Title of article
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain Original Research Article
Author/Authors
Irene Drizin، نويسنده , , Robert J. Gregg، نويسنده , , Marc J.C. Scanio، نويسنده , , Lei Shi، نويسنده , , Michael F. Gross، نويسنده , , Robert N. Atkinson، نويسنده , , James B. Thomas، نويسنده , , Matthew S. Johnson، نويسنده , , William A. Carroll، نويسنده , , Brian E. Marron، نويسنده , , Mark L. Chapman، نويسنده , , Dong Liu، نويسنده , , Michael J. Krambis، نويسنده , , Char-Chang Shieh، نويسنده , , XuFeng Zhang، نويسنده , , Gricelda Hernandez، نويسنده , , Donna M. Gauvin، نويسنده , , Joseph P. Mikusa، نويسنده , , Chang Z. Zhu، نويسنده , , Shailen Joshi، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
8
From page
6379
To page
6386
Abstract
The synthesis and pharmacological characterization of a novel furan-based class of voltage-gated sodium channel blockers is reported. Compounds were evaluated for their ability to block the tetrodotoxin-resistant sodium channel Nav1.8 (PN3) as well as the Nav1.2 and Nav1.5 subtypes. Benchmark compounds from this series possessed enhanced potency, oral bioavailability, and robust efficacy in a rodent model of neuropathic pain, together with improved CNS and cardiovascular safety profiles compared to the clinically used sodium channel blockers mexiletine and lamotrigine.
Keywords
sodium channels , PN3 , Nav1.8 , Furan piperazine , Blocker , Voltage-gated , Pain
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2008
Journal title
Bioorganic and Medicinal Chemistry
Record number
1304442
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