Bioorganic and Medicinal Chemistry Letters p. 4630 - 4634 (2007)
Update date:2022-08-03
Topics:
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.
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.
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