Abstract |
A series of benzazepinones were synthesized and evaluated for block of Nav1.7 sodium channels. Compound 30 from this series displayed potent channel block, good selectivity versus other targets, and dose-dependent oral efficacy in a rat model of neuropathic pain.
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Authors | Scott B Hoyt, Clare London, Catherine Abbadie, John P Felix, Maria L Garcia, Nina Jochnowitz, Bindhu V Karanam, Xiaohua Li, Kathryn A Lyons, Erin McGowan, Birgit T Priest, McHardy M Smith, Vivien A Warren, Brande S Thomas-Fowlkes, Gregory J Kaczorowski, Joseph L Duffy |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 23
Issue 12
Pg. 3640-5
(Jun 15 2013)
ISSN: 1464-3405 [Electronic] England |
PMID | 23652221
(Publication Type: Letter)
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Copyright | Copyright © 2013 Elsevier Ltd. All rights reserved. |
Chemical References |
- Benzazepines
- Sodium Channel Blockers
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Topics |
- Animals
- Benzazepines
(pharmacology)
- Disease Models, Animal
- Neuralgia
(drug therapy)
- Rats
- Sodium Channel Blockers
(pharmacology)
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