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

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.

SUBMITTER: Bagal SK

PROVIDER: S-EPMC4468395 | biostudies-literature | 2015 Jun

REPOSITORIES: biostudies-literature

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

Bagal Sharan K SK Bungay Peter J PJ Denton Stephen M SM Gibson Karl R KR Glossop Melanie S MS Hay Tanya L TL Kemp Mark I MI Lane Charlotte A L CA Lewis Mark L ML Maw Graham N GN Million William A WA Payne C Elizabeth CE Poinsard Cedric C Rawson David J DJ Stammen Blanda L BL Stevens Edward B EB Thompson Lisa R LR

ACS medicinal chemistry letters 20150429 6

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. ...[more]

PMID: 26101568

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