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Updated: May 16, 2026

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
Published on: December 31, 2013
Leucettamols, bifunctionalized marine sphingoids, act as modulators of TRPA1 and TRPM8 channels
Giuseppina Chianese1, Ernesto Fattorusso, Masteria Yunovilsa Putra
1Department of Natural Compounds Chemistry, University of Naples Federico II, Via Montesano 49, 80131 Napoli, Italy.
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.
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