title: Effect of acyclic monoterpene alcohols and their derivatives on TRP channels.
abstract: A series of thirty-six geraniol, nerol, citronellol, geranylamine, and nerylamine derivatives was synthesized and tested on TRPA1, TRPM8, and TRPV1 channels. Most of them acted as strong modulators of TRPA1 channels with EC50 and/or IC50 values <1 μM. None was able to significantly activate TRPM8 channels, while thirteen of them behaved as 'true' TRPM8 antagonists. Little or no effect was generally observed on TRPV1 channels. Some of the compounds examined, that is, compounds 1d,g,n, 2c,d,h,i,o, 3b,e exhibited an appreciable selectivity for TRPA1 subtype.
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy. Electronic address: giorgio.ortar@uniroma1.it.
authors.forename: Giorgio
authors.initials: G
authors.lastname: Ortar
authors.affiliation: Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, via dei Campi Flegrei 34, 80078 Pozzuoli (Napoli), Italy.
authors.forename: Aniello
authors.initials: A
authors.lastname: Schiano Moriello
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy.
authors.forename: Enrico
authors.initials: E
authors.lastname: Morera
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy.
authors.forename: Marianna
authors.initials: M
authors.lastname: Nalli
authors.affiliation: Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, via dei Campi Flegrei 34, 80078 Pozzuoli (Napoli), Italy.
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Di Marzo
authors.affiliation: Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, via dei Campi Flegrei 34, 80078 Pozzuoli (Napoli), Italy. Electronic address: l.depetrocellis@icb.cnr.it.
authors.forename: Luciano
authors.initials: L
authors.lastname: De Petrocellis
mesh_terms: D000438:Alcohols; D006801:Humans; D039821:Monoterpenes / Q000378:metabolism*; D050051:Transient Receptor Potential Channels / Q000037:antagonists & inhibitors*
chemical_list: D000438:Alcohols; D039821:Monoterpenes; D050051:Transient Receptor Potential Channels
keywords: Acyclic monoterpene alcohols; TRPA1; TRPM8; TRPV1; Transient receptor potential channels