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Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain |
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| Authors: | Liang Jun Brochu Richard M Cohen Charles J Dick Ivy E Felix John P Fisher Michael H Garcia Maria L Kaczorowski Gregory J Lyons Kathryn A Meinke Peter T Priest Birgit T Schmalhofer William A Smith McHardy M Tarpley Jason W Williams Brande S Martin William J Parsons William H |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. jun_liang@merck.com |
| Abstract: | 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. |
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