کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1360582 | 981441 | 2008 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 12, 15 June 2008, Pages 6379–6386
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 12, 15 June 2008, Pages 6379–6386
نویسندگان
Irene Drizin, Robert J. Gregg, Marc J.C. Scanio, Lei Shi, Michael F. Gross, Robert N. Atkinson, James B. Thomas, Matthew S. Johnson, William A. Carroll, Brian E. Marron, Mark L. Chapman, Dong Liu, Michael J. Krambis, Char-Chang Shieh, XuFeng Zhang,