Premium
Manipulating transient receptor potential vanilloid 1 antagonists: How to cool down a hot molecule?
Author(s) -
Islas L. D.,
Szallasi A.
Publication year - 2018
Publication title -
acta physiologica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.591
H-Index - 116
eISSN - 1748-1716
pISSN - 1748-1708
DOI - 10.1111/apha.13088
Subject(s) - capsaicin , trpv1 , transient receptor potential channel , perspiration , chemistry , pungency , thermoreceptor , trpm8 , medicine , pharmacology , receptor , neuroscience , psychology , food science , pepper , psychiatry
TRPV1 is a promising pain target. Although a number of small molecule TRPV1 antagonists have been advanced into clinical trials, thus far none has progressed beyond Phase II due to on-target side-effects such as a febrile reaction. In this issue of Acta Physiologica, Romanovsky and colleagues report two TRPV1 antagonists that paradoxically induce hypothermia in experimental animals, potentially opening a new avenue for drug development. This article is protected by copyright. All rights reserved.