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首页> 外文期刊>Life sciences >Inhibition by capsaicin and its related vanilloids of compound action potentials in frog sciatic nerves
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Inhibition by capsaicin and its related vanilloids of compound action potentials in frog sciatic nerves

机译：辣椒素抑制及其在青蛙坐骨神经中的复合作用潜力的相关香草

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Aims Although capsaicin not only activates transient receptor potential vanilloid-1 (TRPV1) channels but also inhibits nerve conduction, the latter action has not yet been fully examined. The purpose of the present study was to know whether various vanilloids have an inhibitory action similar to that of capsaicin and further to compare their actions with that of local anesthetic procaine. Main methods Fast-conducting compound action potentials (CAPs) were recorded from frog sciatic nerve fibers by using the air-gap method. Key findings Capsaicin reversibly and concentration-dependently reduced the peak amplitude of the CAP. TRPV1 antagonist capsazepine did not affect the capsaicin activity, and powerful TRPV1 agonist resiniferatoxin had no effect on CAPs, indicating no involvement of TRPV1 channels. Capsaicin analogs and other various vanilloids also inhibited CAPs in a concentration-dependent manner. An efficacy sequence of these inhibitions was capsaicin = dihydrocapsaicin > capsiate > eugenol > guaiacol ?? zingerone ?? vanillin > vanillylamine. Vanillic acid had almost no effect on CAPs; olvanil and curcumin appeared to be effective less than capsaicin. Capsaicin and eugenol were, respectively, ten- and two-fold effective more than procaine in CAP inhibition, while each of guaiacol, zingerone and vanillin was five-fold effective less than procaine. Significance Various vanilloids exhibit CAP inhibition, the extent of which is determined by the property of the side chain bound to the vanillyl group, and some of them are more effective than procaine. These results may serve to unveil molecular mechanisms for capsaicin-induced conduction block and to develop antinociceptive drugs related to capsaicin. ? 2013 Elsevier Inc. All rights reserved.
机译：目的虽然辣椒素不仅激活瞬态受体潜在的香草1（TRPV1）通道，但也抑制神经传导，但后一种作用尚未完全检查。本研究的目的是知道各种香草醛是否具有与辣椒素的抑制作用相似，并进一步与局部麻醉促进的动作进行比较。主要方法通过使用空气间隙方法从青蛙坐骨神经纤维记录快速导电的复合作用电位（盖子）。键调查胶囊可逆且浓度依赖性降低盖帽的峰值幅度。 TRPV1拮抗剂辣椒囊肿不影响辣椒素活性，强大的TRPV1激动剂树脂植物毒素对盖帽没有影响，表明TRPV1通道没有参与。辣椒素类似物和其他各种香草素也以浓度依赖性的方式抑制盖帽。这些抑制的功效序列是辣椒素=二氢胶囊>胶囊>丁香酚>愈蛋白醇？ Zingerone ??香草蛋白> vanillylamine。香草酸几乎没有对帽的影响;奥万维和姜黄素似乎有效地低于辣椒素。辣椒素和丁香醇分别比普通帽抑制作用的促进剂，两倍，而愈缩芽孢酚，姜酮和香草醛的每种比普华氏菌有5倍。意义各种香草素表现出帽抑制，其程度由与vanilyl组结合的侧链的性质确定，其中一些比普鲁卡因更有效。这些结果可用于揭示辣椒素诱导的传导嵌段的分子机制，并利用与辣椒素相关的抗肤质药物。还是2013年elsevier Inc.保留所有权利。

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