Imidazopyridines: A novel class of hNav1.7 channel blockers
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- 作者：Clare London ; Scott B. Hoyt ; William H. Parsons ; Br ; e S. Williams ; Vivien A. Warren ; Richard Tschirret-Guth ; McHardy M. Smith ; Birgit T. Priest ; Erin McGowan ; William J. Martin ; Kathryn A. Lyons ; Xiao
- 关键词：Sodium channel blockers ; hNav1.7 ; Neuropathic pain ; Voltage-gated sodium channels
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：1 March 2008
- 年：2008
- 卷：18
- 期：5
- 页码：1696-1701
- 全文大小：146 K
文摘
A series of imidazopyridines were evaluated as potential sodium channel blockers for the treatment of neuropathic pain. Several members were identified with good hNav1.7 potency and excellent rat pharmacokinetic profiles. Compound 4 had good efficacy (52 % and 41 % reversal of allodynia at 2 and 4 h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain when dosed orally at 10 mg/kg.