Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain

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• 作者：Liang ; Jun ; Brochu ; Richard M. ; Cohen ; Charles J. ; Dick ; Ivy E. ; Felix ; John P. ; Fisher ; Michael H. ; et. al.
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：June 2, 2005
• 年：2005
• 卷：15
• 期：11
• 页码：2943-2947
• 全文大小：217 K

文摘

A new series of voltage-gated sodium channel blockers with potential for treatment of chronic pain is reported. Systematic structure–activity relationship studies, starting with compound 1, led to identification of potent analogs that displayed use-dependent block of sodium channels, were efficacious in pain models in vivo, and most importantly, were devoid of activity against the cardiac potassium channel hERG.