Tear gasses CN, CR, and CS are potent activators of the human TRPA1 receptor

被引：78

作者：

Brone, Bert ^{[1
]}

Peeters, Pieter J. ^{[1
]}

Marrannes, Roger ^{[1
]}

Mercken, Marc ^{[1
]}

Nuydens, Ronny ^{[1
]}

Meert, Theo ^{[1
]}

Gijsen, Harrie J. M. ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev, Dept Neurosci, Div Janssen Pharmaceut NV, B-2340 Beerse, Belgium

来源：

TOXICOLOGY AND APPLIED PHARMACOLOGY | 2008年 / 231卷 / 02期

关键词：

TRPA1; agonist; ion-channel; patch clamp; tear gas; blepharospasm;

D O I：

10.1016/j.taap.2008.04.005

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The TRPA1 channel is activated by a number of pungent chemicals, such as allylisothiocyanate, present in mustard oil and thiosulfinates present in garlic. Most of the known activating compounds contain reactive, electrophilic chemical groups, reacting with cysteine residues in the active site of the TRPA1 channel. This covalent modification results in activation of the channel and has been shown to be reversible for several ligands. Commonly used tear gasses CN, CR and CS are also pungent chemicals, and in this study we show that they are extremely potent and selective activators of the human TRPA1 receptor. To our knowledge, these are the most potent TRPA1 agonists known to date. The identification of the molecular target for these tear gasses may open up possibilities to alleviate the effects of tear gasses via treatment with TRPA1 antagonists. In addition these results may contribute to the basic knowledge of the TRPA1 channel that is gaining importance as a pharmacological target. (C) 2008 Elsevier Inc. All rights reserved.

引用

页码：150 / 156

页数：7

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