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The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics

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Abstract

In this article, we describe the discovery of an aryl ether series of potent and selective Nav1.3 inhibitors. Based on structural analogy to a similar series of compounds we have previously shown bind to the domain IV voltage sensor region of Nav channels, we propose this series binds in the same location. We describe the development of this series from a published starting point, highlighting key selectivity and potency data, and several studies designed to validate Nav1.3 as a target for pain.

Graphical abstract: The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics

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Publication details

The article was received on 14 Mar 2017, accepted on 26 Apr 2017 and first published on 28 Apr 2017


Article type: Research Article
DOI: 10.1039/C7MD00131B
Citation: Med. Chem. Commun., 2017, Advance Article
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    The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics

    D. C. Pryde, N. A. Swain, P. A. Stupple, C. W. West, B. Marron, C. J. Markworth, D. Printzenhoff, Z. Lin, P. J. Cox, R. Suzuki, S. McMurray, G. J. Waldron, C. E. Payne, J. S. Warmus and M. L. Chapman, Med. Chem. Commun., 2017, Advance Article , DOI: 10.1039/C7MD00131B

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