950509-61-2Relevant articles and documents
Discovery of a novel class of benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain
Hoyt, Scott B.,London, Clare,Gorin, David,Wyvratt, Matthew J.,Fisher, Michael H.,Abbadie, Catherine,Felix, John P.,Garcia, Maria L.,Li, Xiaohua,Lyons, Kathryn A.,McGowan, Erin,MacIntyre, D. Euan,Martin, William J.,Priest, Birgit T.,Ritter, Amy,Smith, McHardy M.,Warren, Vivien A.,Williams, Brande S.,Kaczorowski, Gregory J.,Parsons, William H.
, p. 4630 - 4634 (2008/02/10)
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.