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Items: 1 to 20 of 101

1.

Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor.

Garbaccio RM, Brnardic EJ, Fraley ME, Hartman GD, Hutson PH, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Small JH, Tang C, Kuo Y, Jacobson MA.

ACS Med Chem Lett. 2010 Jul 12;1(8):406-10. doi: 10.1021/ml100115a. eCollection 2010 Nov 11.

2.

Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.

Pero JE, Rossi MA, Kelly MJ 3rd, Lehman HD, Layton ME, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Joyce LA, Sherer EC, Jacobson MA.

ACS Med Chem Lett. 2016 Jan 10;7(3):312-7. doi: 10.1021/acsmedchemlett.5b00459. eCollection 2016 Mar 10.

3.

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.

4.

Positive allosteric modulators of the metabotropic glutamate receptor 2 for the treatment of schizophrenia.

Fraley ME.

Expert Opin Ther Pat. 2009 Sep;19(9):1259-75. doi: 10.1517/13543770903045009. Review.

PMID:
19552508
5.

3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.

Brnardic EJ, Fraley ME, Garbaccio RM, Layton ME, Sanders JM, Culberson C, Jacobson MA, Magliaro BC, Hutson PH, O'Brien JA, Huszar SL, Uslaner JM, Fillgrove KL, Tang C, Kuo Y, Sur SM, Hartman GD.

Bioorg Med Chem Lett. 2010 May 15;20(10):3129-33. doi: 10.1016/j.bmcl.2010.03.089. Epub 2010 Mar 31.

PMID:
20409708
6.

Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.

Layton ME, Reif AJ, Hartingh TJ, Rodzinak K, Dudkin V, Wang C, Arrington K, Kelly MJ 3rd, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Jacobson MA.

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1260-4. doi: 10.1016/j.bmcl.2016.01.021. Epub 2016 Jan 11.

PMID:
26810316
7.

Selective potentiation of the metabotropic glutamate receptor subtype 2 blocks phencyclidine-induced hyperlocomotion and brain activation.

Hackler EA, Byun NE, Jones CK, Williams JM, Baheza R, Sengupta S, Grier MD, Avison M, Conn PJ, Gore JC.

Neuroscience. 2010 Jun 16;168(1):209-18. doi: 10.1016/j.neuroscience.2010.02.057. Epub 2010 Mar 27.

8.

3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization.

Duplantier AJ, Efremov I, Candler J, Doran AC, Ganong AH, Haas JA, Hanks AN, Kraus KG, Lazzaro JT Jr, Lu J, Maklad N, McCarthy SA, O'Sullivan TJ, Rogers BN, Siuciak JA, Spracklin DK, Zhang L.

Bioorg Med Chem Lett. 2009 May 1;19(9):2524-9. doi: 10.1016/j.bmcl.2009.03.032. Epub 2009 Mar 14.

PMID:
19328692
9.

Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.

Nakazato A, Kumagai T, Sakagami K, Yoshikawa R, Suzuki Y, Chaki S, Ito H, Taguchi T, Nakanishi S, Okuyama S.

J Med Chem. 2000 Dec 14;43(25):4893-909.

PMID:
11123999
10.

Discovery of positive allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5).

Williams DL Jr, Lindsley CW.

Curr Top Med Chem. 2005;5(9):825-46. Review.

PMID:
16178729
11.

Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.

Cid JM, Duvey G, Cluzeau P, Nhem V, Macary K, Raux A, Poirier N, Muller J, Boléa C, Finn T, Poli S, Epping-Jordan M, Chamelot E, Derouet F, Girard F, Macdonald GJ, Vega JA, de Lucas AI, Matesanz E, Lavreysen H, Linares ML, Oehlrich D, Oyarzábal J, Tresadern G, Trabanco AA, Andrés JI, Le Poul E, Imogai H, Lutjens R, Rocher JP.

ACS Chem Neurosci. 2010 Dec 15;1(12):788-95. doi: 10.1021/cn1000638. Epub 2010 Aug 23.

12.

A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors.

Hemstapat K, Da Costa H, Nong Y, Brady AE, Luo Q, Niswender CM, Tamagnan GD, Conn PJ.

J Pharmacol Exp Ther. 2007 Jul;322(1):254-64. Epub 2007 Apr 6.

13.

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, Conn PJ.

J Pharmacol Exp Ther. 2006 Jul;318(1):173-85. Epub 2006 Apr 11.

14.

The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.

D'Alessandro PL, Corti C, Roth A, Ugolini A, Sava A, Montanari D, Bianchi F, Garland SL, Powney B, Koppe EL, Rocheville M, Osborne G, Perez P, de la Fuente J, De Los Frailes M, Smith PW, Branch C, Nash D, Watson SP.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):759-62. doi: 10.1016/j.bmcl.2009.11.032. Epub 2009 Nov 26.

PMID:
20005096
15.

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.

16.

Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia.

Conn PJ, Lindsley CW, Jones CK.

Trends Pharmacol Sci. 2009 Jan;30(1):25-31. doi: 10.1016/j.tips.2008.10.006. Epub 2008 Dec 6. Review.

17.

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.

Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Garcia-Barrantes PM, Lavreysen H, Mackie C, Vinson PN, Rook JM, Bridges TM, Daniels JS, Megens A, Langlois X, Drinkenburg WH, Ahnaou A, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW.

ACS Med Chem Lett. 2015 May 20;6(6):716-20. doi: 10.1021/acsmedchemlett.5b00181. eCollection 2015 Jun 11.

19.

3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: a novel series of mGluR2 positive allosteric modulators.

Zhang L, Rogers BN, Duplantier AJ, McHardy SF, Efremov I, Berke H, Qian W, Zhang AQ, Maklad N, Candler J, Doran AC, Lazzaro JT Jr, Ganong AH.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5493-6. doi: 10.1016/j.bmcl.2008.09.026. Epub 2008 Sep 10.

PMID:
18812259
20.

Metabotropic glutamate receptors for new treatments in schizophrenia.

Herman EJ, Bubser M, Conn PJ, Jones CK.

Handb Exp Pharmacol. 2012;(213):297-365. doi: 10.1007/978-3-642-25758-2_11. Review.

PMID:
23027420

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