%0 Journal Article
%T Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels
%A Giuseppina Chianese
%A Ernesto Fattorusso
%A Masteria Yunovilsa Putra
%A Barbara Calcinai
%A Giorgio Bavestrello
%A Aniello Schiano Moriello
%A Luciano De Petrocellis
%A Vincenzo Di Marzo
%A Orazio Taglialatela-Scafati
%J Marine Drugs
%D 2012
%I MDPI AG
%R 10.3390/md10112435
%X 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 CB 1, CB 2 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.
%K leucettamols
%K TRP receptors
%K pain modulation
%U http://www.mdpi.com/1660-3397/10/11/2435