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

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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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2013-11, Vol.23 (22), p.6188-6191
Main Authors: 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.
Format: Article
Language:English
Subjects:
Acrylamide
acrylamides
Acrylamides - chemical synthesis
Acrylamides - chemistry
Acrylamides - pharmacology
Animals
chemistry
Diabetic neuropathy
formalin
KCNQ2
KCNQ2 Potassium Channel - chemistry
KCNQ2 Potassium Channel - metabolism
Kv7.2
Male
Neuralgia - drug therapy
Neuropathic pain
pain
Patch-Clamp Techniques
Rats
Rats, Sprague-Dawley
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Description
Summary: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
1464-3405
DOI:10.1016/j.bmcl.2013.08.092