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Volumn 71, Issue 5, 2007, Pages 1389-1398

Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses

Author keywords

[No Author keywords available]

Indexed keywords

2 METHYL 6 (PHENYLETHYNYL)PYRIDINE; 3 CYANO N (1,3 DIPHENYL 1H PYRAZOL 5 YL)BENZAMIDE; 3,3' DIFLUOROBENZALDAZINE; 4 NITRO N (11,3 DIPHENYL 1H PYRAZOL 5 YL)BENZAMIDE; BENZAMIDE DERIVATIVE; METABOTROPIC RECEPTOR 5; METABOTROPIC RECEPTOR AGONIST; N [4 CHLORO 2 [(1,3 DIOXO 1,3 DIHYDRO 2H ISOINDOL 2 YL)METHYL]PHENYL] 2 HYDROXYBENZAMIDE; UNCLASSIFIED DRUG; VU 29;

EID: 34247477329     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.106.032425     Document Type: Article
Times cited : (84)

References (40)
  • 2
    • 9644281056 scopus 로고    scopus 로고
    • Synthesis and receptor assay of aromatic-ethynyl-aromatic derivatives with potent mGluR5 antagonist activity
    • Alagille D, Baldwin RM, Roth BL, Wroblewski JT, Grajkowska E, and Tamagnan GD (2005b) Synthesis and receptor assay of aromatic-ethynyl-aromatic derivatives with potent mGluR5 antagonist activity. Bioorg Med Chem 13:197-209.
    • (2005) Bioorg Med Chem , vol.13 , pp. 197-209
    • Alagille, D.1    Baldwin, R.M.2    Roth, B.L.3    Wroblewski, J.T.4    Grajkowska, E.5    Tamagnan, G.D.6
  • 3
    • 0034332480 scopus 로고    scopus 로고
    • Activation of metabotropic glutamate receptor 5 has direct excitatory effects and potentiates NMDA receptor currents in neurons of the subthalamic nucleus
    • Awad H, Hubert GW, Smith Y, Levey AI, and Conn PJ (2000) Activation of metabotropic glutamate receptor 5 has direct excitatory effects and potentiates NMDA receptor currents in neurons of the subthalamic nucleus. J Neurosci 20:7871-7879.
    • (2000) J Neurosci , vol.20 , pp. 7871-7879
    • Awad, H.1    Hubert, G.W.2    Smith, Y.3    Levey, A.I.4    Conn, P.J.5
  • 5
    • 34247527928 scopus 로고    scopus 로고
    • Chen Y, Rodriguez AL, and Conn PJ (2004) Two structurally distinct allosteric potentiators of mGluR5 act on different sites of the receptor. Soc Neurosci Abstr 30:627.14.
    • Chen Y, Rodriguez AL, and Conn PJ (2004) Two structurally distinct allosteric potentiators of mGluR5 act on different sites of the receptor. Soc Neurosci Abstr 30:627.14.
  • 7
    • 0030995878 scopus 로고    scopus 로고
    • Pharmacology and functions of metabotropic glutamate receptors
    • Conn PJ and Pin JP (1997) Pharmacology and functions of metabotropic glutamate receptors. Annu Rev Pharmacol Toxicol 37:205-237.
    • (1997) Annu Rev Pharmacol Toxicol , vol.37 , pp. 205-237
    • Conn, P.J.1    Pin, J.P.2
  • 8
    • 0037330358 scopus 로고    scopus 로고
    • 3H]-Methoxymethyl-MTEP and [3H]-methoxy-PEPy: Potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor
    • Cosford ND, Roppe J, Tehrani L, Schweiger EJ, Seiders TJ, Chaudary A, Rao S, and Varney MA (2003) [3H]-Methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. Bioorg Med Chem Lett 13:351-354.
    • (2003) Bioorg Med Chem Lett , vol.13 , pp. 351-354
    • Cosford, N.D.1    Roppe, J.2    Tehrani, L.3    Schweiger, E.J.4    Seiders, T.J.5    Chaudary, A.6    Rao, S.7    Varney, M.A.8
  • 9
    • 0036893246 scopus 로고    scopus 로고
    • Metabotropic glutamate receptors: Electrical and chemical signaling properties
    • Coutinho V and Knopfel T (2002) Metabotropic glutamate receptors: electrical and chemical signaling properties. Neuroscientist 8:551-561.
    • (2002) Neuroscientist , vol.8 , pp. 551-561
    • Coutinho, V.1    Knopfel, T.2
  • 10
    • 33744801125 scopus 로고    scopus 로고
    • Substituent effects of N-(1,3-diphenyl- 1Hpyrazol-5yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes
    • de Paulis T, Hemstapat K, Chen Y, Zhang Y, Saleh S, Alagille D, Baldwin RM, Tamagnan GD, and Conn PJ (2006) Substituent effects of N-(1,3-diphenyl- 1Hpyrazol-5yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. J Med Chem 49:3332-3344.
    • (2006) J Med Chem , vol.49 , pp. 3332-3344
    • de Paulis, T.1    Hemstapat, K.2    Chen, Y.3    Zhang, Y.4    Saleh, S.5    Alagille, D.6    Baldwin, R.M.7    Tamagnan, G.D.8    Conn, P.J.9
  • 11
    • 0012662271 scopus 로고    scopus 로고
    • The roles of metabotropic glutamate receptors in seizures and epilepsy
    • Doherty J and Dingledine R (2002) The roles of metabotropic glutamate receptors in seizures and epilepsy. Curr Drug Target CNS Neurol Disord 1:251-260.
    • (2002) Curr Drug Target CNS Neurol Disord , vol.1 , pp. 251-260
    • Doherty, J.1    Dingledine, R.2
  • 12
    • 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 CK, Hemstapat K, Nong Y, Echemendia NG, Williams LC, de Paulis T, and Conn PJ (2006) 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 318:173-185.
    • (2006) J Pharmacol Exp Ther , vol.318 , pp. 173-185
    • Galici, R.1    Jones, C.K.2    Hemstapat, K.3    Nong, Y.4    Echemendia, N.G.5    Williams, L.C.6    de Paulis, T.7    Conn, P.J.8
  • 13
    • 0036462446 scopus 로고    scopus 로고
    • Allosteric modulators of group I metabotropic glutamate receptors: Novel subtype-selective ligands and therapeutic perspectives
    • Gasparini F, Kuhn R, and Pin JP (2002) Allosteric modulators of group I metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives. Curr Opin Pharmacol 2:43-49.
    • (2002) Curr Opin Pharmacol , vol.2 , pp. 43-49
    • Gasparini, F.1    Kuhn, R.2    Pin, J.P.3
  • 16
    • 33746265808 scopus 로고    scopus 로고
    • A novel class of positive allosteric modulators of mGluR1 interact with a site distinct from that of negative allosteric modulators
    • Hemstapat K, de Paulis T, Chen Y, Brady AE, Grover VK, Alagille D, Tamagnan GD, and Conn PJ (2006) A novel class of positive allosteric modulators of mGluR1 interact with a site distinct from that of negative allosteric modulators. Mol Pharmacol 70:616-626.
    • (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
  • 17
    • 32344445040 scopus 로고    scopus 로고
    • Synthesis and structureactivity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl] pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonist: Search for cocaine medications
    • Iso Y, Grajkowska E, Wroblewski JT, Davis J, Goeders NE, Johnson KM, Sanker S, Roth BL, Tueckmantel W, and Kozikowski AP (2006) Synthesis and structureactivity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl] pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonist: search for cocaine medications. J Med Chem 49:1080-1100.
    • (2006) J Med Chem , vol.49 , pp. 1080-1100
    • Iso, Y.1    Grajkowska, E.2    Wroblewski, J.T.3    Davis, J.4    Goeders, N.E.5    Johnson, K.M.6    Sanker, S.7    Roth, B.L.8    Tueckmantel, W.9    Kozikowski, A.P.10
  • 18
  • 20
    • 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 JN, Malherbe P, Vieira E, Wichmann J, and Kemp JA (2001) Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action and binding site. Proc Natl Acad Sci USA 98:13402-13407.
    • (2001) Proc Natl Acad Sci USA , 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
  • 22
    • 0141569326 scopus 로고    scopus 로고
    • Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine
    • Malherbe P, Kratochwil N, Zenner MT, Piussi J, Diener C, Kratzeisen C, Fischer C, and Porter RH (2003) Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine. Mol Pharmacol 64:823-832.
    • (2003) Mol Pharmacol , vol.64 , pp. 823-832
    • Malherbe, P.1    Kratochwil, N.2    Zenner, M.T.3    Piussi, J.4    Diener, C.5    Kratzeisen, C.6    Fischer, C.7    Porter, R.H.8
  • 23
    • 0036669760 scopus 로고    scopus 로고
    • Haloperidol-induced alteration in the physiological actions of group I mGlus in the subthalamic nucleus and the substantia nigra pars reticulate
    • Marino MJ, Awad-Granko H, Ciombor KJ, and Conn PJ (2002) Haloperidol-induced alteration in the physiological actions of group I mGlus in the subthalamic nucleus and the substantia nigra pars reticulate. Neuropharmacology 43:147-159.
    • (2002) Neuropharmacology , vol.43 , pp. 147-159
    • Marino, M.J.1    Awad-Granko, H.2    Ciombor, K.J.3    Conn, P.J.4
  • 24
    • 0038798022 scopus 로고    scopus 로고
    • Direct and indirect modulation of the N-methyl-D-aspartate receptor
    • Marino MJ and Conn PJ (2002a) Direct and indirect modulation of the N-methyl-D-aspartate receptor. Curr Drug Target CNS Neurol Disord 1:1-16.
    • (2002) Curr Drug Target CNS Neurol Disord , vol.1 , pp. 1-16
    • Marino, M.J.1    Conn, P.J.2
  • 25
    • 0012667907 scopus 로고    scopus 로고
    • Modulation of the basal ganglia by metabotropic glutamate receptors: Potential for novel therapeutics
    • Marino MJ and Conn PJ (2002b) Modulation of the basal ganglia by metabotropic glutamate receptors: potential for novel therapeutics. Curr Drug Target CNS Neurol Disord 1:239-250.
    • (2002) Curr Drug Target CNS Neurol Disord , vol.1 , pp. 239-250
    • Marino, M.J.1    Conn, P.J.2
  • 27
    • 0035884943 scopus 로고    scopus 로고
    • Activation of group I metabotropic glutamate receptors produces a direct excitation and disinhibition of GABAergic projection neurons in the substantia nigra pars reticulata
    • Marino MJ, Wittmann M, Bradley SR, Hubert GW, Smith Y, and Conn PJ (2001) Activation of group I metabotropic glutamate receptors produces a direct excitation and disinhibition of GABAergic projection neurons in the substantia nigra pars reticulata. J Neurosci 21:7001-7012.
    • (2001) J Neurosci , vol.21 , pp. 7001-7012
    • Marino, M.J.1    Wittmann, M.2    Bradley, S.R.3    Hubert, G.W.4    Smith, Y.5    Conn, P.J.6
  • 28
    • 0141869933 scopus 로고    scopus 로고
    • Allosteric modulators of G-protein-coupled receptors
    • May LT and Christopoulos A (2003) Allosteric modulators of G-protein-coupled receptors. Curr Opin Pharmacol 3:551-556.
    • (2003) Curr Opin Pharmacol , vol.3 , pp. 551-556
    • May, L.T.1    Christopoulos, A.2
  • 32
    • 0034721795 scopus 로고    scopus 로고
    • The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b] chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors
    • Pagano A, Ruegg D, Litschig S, Stoehr N, Stierlin C, Heinrich M, Floersheim P, Prezeau L, Carroll F, Pin JP, et al. (2000) The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b] chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors. J Biol Chem 275:33750-33758.
    • (2000) J Biol Chem , vol.275 , pp. 33750-33758
    • Pagano, A.1    Ruegg, D.2    Litschig, S.3    Stoehr, N.4    Stierlin, C.5    Heinrich, M.6    Floersheim, P.7    Prezeau, L.8    Carroll, F.9    Pin, J.P.10
  • 33
    • 0036965681 scopus 로고    scopus 로고
    • On the role of metabotropic glutamate receptors in the mechanisms of action of antidepressants
    • Palucha A and Pilc A (2002) On the role of metabotropic glutamate receptors in the mechanisms of action of antidepressants. Pol J Pharmacol 54:581-586.
    • (2002) Pol J Pharmacol , vol.54 , pp. 581-586
    • Palucha, A.1    Pilc, A.2
  • 34
    • 0035894851 scopus 로고    scopus 로고
    • Metabotropic glutamate receptor 5-induced phosphorylation of extracellular signal-regulated kinase in astrocytes depends on transactivation of the epidermal growth factor receptor
    • Peavy RD, Chang MS, Sanders-Bush E, and Conn PJ (2001) Metabotropic glutamate receptor 5-induced phosphorylation of extracellular signal-regulated kinase in astrocytes depends on transactivation of the epidermal growth factor receptor. J Neurosci 21:9619-9628.
    • (2001) J Neurosci , vol.21 , pp. 9619-9628
    • Peavy, R.D.1    Chang, M.S.2    Sanders-Bush, E.3    Conn, P.J.4
  • 35
    • 0042521068 scopus 로고    scopus 로고
    • LY-354740 (Eli Lilly)
    • Pilc A (2003) LY-354740 (Eli Lilly). IDrugs 6:66-71.
    • (2003) IDrugs , vol.6 , pp. 66-71
    • Pilc, A.1
  • 36
    • 27844482134 scopus 로고    scopus 로고
    • A close structural analog of MPEP acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators
    • Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, Conn PJ (2005) A close structural analog of MPEP 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.
    • (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
  • 38
    • 0001050064 scopus 로고    scopus 로고
    • Metabotropic glutamate receptor involvement in models of acute and persistent pain: Prospects for the development of novel analgesics
    • Varney MA and Gereau RW 4th (2002) Metabotropic glutamate receptor involvement in models of acute and persistent pain: prospects for the development of novel analgesics. Curr Drug Target CNS Neurol Disord 1:283-296.
    • (2002) Curr Drug Target CNS Neurol Disord , vol.1 , pp. 283-296
    • Varney, M.A.1    Gereau 4th, R.W.2
  • 39
    • 0036078428 scopus 로고    scopus 로고
    • (S)-3,5-DHPG: A review
    • Wisniewski K and Carr H (2002) (S)-3,5-DHPG: a review. CNS Drug Rev 8:101-116.
    • (2002) CNS Drug Rev , vol.8 , pp. 101-116
    • Wisniewski, K.1    Carr, H.2
  • 40
    • 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 AL, and Conn PJ (2005) Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes. J Pharmacol Exp Ther 315:1212-1219.
    • (2005) J Pharmacol Exp Ther , vol.315 , pp. 1212-1219
    • Zhang, Y.1    Rodriguez, A.L.2    Conn, P.J.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.