Channelpedia

PubMed 25455494


Referenced in Channelpedia wiki pages of: none

Automatically associated channels: Kir2.3 , TRP , TRPA , TRPA1 , TRPM , TRPM8 , TRPV , TRPV1



Title: Effect of acyclic monoterpene alcohols and their derivatives on TRP channels.

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

Journal, date & volume: Bioorg. Med. Chem. Lett., 2014 Dec 1 , 24, 5507-11

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/25455494


Abstract
A series of thirty-six geraniol, nerol, citronellol, geranylamine, and nerylamine derivatives was synthesized and tested on TRPA1, TRPM8, and TRPV1 channels. Most of them acted as strong modulators of TRPA1 channels with EC50 and/or IC50 values <1 μM. None was able to significantly activate TRPM8 channels, while thirteen of them behaved as 'true' TRPM8 antagonists. Little or no effect was generally observed on TRPV1 channels. Some of the compounds examined, that is, compounds 1d,g,n, 2c,d,h,i,o, 3b,e exhibited an appreciable selectivity for TRPA1 subtype.