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Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels
Department of Natural Compounds Chemistry, University of Naples Federico II, Via Montesano 49, 80131 Napoli, Italy
Department of Marine Science, Polytechnic University of Marche, Via Brecce Bianche, 60131 Ancona, Italy
Department for the Study of the Territory and its Resources, University of Genoa, Corso Europa 26, 16132, Genova, Italy
Endocannabinoid Research Group, Istituto di Cibernetica-CNR, Via Campi Flegrei 34, 80078 Pozzuoli (Naples), Italy
Endocannabinoid Research Group, Istituto di Chimica Biomolecolare-CNR, Via Campi Flegrei 34, 80078 Pozzuoli (Naples), Italy
Deceased on 7 July 2012.
* Author to whom correspondence should be addressed.
Received: 30 August 2012; in revised form: 15 October 2012 / Accepted: 18 October 2012 / Published: 2 November 2012
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.
Keywords: 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.
Chianese G, Fattorusso E, Putra MY, Calcinai B, Bavestrello G, Moriello AS, Petrocellis LD, Marzo VD, Taglialatela-Scafati O. Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels. Marine Drugs. 2012; 10(11):2435-2447.
Chianese, Giuseppina; Fattorusso, Ernesto; Putra, Masteria Y.; Calcinai, Barbara; Bavestrello, Giorgio; Moriello, Aniello S.; Petrocellis, Luciano D.; Marzo, Vincenzo D.; Taglialatela-Scafati, Orazio. 2012. "Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels." Mar. Drugs 10, no. 11: 2435-2447.