Discovery of (S, E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy) phenyl) ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7. 2) opener for the treatment of …

…, P Chen, H He, C Bourin, V Calandra, JL Polino…

文献索引：Wu, Yong-Jin; Conway, Charles M.; Sun, Li-Qiang; Machet, Frederic; Chen, Jie; Chen, Ping; He, Huan; Bourin, Clotilde; Calandra, Vincenzo; Polino, Joseph L.; Davis, Carl D.; Heman, Karen; Gribkoff, Valentin K.; Boissard, Christopher G.; Knox, Ronald J.; Thompson, Mark W.; Fitzpatrick, William; Weaver, David; Harden, David G.; Natale, Joanne; Dworetzky, Steven I.; Starrett Jr., John E. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 22 p. 6188 - 6191

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被引用次数: 7

摘要

Abstract Acrylamide (S)-6, a potent and efficacious KCNQ2 (Kv7. 2) opener, demonstrated significant activity in two models of neuropathic pain and in the formalin test, suggesting that KCNQ2 openers may be useful in the treatment of neuropathic pain including diabetic neuropathy.