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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：辣椒素及其相关香草素对青蛙坐骨神经复合动作电位的抑制作用

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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：目的尽管辣椒素不仅激活瞬态受体电位香草酸1（TRPV1）通道，而且还抑制神经传导，但后者的作用尚未得到充分研究。本研究的目的是了解各种类香草素是否具有与辣椒素相似的抑制作用，并进一步将其与局部麻醉性普鲁卡因的作用进行比较。主要方法采用气隙法从青蛙坐骨神经纤维中记录快速传导复合动作电位（CAPs）。主要发现辣椒素可逆地和浓度依赖性地降低了CAP的峰值幅度。 TRPV1拮抗剂辣椒碱没有影响辣椒素的活性，强大的TRPV1激动剂resiniferatoxin对CAP没有影响，表明没有TRPV1通道参与。辣椒素类似物和其他各种类香草素也以浓度依赖性方式抑制CAP。这些抑制作用的效力顺序为辣椒素=二氢辣椒素>辣椒素>丁子香酚>愈创木酚??姜油酮香兰素>香兰素胺。香草酸对CAP几乎没有影响; olvanil和姜黄素似乎比辣椒素有效。辣椒素和丁子香酚的CAP抑制作用分别比普鲁卡因高十倍和两倍，而愈创木酚，姜油酮和香兰素的功效比普鲁卡因低五倍。重要性各种类香草素均显示出CAP抑制作用，其程度取决于与香草基结合的侧链的性质，其中一些比普鲁卡因更有效。这些结果可能有助于揭示辣椒素诱导的传导阻滞的分子机制，并开发与辣椒素有关的镇痛药。 ？ 2013 Elsevier Inc.保留所有权利。

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