Cregg, R;
Cox, JJ;
Bennett, DL;
Wood, JN;
Werdehausen, R;
(2014)
Mexiletine as a treatment for primary erythromelalgia: normalization of biophysical properties of mutant L858F NaV 1.7 sodium channels.
Br J Pharmacol
, 171
(19)
pp. 4455-4563.
10.1111/bph.12788.
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Abstract
The non-selective sodium channel inhibitor mexiletine has been found to be effective in several animal models of chronic pain and became popular in the clinical setting as an orally available alternative to lidocaine. It remains unclear why patients with monogenic pain disorders secondary to gain-of-function SCN9a mutations benefit from a low systemic concentration of mexiletine, which usually does not induce adverse neurologic effects. The aim of this study was therefore to investigate the biophysical effects of mexiletine on the L858F primary erythromelalgia NaV 1.7 mutation in vitro.
| Type: | Article |
|---|---|
| Title: | Mexiletine as a treatment for primary erythromelalgia: normalization of biophysical properties of mutant L858F NaV 1.7 sodium channels. |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1111/bph.12788 |
| Publisher version: | http://dx.doi.org/10.1111/bph.12788 |
| Additional information: | © 2014 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of The British Pharmacological Society. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. |
| Keywords: | Mexiletine, NaV1.7, erythromelalgia, gain-of-function mutations, neuropathic pain, voltage-gated sodium channels |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine > Wolfson Inst for Biomedical Research UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Surgery and Interventional Sci UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Surgery and Interventional Sci > Department of Targeted Intervention |
| URI: | https://discovery.ucl.ac.uk/id/eprint/1431220 |
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