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

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

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.

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2013-11, Vol.23 (22), p.6188-6191
Hauptverfasser: 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, John E
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Sprache:eng
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Zusammenfassung: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.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2013.08.092