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ADX-47273

ADX 47273 is a positive allosteric modulator of metabotropic glutamate receptor mGluR5 that displays antipsychotic, neuromodulatory, and cognition enhancing activities. In vivo, ADX 47273 increases waking and decreases deep sleep behaviors; it also increases late phase long-term potentiation (LTP) and enhances adaptive learning. In other animal models, ADX 47273 decreases amphetamine- and phencyclidine-induced hyperlocomotion and accumbal dopamine levels.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18836567

Cas No.

851881-60-2

Formula

C20H17F2N3O2

Formula Wt.

369.36

Ahnaou A, Langlois X, Steckler T, et al. Negative versus positive allosteric modulation of metabotropic glutamate receptors (mGluR5): indices for potential pro-cognitive drug properties based on EEG network oscillations and sleep-wake organization in rats. Psychopharmacology (Berl). 2015 Mar;232(6):1107-22. PMID: 25323624.

Xu J, Zhu Y, Kraniotis S, et al. Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning. Learn Mem. 2013 Jul 18;20(8):438-45. PMID: 23869026.

Kroker KS, Rast G, Rosenbrock H. Differential effect of the mGlu5 receptor positive allosteric modulator ADX-47273 on early and late hippocampal LTP. Neuropharmacology. 2011 Sep;61(4):707-14. PMID: 21640734.

Schlumberger C, Pietraszek M, Gravius A, et al. Comparison of the mGlu(5) receptor positive allosteric modulator ADX47273 and the mGlu(2/3) receptor agonist LY354740 in tests for antipsychotic-like activity. Eur J Pharmacol. 2009 Nov 25;623(1-3):73-83. PMID: 19765575.

Liu F, Grauer S, Kelley C, et al. 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. J Pharmacol Exp Ther. 2008 Dec;327(3):827-39. PMID: 18753411.

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