Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain

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• 作者：Sharan K. Bagal ; Peter J. Bungay ; Stephen M. Denton ; Karl R. Gibson ; Melanie S. Glossop ; Tanya L. Hay ; Mark I. Kemp ; Charlotte A. L. Lane ; Mark L. Lewis ; Graham N. Maw ; William A. Million ; C. Elizabeth Payne ; Cedric Poinsard ; David J. Rawson ; Blanda L. Stammen ; Edward B. Stevens ; Lisa R. Thompson
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2015
• 出版时间：June 11, 2015
• 年：2015
• 卷：6
• 期：6
• 页码：650-654
• 全文大小：305K
• ISSN：1948-5875

文摘

Voltage-gated sodium channels, in particular Na_v1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we described the optimization of Na_v1.8 modulator series to deliver subtype selective, state, and use-dependent chemical matter that is efficacious in preclinical models of neuropathic and inflammatory pain.