Article ID Journal Published Year Pages File Type
10596707 Bioorganic & Medicinal Chemistry Letters 2010 5 Pages PDF
Abstract
Development of SAR in a 3-cyano-5-fluoro-N-arylbenzamide series of non-competitive antagonists of mGlu5 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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Physical Sciences and Engineering Chemistry Organic Chemistry
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