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Results: 1 to 20 of 137

1.

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.

PMID:
23348500
[PubMed - indexed for MEDLINE]
Free PMC Article
2.
3.

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
[PubMed - indexed for MEDLINE]
Free Article
4.

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.

PMID:
19737913
[PubMed - indexed for MEDLINE]
Free PMC Article
5.

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.

PMID:
24076101
[PubMed - indexed for MEDLINE]
Free Article
6.

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
[PubMed - indexed for MEDLINE]
Free Article
7.

The effect of mGlu5 receptor positive allosteric modulators on signaling molecules in brain slices.

Liu F, Zhang G, Hornby G, Vasylyev D, Bowlby M, Park K, Gilbert A, Marquis K, Andree TH.

Eur J Pharmacol. 2006 May 1;536(3):262-8. Epub 2006 Apr 5.

PMID:
16600209
[PubMed - indexed for MEDLINE]
8.

Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism.

Bridges TM, Rook JM, Noetzel MJ, Morrison RD, Zhou Y, Gogliotti RD, Vinson PN, Xiang Z, Jones CK, Niswender CM, Lindsley CW, Stauffer SR, Conn PJ, Daniels JS.

Drug Metab Dispos. 2013 Sep;41(9):1703-14. doi: 10.1124/dmd.113.052084. Epub 2013 Jul 2.

PMID:
23821185
[PubMed - indexed for MEDLINE]
9.

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
[PubMed - indexed for MEDLINE]
Free Article
10.

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.

PMID:
20923853
[PubMed - indexed for MEDLINE]
Free PMC Article
11.

Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.

Rook JM, Noetzel MJ, Pouliot WA, Bridges TM, Vinson PN, Cho HP, Zhou Y, Gogliotti RD, Manka JT, Gregory KJ, Stauffer SR, Dudek FE, Xiang Z, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ.

Biol Psychiatry. 2013 Mar 15;73(6):501-9. doi: 10.1016/j.biopsych.2012.09.012. Epub 2012 Nov 7.

PMID:
23140665
[PubMed - indexed for MEDLINE]
Free PMC Article
12.

Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).

Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, Meiler J, Conn PJ, Lindsley CW, Stauffer SR.

J Med Chem. 2013 Oct 24;56(20):7976-96. doi: 10.1021/jm401028t. Epub 2013 Oct 9.

PMID:
24050755
[PubMed - indexed for MEDLINE]
13.

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.

Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, Conn PJ.

Mol Pharmacol. 2005 Dec;68(6):1793-802. Epub 2005 Sep 9.

PMID:
16155210
[PubMed - indexed for MEDLINE]
Free Article
14.

Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes.

Zhang Y, Rodriguez AL, Conn PJ.

J Pharmacol Exp Ther. 2005 Dec;315(3):1212-9. Epub 2005 Aug 31.

PMID:
16135701
[PubMed - indexed for MEDLINE]
Free Article
15.

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
[PubMed - indexed for MEDLINE]
16.

CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.

Lindemann L, Jaeschke G, Michalon A, Vieira E, Honer M, Spooren W, Porter R, Hartung T, Kolczewski S, Büttelmann B, Flament C, Diener C, Fischer C, Gatti S, Prinssen EP, Parrott N, Hoffmann G, Wettstein JG.

J Pharmacol Exp Ther. 2011 Nov;339(2):474-86. doi: 10.1124/jpet.111.185660. Epub 2011 Aug 17.

PMID:
21849627
[PubMed - indexed for MEDLINE]
Free Article
17.

Progress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Stauffer SR.

ACS Chem Neurosci. 2011 Aug 17;2(8):450-70. doi: 10.1021/cn2000519. Epub 2011 Jun 27. Review.

PMID:
22860171
[PubMed - indexed for MEDLINE]
Free PMC Article
18.

N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.

Gregory KJ, Herman EJ, Ramsey AJ, Hammond AS, Byun NE, Stauffer SR, Manka JT, Jadhav S, Bridges TM, Weaver CD, Niswender CM, Steckler T, Drinkenburg WH, Ahnaou A, Lavreysen H, Macdonald GJ, Bartolomé JM, Mackie C, Hrupka BJ, Caron MG, Daigle TL, Lindsley CW, Conn PJ, Jones CK.

J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. doi: 10.1124/jpet.113.206623. Epub 2013 Aug 21.

PMID:
23965381
[PubMed - indexed for MEDLINE]
19.

Differential effects of the mGluR5 positive allosteric modulator CDPPB in the cortex and striatum following repeated administration.

Parmentier-Batteur S, O'Brien JA, Doran S, Nguyen SJ, Flick RB, Uslaner JM, Chen H, Finger EN, Williams TM, Jacobson MA, Hutson PH.

Neuropharmacology. 2012 Mar;62(3):1453-60. doi: 10.1016/j.neuropharm.2010.11.013. Epub 2010 Nov 26.

PMID:
21112344
[PubMed - indexed for MEDLINE]
20.

Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.

Manka JT, Vinson PN, Gregory KJ, Zhou Y, Williams R, Gogi K, Days E, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2012 Oct 15;22(20):6481-5. doi: 10.1016/j.bmcl.2012.08.043. Epub 2012 Aug 24.

PMID:
22981332
[PubMed - indexed for MEDLINE]
Free PMC Article

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