Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.
Scott B Hoyt, Clare London, Hyun Ok, Edward Gonzalez, Joseph L Duffy, Catherine Abbadie, Brian Dean, John P Felix, Maria L Garcia, Nina Jochnowitz, Bindhu V Karanam, Xiaohua Li, Kathryn A Lyons, Erin McGowan, D Euan Macintyre, William J Martin, Birgit T Priest, McHardy M Smith, Richard Tschirret-Guth, Vivien A Warren, Brande S Williams, Gregory J Kaczorowski, William H Parsons
Index: Bioorg. Med. Chem. Lett. 17(22) , 6172-7, (2007)
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Abstract
A series of benzazepinones were synthesized and evaluated as hNa(v)1.7 sodium channel blockers. Several compounds from this series displayed good oral bioavailability and exposure and were efficacious in a rat model of neuropathic pain.
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[Biochem. Pharmacol. 44(10) , 1935-46, (1992)]