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TRPM8/TRPA1通道激动剂艾西利定(AG-3-5)的差异行为效应。

Differential behavioral effect of the TRPM8/TRPA1 channel agonist icilin (AG-3-5).

作者信息

Rawls Scott M, Gomez Teresa, Ding Zhe, Raffa Robert B

机构信息

Department of Pharmaceutical Sciences, Temple University School of Pharmacy, Philadelphia, PA 19140, USA.

出版信息

Eur J Pharmacol. 2007 Dec 1;575(1-3):103-4. doi: 10.1016/j.ejphar.2007.07.060. Epub 2007 Aug 3.

Abstract

Molecular identification of two new transient receptor potential (TRP) channels, TRPM8 and TRPA1, has prompted an intense interest in their functional roles. We report that an acute exposure to the TRPM8/TRPA1 agonist icilin (0.01-100 microM), but not TRPV1 agonist capsaicin (10 microM), causes an atypical dose-related increase in planarian motility. This is the first demonstration of a TRPM8/TRPA1 channel subtype agonist-induced differential pharmacological effect in invertebrates and provides a novel sensitive, quantifiable end-point for studying TRP channel pharmacology.

摘要

两种新的瞬时受体电位(TRP)通道TRPM8和TRPA1的分子鉴定引发了人们对其功能作用的浓厚兴趣。我们报告称,急性暴露于TRPM8/TRPA1激动剂冰片(0.01 - 100微摩尔),而非TRPV1激动剂辣椒素(10微摩尔),会导致涡虫运动出现非典型的剂量相关增加。这是首次在无脊椎动物中证明TRPM8/TRPA1通道亚型激动剂诱导的差异药理作用,并为研究TRP通道药理学提供了一种新颖、敏感且可量化的终点指标。

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