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Items: 1 to 20 of 382

1.

Development of allosteric modulators of GPCRs for treatment of CNS disorders.

Nickols HH, Conn PJ.

Neurobiol Dis. 2014 Jan;61:55-71. doi: 10.1016/j.nbd.2013.09.013. Epub 2013 Sep 27. Review.

2.

Identification of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Acting at Site Distinct from 2-Methyl-6-(phenylethynyl)-pyridine Binding.

Butkiewicz M, Rodriguez AL, Rainey SE, Wieting J, Luscombe VB, Stauffer SR, Lindsley CW, Conn PJ, Meiler J.

ACS Chem Neurosci. 2019 Jun 17. doi: 10.1021/acschemneuro.8b00227. [Epub ahead of print]

PMID:
31132237
4.
5.

Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor.

Khajehali E, Valant C, Jörg M, Tobin AB, Conn PJ, Lindsley CW, Sexton PM, Scammells PJ, Christopoulos A.

Biochem Pharmacol. 2018 Aug;154:243-254. doi: 10.1016/j.bcp.2018.05.009. Epub 2018 May 17.

6.

Neurophysiological signals as potential translatable biomarkers for modulation of metabotropic glutamate 5 receptors.

Harvey BD, Siok CJ, Kiss T, Volfson D, Grimwood S, Shaffer CL, Hajós M.

Neuropharmacology. 2013 Dec;75:19-30. doi: 10.1016/j.neuropharm.2013.06.020. Epub 2013 Jul 4.

PMID:
23831682
7.

A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling.

Noetzel MJ, Gregory KJ, Vinson PN, Manka JT, Stauffer SR, Lindsley CW, Niswender CM, Xiang Z, Conn PJ.

Mol Pharmacol. 2013 Apr;83(4):835-47. doi: 10.1124/mol.112.082891. Epub 2013 Jan 24. Erratum in: Mol Pharmacol. 2013 Oct;84(4):654.

8.

Quantitative analysis reveals multiple mechanisms of allosteric modulation of the mGlu5 receptor in rat astroglia.

Bradley SJ, Langmead CJ, Watson JM, Challiss RA.

Mol Pharmacol. 2011 May;79(5):874-85. doi: 10.1124/mol.110.068882. Epub 2011 Feb 14.

9.

Effects of positive allosteric modulators on single-cell oscillatory Ca2+ signaling initiated by the type 5 metabotropic glutamate receptor.

Bradley SJ, Watson JM, Challiss RA.

Mol Pharmacol. 2009 Dec;76(6):1302-13. doi: 10.1124/mol.109.059170. Epub 2009 Sep 8.

10.

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

Chen Y, Nong Y, Goudet C, Hemstapat K, de Paulis T, Pin JP, Conn PJ.

Mol Pharmacol. 2007 May;71(5):1389-98. Epub 2007 Feb 15.

PMID:
17303702
11.

Chronic treatment with MPEP, an mGlu5 receptor antagonist, normalizes basal ganglia glutamate neurotransmission in L-DOPA-treated parkinsonian monkeys.

Morin N, Morissette M, Grégoire L, Gomez-Mancilla B, Gasparini F, Di Paolo T.

Neuropharmacology. 2013 Oct;73:216-31. doi: 10.1016/j.neuropharm.2013.05.028. Epub 2013 Jun 10.

PMID:
23756168
12.

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 AE, Grover VK, Alagille D, Tamagnan GD, Conn PJ.

Mol Pharmacol. 2006 Aug;70(2):616-26. Epub 2006 Apr 27.

PMID:
16645124
13.

Pharmacological effects of metabotropic glutamate receptor ligands on prepulse inhibition in DBA/2J mice.

Hikichi H, Nishino M, Fukushima M, Satow A, Maehara S, Kawamoto H, Ohta H.

Eur J Pharmacol. 2010 Aug 10;639(1-3):99-105. doi: 10.1016/j.ejphar.2010.03.046. Epub 2010 Apr 2.

PMID:
20371235
14.

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 AL, Grier MD, Jones CK, Herman EJ, Kane AS, Smith RL, Williams R, Zhou Y, Marlo JE, Days EL, Blatt TN, Jadhav S, Menon UN, Vinson PN, Rook JM, Stauffer SR, Niswender CM, Lindsley CW, Weaver CD, Conn PJ.

Mol Pharmacol. 2010 Dec;78(6):1105-23. doi: 10.1124/mol.110.067207. Epub 2010 Oct 5.

15.

Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.

Jaeschke G, Kolczewski S, Spooren W, Vieira E, Bitter-Stoll N, Boissin P, Borroni E, Büttelmann B, Ceccarelli S, Clemann N, David B, Funk C, Guba W, Harrison A, Hartung T, Honer M, Huwyler J, Kuratli M, Niederhauser U, Pähler A, Peters JU, Petersen A, Prinssen E, Ricci A, Rueher D, Rueher M, Schneider M, Spurr P, Stoll T, Tännler D, Wichmann J, Porter RH, Wettstein JG, Lindemann L.

J Med Chem. 2015 Feb 12;58(3):1358-71. doi: 10.1021/jm501642c. Epub 2015 Feb 2.

PMID:
25565255
16.

Dopamine agonist-induced yawning in rats: a dopamine D3 receptor-mediated behavior.

Collins GT, Witkin JM, Newman AH, Svensson KA, Grundt P, Cao J, Woods JH.

J Pharmacol Exp Ther. 2005 Jul;314(1):310-9. Epub 2005 Apr 15.

18.

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 CK, Bubser M, Thompson AD, Dickerson JW, Turle-Lorenzo N, Amalric M, Blobaum AL, Bridges TM, Morrison RD, Jadhav S, Engers DW, Italiano K, Bode J, Daniels JS, Lindsley CW, Hopkins CR, Conn PJ, Niswender CM.

J Pharmacol Exp Ther. 2012 Feb;340(2):404-21. doi: 10.1124/jpet.111.187443. Epub 2011 Nov 16.

19.

Pharmacological modulation of glutamate transmission in a rat model of L-DOPA-induced dyskinesia: effects on motor behavior and striatal nuclear signaling.

Rylander D, Recchia A, Mela F, Dekundy A, Danysz W, Cenci MA.

J Pharmacol Exp Ther. 2009 Jul;330(1):227-35. doi: 10.1124/jpet.108.150425. Epub 2009 Apr 8.

20.

A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain.

O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Schaffhauser HJ, Rowe B, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL Jr.

J Pharmacol Exp Ther. 2004 May;309(2):568-77. Epub 2004 Jan 27.

PMID:
14747613

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