UCL Discovery
UCL home » Library Services » Electronic resources » UCL Discovery

Nav1.7 and other voltage-gated sodium channels as drug targets for pain relief

Emery, EC; Luiz, AP; Wood, JN; (2016) Nav1.7 and other voltage-gated sodium channels as drug targets for pain relief. Expert Opinion on Therapeutic Targets , 20 (8) pp. 975-983. 10.1517/14728222.2016.1162295. Green open access

[img]
Preview
Text
Emery_Nav1 7.pdf - Published version

Download (1MB) | Preview

Abstract

INTRODUCTION: Chronic pain is a massive clinical problem. We discuss the potential of subtype selective sodium channel blockers that may provide analgesia with limited side effects. AREAS COVERED: Sodium channel subtypes have been linked to human pain syndromes through genetic studies. Gain of function mutations in Nav1.7, 1.8 and 1.9 can cause pain, whilst loss of function Nav1.7 mutations lead to loss of pain in otherwise normal people. Intriguingly, both human and mouse Nav1.7 null mutants have increased opioid drive, because naloxone, an opioid antagonist, can reverse the analgesia associated with the loss of Nav1.7 expression. EXPERT OPINION: We believe there is a great future for sodium channel antagonists, particularly Nav1.7 antagonists in treating most pain syndromes. This review deals with recent attempts to develop specific sodium channel blockers, the mechanisms that underpin the Nav1.7 null pain-free phenotype and new routes to analgesia using, for example, gene therapy or combination therapy with subtype specific sodium channel blockers and opioids. The use of selective Nav1.7 antagonists together with either enkephalinase inhibitors or low dose opioids has the potential for side effect-free analgesia, as well as an important opioid sparing function that may be clinically very significant.

Type: Article
Title: Nav1.7 and other voltage-gated sodium channels as drug targets for pain relief
Location: England
Open access status: An open access version is available from UCL Discovery
DOI: 10.1517/14728222.2016.1162295
Publisher version: http://dx.doi.org/10.1517/14728222.2016.1162295
Additional information: © 2016 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Keywords: Nav1.7, SCN9A, opioids, pain, sensory neurons
UCL classification: UCL
UCL > Provost and Vice Provost Offices
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
URI: https://discovery.ucl.ac.uk/id/eprint/1490294
Downloads since deposit
460Downloads
Download activity - last month
Download activity - last 12 months
Downloads by country - last 12 months

Archive Staff Only

View Item View Item