1-[(1-Methyl-1 H-imidazol-2-yl) methyl]-4-phenylpiperidines as mGluR2 Positive Allosteric Modulators for the Treatment of Psychosis

…, J Candler, AC Doran, AJ Duplantier…

Index: Zhang, Lei; Brodney, Michael A.; Candler, John; Doran, Angela C.; Duplantier, Allen J.; Efremov, Ivan V.; Evrard, Edel; Kraus, Kenneth; Ganong, Alan H.; Haas, Jessica A.; Hanks, Ashley N.; Jenza, Keith; Lazzaro, John T.; Maklad, Noha; McCarthy, Sheryl A.; Qian, Weimin; Rogers, Bruce N.; Rottas, Melinda D.; Schmidt, Christopher J.; Siuciak, Judith A.; Tingley III, F. David; Zhang, Andy Q. Journal of Medicinal Chemistry, 2011 , vol. 54, # 6 p. 1724 - 1739

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Citation Number: 13

Abstract

A novel series of mGluR2 positive allosteric modulators (PAMs), 1-[(1-methyl-1 H-imidazol-2- yl) methyl]-4-phenylpiperidines, is herein disclosed. Structure− activity relationship studies led to potent, selective mGluR2 PAMs with excellent pharmacokinetic profiles. A representative lead compound (+)-17e demonstrated dose-dependent inhibition of methamphetamine-induced hyperactivity and mescaline-induced scratching in mice, ...