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J Med Chem. 2011 Mar 24;54(6):1724-39. doi: 10.1021/jm101414h. Epub 2011 Mar 2.

1-[(1-methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 positive allosteric modulators for the treatment of psychosis.

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  • 1Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, Connecticut 06340, United States. Lei.Zhang3@pfizer.com

Abstract

A novel series of mGluR2 positive allosteric modulators (PAMs), 1-[(1-methyl-1H-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, providing support for potential efficacy in treating psychosis.

PMID:
21366332
[PubMed - indexed for MEDLINE]
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