Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds
2012
Ortar, Giorgio | Morera, Ludovica | Schiano Moriello, Aniello | Morera, Enrico | Nalli, Marianna | Di Marzo, Vincenzo | De Petrocellis, Luciano
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 EC₅₀ and/or IC₅₀ 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.
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