Literature DB >> 24070783

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.

Yong-Jin Wu1, Charles M Conway, Li-Qiang Sun, Frederic Machet, Jie Chen, Ping Chen, Huan He, Clotilde Bourin, Vincenzo Calandra, Joseph L Polino, Carl D Davis, Karen Heman, Valentin K Gribkoff, Christopher G Boissard, Ronald J Knox, Mark W Thompson, William Fitzpatrick, David Weaver, David G Harden, Joanne Natale, Steven I Dworetzky, John E Starrett.   

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.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Acrylamide; Diabetic neuropathy; KCNQ2; Kv7.2; Neuropathic pain

Mesh：

Substances：

Year:  2013        PMID： 24070783     DOI： 10.1016/j.bmcl.2013.08.092

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Breaking barriers to novel analgesic drug development.

Authors:  Ajay S Yekkirala; David P Roberson; Bruce P Bean; Clifford J Woolf
Journal:  Nat Rev Drug Discov       Date:  2017-06-09       Impact factor: 84.694

Review 2.  Chemical modulation of Kv7 potassium channels.

Authors:  Matteo Borgini; Pravat Mondal; Ruiting Liu; Peter Wipf
Journal:  RSC Med Chem       Date:  2021-01-14

Review 3.  M-type K+ channels in peripheral nociceptive pathways.

Authors:  Xiaona Du; Haixia Gao; David Jaffe; Hailin Zhang; Nikita Gamper
Journal:  Br J Pharmacol       Date:  2017-09-17       Impact factor: 8.739

4.  RNA interference-based functional knockdown of the voltage-gated potassium channel Kv7.2 in dorsal root ganglion neurons after in vitro and in vivo gene transfer by adeno-associated virus vectors.

Authors:  Markus Valdor; Anke Wagner; Viola Röhrs; Johanna Berg; Henry Fechner; Wolfgang Schröder; Thomas M Tzschentke; Gregor Bahrenberg; Thomas Christoph; Jens Kurreck
Journal:  Mol Pain       Date:  2017-12-06       Impact factor: 3.395
  4 in total

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