RESEARCH ARTICLE
Targeting TRPM8 for Pain Relief
Carlos Fernández-Peña, Felix Viana*
Article Information
Identifiers and Pagination:
Year: 2013Volume: 6
First Page: 154
Last Page: 164
Publisher ID: TOPAINJ-6-154
DOI: 10.2174/1876386301306010154
Article History:
Received Date: 09/08/2012Revision Received Date: 09/08/2012
Acceptance Date: 16/08/2012
Electronic publication date: 08/3/2013
Collection year: 2013
open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 International Public License (CC-BY 4.0), a copy of which is available at: https://creativecommons.org/licenses/by/4.0/legalcode. This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Abstract
Transient receptor potential melastatin 8 (TRPM8) is a non-selective cation channel activated by cold temperature and cooling agents. TRPM8 is expressed in peripheral cold thermoreceptors and plays a fundamental role in sensing mild, cool temperatures. In addition, cumulative evidence obtained in humans and different animals models, combined with pharmacological and gene silencing techniques, suggest that TRPM8 may also play a role in cold discomfort and the pathophysiology of cold pain. This article reviews the available evidence in a critical fashion. In addition, the article reviews the possible role of TRPM8 in basal tearing, cold urticaria and airway irritation. Collectively, these results suggest that pharmacological modulators of TRPM8 could have potential indications in a variety of conditions, including dry eye disease, airway irritation, teeth hypersensitivity, migraine and neuropathic pain. However, additional studies, especially in humans, are needed to verify these preliminary observations. The paucity of potent, specific pharmacological TRPM8 antagonists available is a current limitation for further progress in this field.