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多巴酚丁胺及几种儿茶酚胺对各种平滑肌的药理作用(作者译)

[Pharmacological effects of dobutamine and several catecholamines on various smooth muscles (author's transl)].

作者信息

Doteuchi M, Otani K, Hirose F, Sai M, Hirose A, Takeda H

出版信息

Nihon Yakurigaku Zasshi. 1979 Mar;75(2):159-70. doi: 10.1254/fpj.75.159.

Abstract

Pharmacological effects of dobutamine (DOB), a positive inotropic drug, on smooth muscles were compared with those of catecholamines such as norepinephrine (NE), epinephrine (E), isoproterenol (ISO) and dopamine (DA). DOB acted as a partial agonist and simultaneously as an antagonist on alpha-adrenergic receptors in the thoracic artery. Large doses of DOB induced uterine contraction in rabbits, but antagonised the contraction of the vas deferens of guinea pigs, as was induced by electrical stimulation. However, DOB showed a potent activity, similar to that seen with NE or E as an alpha-adrenergic agonist, on the portal vein. Doses of DOB required to produce a relaxation in the trachea of guinea pigs both in vitro and in vivo were 1/250 and 1/600 of ISO, respectively, and were considerably less regarding inhibition of uterine motility in rats. Inhibiting activity of DOB on the transport rate of intestinal contents in mice and gastro-intestinal motility of rabbits was much less than the activity seen with ISO, E and NE. Spasmolytic activity of DOB was also less than that of ISO, NE and E, but was more than that of DA. It is concluded that DOB is a more selective beta 1-agonist than ISO because of its weaker activity on alpha- and beta 2-receptors. The alpha-agonist activity of DOB in the portal vein was however, potent.

摘要

将强心药物多巴酚丁胺(DOB)对平滑肌的药理作用与去甲肾上腺素(NE)、肾上腺素(E)、异丙肾上腺素(ISO)和多巴胺(DA)等儿茶酚胺类药物的药理作用进行了比较。DOB在胸主动脉中对α-肾上腺素能受体起部分激动剂作用,同时起拮抗剂作用。大剂量的DOB可诱导兔子宫收缩,但能拮抗电刺激诱导的豚鼠输精管收缩。然而,DOB在门静脉上表现出与NE或E作为α-肾上腺素能激动剂时相似的强效活性。在体外和体内使豚鼠气管松弛所需的DOB剂量分别为ISO的1/250和1/600,在抑制大鼠子宫运动方面剂量则小得多。DOB对小鼠肠内容物运输速率和兔胃肠运动的抑制活性远低于ISO、E和NE。DOB的解痉活性也低于ISO、NE和E,但高于DA。得出的结论是,由于DOB对α-和β2-受体的活性较弱,它是一种比ISO更具选择性的β1-激动剂。然而,DOB在门静脉中的α-激动剂活性很强。

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