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N-Acyl-N′-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats

✍ Scribed by Lovell, Kimberly M.; Felts, Andrew S.; Rodriguez, Alice L.; Venable, Daryl F.; Cho, Hyekyung P.; Morrison, Ryan D.; Byers, Frank W.; Daniels, J. Scott; Niswender, Colleen M.; Conn, P. Jeffrey; Lindsley, Craig W.; Emmitte, Kyle A.

Book ID: 122414112
Publisher: Elsevier Science
Year: 2013
Tongue: English
Weight: 694 KB
Volume: 23
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2013.05.020

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✍ Andrew S. Felts; Stacey R. Lindsley; Jeffrey P. Lamb; Alice L. Rodriguez; Usha N 📂 Article 📅 2010 🏛 Elsevier Science 🌐 English ⚖ 224 KB

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