title: Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds.
abstract: A series of thirty-three thymol, p-cymene-3-carboxylic acid, and 3-amino-p-cymene derivatives was synthesized and tested on TRPA1, TRPM8, and TRPV3 channels. Most of them acted as strong modulators of TRPA1, TRPM8, and TRPV3 channels with EC(50) and/or IC(50) values distinctly lower than those of thymol and related monoterpenoids. Some of the compounds examined, that is, 3c, 4e, f, 6b, and 8b exhibited an appreciable subtype-selectivity.
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Roma, Italy. giorgio.ortar@uniroma1.it
authors.forename: Giorgio
authors.initials: G
authors.lastname: Ortar
authors.forename: Ludovica
authors.initials: L
authors.lastname: Morera
authors.forename: Aniello Schiano
authors.initials: AS
authors.lastname: Moriello
authors.forename: Enrico
authors.initials: E
authors.lastname: Morera
authors.forename: Marianna
authors.initials: M
authors.lastname: Nalli
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Di Marzo
authors.forename: Luciano
authors.initials: L
authors.lastname: De Petrocellis
mesh_terms: D000818:Animals; D002460:Cell Line; D006801:Humans; D051381:Rats; D013943:Thymol / Q000737:chemistry / Q000494:pharmacology*; D050051:Transient Receptor Potential Channels / Q000187:drug effects*
chemical_list: D050051:Transient Receptor Potential Channels; D013943:Thymol