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Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds. 2012
Giorgio Ortar, and
Ludovica Morera, and
Aniello Schiano Moriello, and
Enrico Morera, and
Marianna Nalli, and
Vincenzo Di Marzo, and
Luciano De Petrocellis
Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Roma, Italy. giorgio.ortar@uniroma1.it
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.
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