Discovery of a novel class of benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain
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- 作者：Scott B. Hoyt ; Clare London ; David Gorin ; Matthew J. Wyvratt ; Michael H. Fisher ; Catherine Abbadie ; John P. Felix ; Maria L. Garcia ; Xiaohua Li ; Kathryn A. Lyons ; Erin McGowan ; D. Euan MacIntyre ; Willi
- 关键词：Sodium channel ; Neuropathic pain ; Nav1.7 ; Benzazepinone ; Benzodiazepine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：15 August 2007
- 年：2007
- 卷：17
- 期：16
- 页码：4630-4634
- 全文大小：151 K
文摘
A series of benzodiazepines and benzazepinones were synthesized and evaluated as potential sodium channel blockers in a functional, membrane potential-based assay. One member of the benzazepinone series, compound 47, displayed potent, state-dependent block of hNav1.7, and was orally efficacious in a rat model of neuropathic pain.