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Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): efficacy in an animal model for schizophrenia.

Bioorganic & medicinal chemistry letters 2005 Sep 15; 15(18):4068-72

Link to PubMed abstract

Govek S SP, Bonnefous C C, Hutchinson J JH, Kamenecka T T, McQuiston J J, Pracitto R R, Zhao L LX, Gardner M MF, James J JK, Daggett L LP, Rowe B BA, Schaffhauser H H, Bristow L LJ, Campbell U UC, Rodriguez D DE, Vernier J JM

Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA. sgovek@san.rr.com

Metabotropic glutamate receptor 2 (mGluR2) has been implicated in a variety of CNS disorders, including schizophrenia. Disclosed herein is the development of a new series of allosteric potentiators of mGluR2. Structure-activity relationship studies in conjunction with pharmacokinetic data led to the discovery of indole 5, which is active in an animal model for schizophrenia.