issue.6854
, pp. 381-382
-
-
Nash, M.S.1
Young, K.W.2
Challiss, R.A.J.3
Nahorski, S.R.4
-
33
-
-
77949516412
-
Metabotropic glutamate receptors: Physiology, pharmacology, and disease
-
Niswender CM and Conn PJ (2010) Metabotropic glutamate receptors: physiology, pharmacology, and disease. Annu Rev Pharmacol Toxicol 50:295-322.
-
(2010)
Annu. Rev. Pharmacol. Toxicol.
, vol.50
, pp. 295-322
-
-
Niswender, C.M.1
Conn, P.J.2
-
34
-
-
0041353568
-
A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5
-
DOI 10.1124/mol.64.3.731
-
O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Lindsley CW, Schaffhauser HJ, Sur C, Pettibone DJ, et al. (2003) A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol 64:731-740. (Pubitemid 37048578)
-
(2003)
Molecular Pharmacology
, vol.64
, Issue.3
, pp. 731-740
-
-
O'Brien, J.A.1
Lemaire, W.2
Chen, T.-B.3
Chang, R.S.L.4
Jacobson, M.A.5
Ha, S.N.6
Lindsley, C.W.7
Schaffhauser, H.J.8
Sur, C.9
Pettibone, D.J.10
Conn, P.J.11
Williams Jr., D.L.12
-
35
-
-
11144354887
-
A Novel Selective Allosteric Modulator Potentiates the Activity of Native Metabotropic Glutamate Receptor Subtype 5 in Rat Forebrain
-
DOI 10.1124/jpet.103.061747
-
O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Schaffhauser HJ, Rowe B, Sur C, et al. (2004) A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. J Pharmacol Exp Ther 309:568-577. (Pubitemid 38542609)
-
(2004)
Journal of Pharmacology and Experimental Therapeutics
, vol.309
, Issue.2
, pp. 568-577
-
-
O'Brien, J.A.1
Lemaire, W.2
Wittmann, M.3
Jacobson, M.A.4
Ha, S.N.5
Wisnoski, D.D.6
Lindsley, C.W.7
Schaffhauser, H.J.8
Rowe, B.9
Sur, C.10
Duggan, M.E.11
Pettibone, D.J.12
Conn, P.J.13
Williams Jr., D.L.14
-
36
-
-
27844482134
-
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
-
DOI 10.1124/mol.105.016139
-
Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, and Conn PJ (2005) 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 68:1793-1802. (Pubitemid 41654362)
-
(2005)
Molecular Pharmacology
, vol.68
, Issue.6
, 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
-
38
-
-
14044258729
-
Metabotropic glutamate receptors as novel targets for anxiety and stress disorders
-
DOI 10.1038/nrd1630
-
Swanson CJ, Bures M, Johnson MP, Linden AM, Monn JA, and Schoepp DD (2005) Metabotropic glutamate receptors as novel targets for anxiety and stress disorders. Nat Rev Drug Discov 4:131-144. (Pubitemid 40277494)
-
(2005)
Nature Reviews Drug Discovery
, vol.4
, Issue.2
, 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
-
39
-
-
34249776663
-
Glutamate-mediated neuronal-glial transmission
-
DOI 10.1111/j.1469-7580.2007.00734.x
-
Verkhratsky A and Kirchhoff F (2007) Glutamate-mediated neuronal-glial transmission. J Anat 210:651-660. (Pubitemid 46851000)
-
(2007)
Journal of Anatomy
, vol.210
, Issue.6
, pp. 651-660
-
-
Verkhratsky, A.1
Kirchhoff, F.2
-
40
-
-
64949091023
-
Metabotropic glutamate receptors in the tripartite synapse as a target for new psychotropic drugs
-
Wierońska JM and Pilc A (2009) Metabotropic glutamate receptors in the tripartite synapse as a target for new psychotropic drugs. Neurochem Int 55:85-97.
-
(2009)
Neurochem. Int.
, vol.55
, pp. 85-97
-
-
Wierońska, J.M.1
Pilc, A.2
|