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3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu5: Identification of easily prepared tool compounds with CNS exposure in rats

✍ Scribed by Andrew S. Felts; Stacey R. Lindsley; Jeffrey P. Lamb; Alice L. Rodriguez; Usha N. Menon; Satyawan Jadhav; Carrie K. Jones; P. Jeffrey Conn; Craig W. Lindsley; Kyle A. Emmitte

Book ID: 104004542
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 224 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.06.064

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✦ Synopsis

Development of SAR in a 3-cyano-5-fluoro-N-arylbenzamide series of non-competitive antagonists of mGlu 5 using a functional cell-based assay is described in this Letter. Further characterization of selected potent compounds in in vitro assays designed to measure their metabolic stability and protein binding is also presented. Subsequent evaluation of two new compounds in pharmacokinetic studies using intraperitoneal dosing in rats demonstrated good exposure in both plasma and brain samples.

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