Concepedia

Discovery and Optimization of Selective Na <sub>v</sub> 1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain

Sharan K. Bagal, Peter J. Bungay, Stephen M. Denton, Karl R. Gibson, Melanie S. Glossop, Tanya Hay, Mark I. Kemp, Charlotte A. L. Lane, Mark L. Lewis, Graham N. Maw,

ACS Medicinal Chemistry Letters · 2015 · 41 citations · 15 references

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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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