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Mar. Drugs 2012, 10(11), 2435-2447; doi:10.3390/md10112435

Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels

1,†, 1,2
Received: 30 August 2012 / Revised: 15 October 2012 / Accepted: 18 October 2012 / Published: 2 November 2012
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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.
Keywords: leucettamols; TRP receptors; pain modulation leucettamols; TRP receptors; pain modulation
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Chianese, G.; Fattorusso, E.; Putra, M.Y.; Calcinai, B.; Bavestrello, G.; Moriello, A.S.; Petrocellis, L.D.; Marzo, V.D.; Taglialatela-Scafati, O. Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels. Mar. Drugs 2012, 10, 2435-2447.

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