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Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): efficacy in an animal model for schizophrenia.
Govek SP,
Bonnefous C,
Hutchinson JH,
Kamenecka T,
McQuiston J,
Pracitto R,
Zhao LX,
Gardner MF,
James JK,
Daggett LP,
Rowe BA,
Schaffhauser H,
Bristow LJ,
Campbell UC,
Rodriguez DE,
Vernier 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.
PMID: 16005222 [PubMed - indexed for MEDLINE]
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