Smooth Muscle-Depressant Activity of AP-18, a Putative TRPA1 Antagonist in the Guinea Pig Intestine
Smooth Muscle-Depressant Activity of AP-18, a Putative TRPA1 Antagonist in the Guinea Pig Intestine
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DOI：
10.1159/000366023
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发表时间：
2014-01-01
期刊：
影响因子：
3.1
通讯作者：
Benko, Rita
中科院分区：
文献类型：
--
作者：
Bartho, Lorand;Sandor, Zsolt;Benko, Rita
AP-18是一种推测的TRPA1受体/离子通道拮抗剂，在10-100 μ mol/l时引起平滑肌松弛。抑制电场刺激胆碱能神经引起的胆碱能抽搐反应以及乙酰胆碱和组胺对豚鼠小肠的收缩反应。AP-18 （30 μ mol/l）阻断人空肠纵条自发收缩。因此，AP-18在研究trpa1介导的平滑肌反应方面可能价值有限，在其他制剂中可能存在非特异性作用，因此应谨慎使用。(C) 2014 S. Karger AG，巴塞尔
AP-18, a putative antagonist at TRPA1 receptor/ion channel, caused smooth muscle relaxation at 10-100 mu mol/l. It inhibited cholinergic twitch responses evoked by electrical field stimulation of cholinergic nerves as well as contractions in response to acetylcholine and histamine in the guinea pig small intestine. AP-18 (30 mu mol/l) blocked spontaneous contractions of longitudinal strips of human jejunum. It is concluded that AP-18 may have limited value in studying TRPA1-mediated responses in smooth muscles and should probably be used with care in other preparations because of possible nonspecific effects. (C) 2014 S. Karger AG, Basel