1276655-77-6Relevant articles and documents
1-[(1-methyl-1 H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 positive allosteric modulators for the treatment of psychosis
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.
, p. 1724 - 1739 (2011)
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.
