Channelpedia

PubMed 23203269


Referenced in Channelpedia wiki pages of: none

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



Title: Leucettamols, bifunctionalized marine sphingoids, act as modulators of TRPA1 and TRPM8 channels.

Authors: Giuseppina Chianese, Ernesto Fattorusso, Masteria Yunovilsa Putra, Barbara Calcinai, Giorgio Bavestrello, Aniello Schiano Moriello, Luciano De Petrocellis, Vincenzo Di Marzo, Orazio Taglialatela-Scafati

Journal, date & volume: Mar Drugs, 2012 Nov , 10, 2435-47

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23203269


Abstract
Leucettamols, bifunctionalized sphingoid-like compounds obtained from a marine sponge Leucetta sp., act as non-electrophilic activators of the TRPA1 channel and potent inhibitors of the icilin-mediated activation of the TRPM8 channel, while they are inactive on CB₁, CB₂ and TRPV1 receptors. Leucettamols represent the first compounds of marine origin to target TRPA1 and the first class of natural products to inhibit TRPM8 channels. The preparation of a small series of semi-synthetic derivatives revealed interesting details on the structure-activity relationships within this new chemotype of simple acyclic TRP modulators.