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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. Gregory KJ, et al. Among authors: conn pj. J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. doi: 10.1124/jpet.113.206623. Epub 2013 Aug 21. J Pharmacol Exp Ther. 2013. PMID: 23965381 Free PMC article.
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. O'Brien JA, et al. Among authors: conn pj. J Pharmacol Exp Ther. 2004 May;309(2):568-77. doi: 10.1124/jpet.103.061747. Epub 2004 Jan 27. J Pharmacol Exp Ther. 2004. PMID: 14747613
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL Jr, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR. Lindsley CW, et al. Among authors: conn pj. J Med Chem. 2004 Nov 18;47(24):5825-8. doi: 10.1021/jm049400d. J Med Chem. 2004. PMID: 15537338
498 results