Details

Autor(en) / Beteiligte

• 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, F. David
• Zhang, Andy Q

Titel

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

Ist Teil von

• Journal of medicinal chemistry, 2011-03, Vol.54 (6), p.1724-1739

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2011

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.