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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. Parmentier-Batteur S, et al. Neuropharmacology. 2014 Jul;82:161-73. doi: 10.1016/j.neuropharm.2012.12.003. Epub 2013 Jan 2. Neuropharmacology. 2014. PMID: 23291536
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. J Med Chem. 2004 Nov 18;47(24):5825-8. doi: 10.1021/jm049400d. J Med Chem. 2004. PMID: 15537338
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. Kinney GG, et al. J Pharmacol Exp Ther. 2005 Apr;313(1):199-206. doi: 10.1124/jpet.104.079244. Epub 2004 Dec 17. J Pharmacol Exp Ther. 2005. PMID: 15608073
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. Brnardic EJ, et al. Bioorg Med Chem Lett. 2010 May 15;20(10):3129-33. doi: 10.1016/j.bmcl.2010.03.089. Epub 2010 Mar 31. Bioorg Med Chem Lett. 2010. PMID: 20409708
260 results