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Weaver Lab

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 neuropathic pain.

AUTHORS

Wu YJYong-Jin , Conway CM Charles M , Sun LQ Li-Qiang , Machet F Frederic , Chen J Jie , Chen P Ping , He H Huan , Bourin C Clotilde , Calandra V Vincenzo , Polino JL Joseph L , Davis CD Carl D , Heman K Karen , Gribkoff VK Valentin K , Boissard CG Christopher G , Knox RJ Ronald J , Thompson MW Mark W , Fitzpatrick W William , Weaver D David , Harden DG David G , Natale J Joanne , Dworetzky SI Steven I , Starrett JE John E . Bioorganic & medicinal chemistry letters. 2013 11 15; 23(22). 6188-91

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.

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.