Literature DB >> 20709545

Substituted biaryl pyrazoles as sodium channel blockers.

Sriram Tyagarajan1, Prasun K Chakravarty, Bishan Zhou, Brett Taylor, Michael H Fisher, Mathew J Wyvratt, Kathy Lyons, Tracy Klatt, Xiaohua Li, Sanjeev Kumar, Brande Williams, John Felix, Birgit T Priest, Richard M Brochu, Vivien Warren, McHardy Smith, Maria Garcia, Gregory J Kaczorowski, William J Martin, Catherine Abbadie, Erin McGowan, Nina Jochnowitz, William H Parsons.   

Abstract

Voltage-gated sodium channels have been shown to play a critical role in neuropathic pain. A series of low molecular weight biaryl substituted pyrazole carboxamides were identified with good in-vitro potency and in-vivo efficacy. Compound 26, a Nav1.7 blocker has excellent efficacy in the Chung model of neuropathic pain. Copyright (c) 2010 Elsevier Ltd. All rights reserved.

Entities:  

Mesh:

Substances:

Year:  2010        PMID: 20709545     DOI: 10.1016/j.bmcl.2010.07.080

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


  4 in total

Review 1.  AMPK: An emerging target for modification of injury-induced pain plasticity.

Authors:  Theodore J Price; Gregory Dussor
Journal:  Neurosci Lett       Date:  2013-07-03       Impact factor: 3.046

2.  Targeting adenosine monophosphate-activated protein kinase (AMPK) in preclinical models reveals a potential mechanism for the treatment of neuropathic pain.

Authors:  Ohannes K Melemedjian; Marina N Asiedu; Dipti V Tillu; Raul Sanoja; Jin Yan; Arianna Lark; Arkady Khoutorsky; Jessica Johnson; Katherine A Peebles; Talya Lepow; Nahum Sonenberg; Gregory Dussor; Theodore J Price
Journal:  Mol Pain       Date:  2011-09-21       Impact factor: 3.395

3.  Recent developments regarding voltage-gated sodium channel blockers for the treatment of inherited and acquired neuropathic pain syndromes.

Authors:  Jonathan W Theile; Theodore R Cummins
Journal:  Front Pharmacol       Date:  2011-10-04       Impact factor: 5.810

4.  The AMPK Activator A769662 Blocks Voltage-Gated Sodium Channels: Discovery of a Novel Pharmacophore with Potential Utility for Analgesic Development.

Authors:  Marina N Asiedu; Chongyang Han; Sulayman D Dib-Hajj; Stephen G Waxman; Theodore J Price; Gregory Dussor
Journal:  PLoS One       Date:  2017-01-24       Impact factor: 3.240

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.