Channelpedia

PubMed 22503249


Referenced in: none

Automatically associated channels: Kir2.3 , TRP , TRPA , TRPA1 , TRPM , TRPM8 , TRPV , TRPV3



Title: Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds.

Authors: Giorgio Ortar, Ludovica Morera, Aniello Schiano Moriello, Enrico Morera, Marianna Nalli, Vincenzo Di Marzo, Luciano De Petrocellis

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 May 15 , 22, 3535-9

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22503249


Abstract
A series of thirty-three thymol, p-cymene-3-carboxylic acid, and 3-amino-p-cymene derivatives was synthesized and tested on TRPA1, TRPM8, and TRPV3 channels. Most of them acted as strong modulators of TRPA1, TRPM8, and TRPV3 channels with EC(50) and/or IC(50) values distinctly lower than those of thymol and related monoterpenoids. Some of the compounds examined, that is, 3c, 4e, f, 6b, and 8b exhibited an appreciable subtype-selectivity.