کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376025 | 981948 | 2005 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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.
The discovery and structure–activity relationship (SAR) studies of a novel class of sodium channel blockers are disclosed.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 11, 2 June 2005, Pages 2943–2947
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 11, 2 June 2005, Pages 2943–2947
نویسندگان
Jun Liang, Richard M. Brochu, Charles J. Cohen, Ivy E. Dick, John P. Felix, Michael H. Fisher, Maria L. Garcia, Gregory J. Kaczorowski, Kathryn A. Lyons, Peter T. Meinke, Birgit T. Priest, William A. Schmalhofer, McHardy M. Smith, Jason W. Tarpley,