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

发现和优化在疼痛临床前模型中证明有效的选择性 Nav1.8 调节剂系列

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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

期刊：

ACS Medicinal Chemistry Letters

影响因子：

3.500

时间：

2015

起止号：

2015 Apr 29;6(6):650-4.

doi：

10.1021/acsmedchemlett.5b00059

Abstract

Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we described the optimization of Nav1.8 modulator series to deliver subtype selective, state, and use-dependent chemical matter that is efficacious in preclinical models of neuropathic and inflammatory pain.

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