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Items: 1 to 20 of 514

2.

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
3.
4.

Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)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, Conn PJ.

J Med Chem. 2006 Jun 1;49(11):3332-44.

PMID:
16722652
5.

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
6.

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
7.

Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC).

Suzuki G, Kimura T, Satow A, Kaneko N, Fukuda J, Hikichi H, Sakai N, Maehara S, Kawagoe-Takaki H, Hata M, Azuma T, Ito S, Kawamoto H, Ohta H.

J Pharmacol Exp Ther. 2007 Jun;321(3):1144-53. Epub 2007 Mar 14.

PMID:
17360958
8.

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
9.

A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models.

Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL Jr.

J Pharmacol Exp Ther. 2005 Apr;313(1):199-206. Epub 2004 Dec 17.

PMID:
15608073
10.

Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.

Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Wittman M, Ha SN, Schaffhauser H, Sur C, Pettibone DJ, Duggan ME, Conn PJ, Hartman GD, Lindsley CW.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1386-91. Epub 2006 Dec 3.

PMID:
17210250
12.

A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Lindsley CW, Schaffhauser HJ, Sur C, Pettibone DJ, Conn PJ, Williams DL Jr.

Mol Pharmacol. 2003 Sep;64(3):731-40.

PMID:
12920211
13.

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.

14.

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.

15.

Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2.

Schaffhauser H, Rowe BA, Morales S, Chavez-Noriega LE, Yin R, Jachec C, Rao SP, Bain G, Pinkerton AB, Vernier JM, Bristow LJ, Varney MA, Daggett LP.

Mol Pharmacol. 2003 Oct;64(4):798-810.

PMID:
14500736
16.

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.

Neuropharmacology. 2009 Sep;57(4):438-45. doi: 10.1016/j.neuropharm.2009.06.017. Epub 2009 Jun 24.

PMID:
19559036
17.

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 procognitive activities.

Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, Atkinson PJ, Popiolek M, Wantuch C, Khawaja X, Smith D, Olsen M, Kouranova E, Lai M, Pruthi F, Pulicicchio C, Day M, Gilbert A, Pausch MH, Brandon NJ, Beyer CE, Comery TA, Logue S, Rosenzweig-Lipson S, Marquis KL.

J Pharmacol Exp Ther. 2008 Dec;327(3):827-39. doi: 10.1124/jpet.108.136580. Epub 2008 Aug 27.

PMID:
18753411
18.

Orthosteric and allosteric drug binding sites in the Caenorhabditis elegans mgl-2 metabotropic glutamate receptor.

Tharmalingam S, Burns AR, Roy PJ, Hampson DR.

Neuropharmacology. 2012 Sep;63(4):667-74. doi: 10.1016/j.neuropharm.2012.05.029. Epub 2012 May 28.

PMID:
22652059
19.
20.

Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.

Hammond AS, Rodriguez AL, Townsend SD, Niswender CM, Gregory KJ, Lindsley CW, Conn PJ.

ACS Chem Neurosci. 2010 Oct 20;1(10):702-716. Epub 2010 Aug 19.

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