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4-氨基-α-(叔丁氨基)甲基]-3,5-二氯苄醇盐酸盐(N-AB 365,克伦特罗)对呼吸系统的作用(作者译)

[Action of 4-amino-alpha-](tertbutylamino) methyl]-3, 5-dichlorobenzylalchol hydrochloride (N-AB 365, clenbuterol) on the respiratory system (author's transl)].

作者信息

Miyata T, Takahama K, Hasanat A, Ikegami K, Iwasaki K, Okano Y, Kasé Y

出版信息

Nihon Yakurigaku Zasshi. 1978 Jul;74(5):573-88.

PMID:700519
Abstract

The bronchodilating effect and other related pharmacological properties of N-AB 365 were studied in comparison with those of isoproterenol, salbutamol and clorprenaline. N-AB 365 was found to produce a bronchodilating effect 1/20 approximately 1/100, 1/10 approximately 1/40 and was 2 to 5 times as strong as effects of isoproterenol, salbutamol and clorprenaline, respectively. The bronchodilating effect of N-AB 365 was sustained more than 10 times as long as those of isoproterenol and salbutamol, and in particular with oral administration, was much more potent. The bronchodilating effect of N-AB 365 seems to be due mainly to excitation of the adrenergic beta2-receptor and partially to papaverine-like action. N-AB 365 showed an inhibitory effect on experimentally induced bronchial asthma by spraying of bronchoconstrictors and the effect by oral administration was much stronger than those of isoproterenol and salbutamol. N-AB 365 affected neither the volume output of respiratory tract fluid nor the tracheal ciliary movement with the doses around ED50 in bronchodilating action, however, it increased ciliary activity and decreased the volume output of respiratory tract fluid with large doses. Antitussive effect was also demonstrated only with the large doses. N-AB 365 induced a moderate decrease in blood pressure through vasodilatation but did not influence respiration. The effect of N-AB 365 on heart rate varied. There were cases of no change, slight increase or slight decrease in heart rate.

摘要

将N - AB 365的支气管扩张作用及其他相关药理特性与异丙肾上腺素、沙丁胺醇和氯丙那林进行了比较研究。发现N - AB 365产生的支气管扩张作用约为异丙肾上腺素的1/20至1/100、沙丁胺醇的1/10至1/40,其强度分别是异丙肾上腺素、沙丁胺醇和氯丙那林的2至5倍。N - AB 365的支气管扩张作用持续时间比异丙肾上腺素和沙丁胺醇长10倍以上,尤其是口服给药时,效力更强。N - AB 365的支气管扩张作用似乎主要归因于肾上腺素能β2受体的兴奋,部分归因于类似罂粟碱的作用。N - AB 365对通过喷洒支气管收缩剂诱发的实验性支气管哮喘有抑制作用,口服给药的效果比异丙肾上腺素和沙丁胺醇更强。在支气管扩张作用中,当剂量接近ED50时,N - AB 365对呼吸道液体的排出量和气管纤毛运动均无影响,然而,大剂量时它会增加纤毛活性并减少呼吸道液体的排出量。仅在大剂量时才显示出镇咳作用。N - AB 365通过血管舒张使血压适度下降,但不影响呼吸。N - AB 365对心率的影响各不相同。存在心率无变化、略有增加或略有下降的情况。

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