基于百里香酚的化合物对热瞬态受体电位（thermo-TRP）通道的调制。

Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds.

机构信息

Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Roma, Italy.

出版信息

Bioorg Med Chem Lett. 2012 May 15;22(10):3535-9. doi: 10.1016/j.bmcl.2012.03.055. Epub 2012 Mar 20.

DOI:10.1016/j.bmcl.2012.03.055

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.

摘要

合成了一系列 33 种麝香草酚、对伞花烃-3-羧酸和 3-氨基对伞花烃衍生物，并对它们在 TRPA1、TRPM8 和 TRPV3 通道上的作用进行了测试。其中大多数化合物都能强烈调节 TRPA1、TRPM8 和 TRPV3 通道，其 EC50 和/或 IC50 值明显低于麝香草酚和相关单萜类化合物。在所研究的一些化合物中，即 3c、4e、f、6b 和 8b，表现出相当的亚型选择性。