1-[(1-Methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 Positive Allosteric Modulators for the Treatment of Psychosis
Journal of Medicinal Chemistry March 2, 2011 Lei Zhang, Michael A. Brodney, John Candler et al. 32 citations
A new class of compounds, 1-[(1-methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines, acts as positive allosteric modulators (PAMs) of the metabotropic glutamate receptor 2 (mGluR2). Structure-activity relationship studies produced potent and selective mGluR2 PAMs with favorable pharmacokinetic properties. The lead compound (+)-17e dose-dependently reduced methamphetamine-induced hyperactivity and mescaline-induced scratching in mice, suggesting potential for treating psychosis.