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Items: 1 to 20 of 215

1.

Preclinical profile of a novel metabotropic glutamate receptor 5 positive allosteric modulator.

Spear N, Gadient RA, Wilkins DE, Do M, Smith JS, Zeller KL, Schroeder P, Zhang M, Arora J, Chhajlani V.

Eur J Pharmacol. 2011 Jun 1;659(2-3):146-54. doi: 10.1016/j.ejphar.2011.02.003. Epub 2011 Feb 16.

PMID:
21335002
2.

In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.

Gilmour G, Broad LM, Wafford KA, Britton T, Colvin EM, Fivush A, Gastambide F, Getman B, Heinz BA, McCarthy AP, Prieto L, Shanks E, Smith JW, Taboada L, Edgar DM, Tricklebank MD.

Neuropharmacology. 2013 Jan;64:224-39. doi: 10.1016/j.neuropharm.2012.07.030. Epub 2012 Aug 1.

PMID:
22884720
3.

Functional interaction of metabotropic glutamate receptor 5 and NMDA-receptor by a metabotropic glutamate receptor 5 positive allosteric modulator.

Rosenbrock H, Kramer G, Hobson S, Koros E, Grundl M, Grauert M, Reymann KG, Schröder UH.

Eur J Pharmacol. 2010 Aug 10;639(1-3):40-6. doi: 10.1016/j.ejphar.2010.02.057. Epub 2010 Apr 2.

PMID:
20371241
4.

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.

6.

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.

7.

Recent patents on positive allosteric modulators of the metabotropic glutamate 5 receptor as a potential treatment for schizophrenia.

Kanuma K, Aoki T, Shimazaki Y.

Recent Pat CNS Drug Discov. 2010 Jan;5(1):23-34. Review.

PMID:
19832691
8.

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.

9.

Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target.

Parmentier-Batteur S, Hutson PH, Menzel K, Uslaner JM, Mattson BA, O'Brien JA, Magliaro BC, Forest T, Stump CA, Tynebor RM, Anthony NJ, Tucker TJ, Zhang XF, Gomez R, Huszar SL, Lambeng N, Fauré H, Le Poul E, Poli S, Rosahl TW, Rocher JP, Hargreaves R, Williams TM.

Neuropharmacology. 2014 Jul;82:161-73. doi: 10.1016/j.neuropharm.2012.12.003. Epub 2013 Jan 2.

PMID:
23291536
10.

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.

11.

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.

12.

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.

13.

The role of the mGluR allosteric modulation in the NMDA-hypofunction model of schizophrenia.

Doreulee N, Alania M, Mitaishvili E, Chikovani M, Chkhartishvili B.

Georgian Med News. 2009 Dec;(177):59-65.

PMID:
20090156
14.

The mGlu(4) receptor allosteric modulator N-phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide acts as a direct agonist at mGlu(6) receptors.

Beqollari D, Kammermeier PJ.

Eur J Pharmacol. 2008 Jul 28;589(1-3):49-52. doi: 10.1016/j.ejphar.2008.06.054. Epub 2008 Jun 19.

PMID:
18593581
15.

In vitro binding of a radio-labeled positive allosteric modulator for metabotropic glutamate receptor subtype 5.

Zysk JR, Spear N, Fieles W, Stein MM, Sygowski LS, King MM, Hoesch V, Hastings R, Brockel B, Do M, Ström P, Gadient R, Chhajlani V, Elmore CS, Maier DL.

Synapse. 2013 Mar;67(3):135-44. doi: 10.1002/syn.21625. Epub 2012 Dec 6.

PMID:
23150216
18.

mGlu(2) receptor-mediated modulation of conditioned avoidance behavior in rats.

Megens AA, Hendrickx HM, Hens KA, Talloen WJ, Lavreysen H.

Eur J Pharmacol. 2014 Mar 15;727:130-9. doi: 10.1016/j.ejphar.2014.01.044. Epub 2014 Jan 30.

PMID:
24486391
19.

The mGlu₅ positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat.

Gastambide F, Gilmour G, Robbins TW, Tricklebank MD.

Neuropharmacology. 2013 Jan;64:240-7. doi: 10.1016/j.neuropharm.2012.07.039. Epub 2012 Aug 1.

PMID:
22884612
20.

Group 5 metabotropic glutamate receptors: role in modulating cortical activity and relevance to cognition.

Homayoun H, Moghaddam B.

Eur J Pharmacol. 2010 Aug 10;639(1-3):33-9. doi: 10.1016/j.ejphar.2009.12.042. Epub 2010 Apr 2. Review.

PMID:
20371231

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