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雌激素或孕激素主导的大鼠子宫中β1和β2受体刺激作用的比较

Comparison of beta 1- and beta 2-receptor stimulation in oestrogen or progesterone dominated rat uterus.

作者信息

Johansson S R, Andersson R G, Wikberg J E

出版信息

Acta Pharmacol Toxicol (Copenh). 1980 Oct;47(4):252-8.

PMID:6258384
Abstract

Electrical stimulation of rat uterine preparations induced constant and reproducible contractions. The inhibitory effect of some adrenergic substances was tested on oestrogen- or progesterone-primed electrically stimulated rat uteri. The rank order of the relative potencies of some adrenergic agonists was shifted from Iso greater than E greater than Salb greater than Ne greater than H 133/22 greater than Phe greater than Clo in the oestrogen primed uterus to Iso greater than Salb greater than E greater than Ne greater than Phe greater than Clo greater than H 133/22 in progesterone primed uterus. The selective beta 2- agonist salbutamol was relatively more potent in progesterone treated rats than in oestrogen treated, while the beta 1-agonist H 133/22 was more potent in oestrogen dominated uterus. We therefore suggested that beta 2-receptors is dominating in the progesterone primed uterus, while both beta 1 and beta 2-receptors could be found in oestrogen primed uterus. No dissociation between the inhibitory effect on contractility and the cAMP increasing effect of isoprenaline could be demonstrated in rat uteri.

摘要

对大鼠子宫标本进行电刺激可诱发持续且可重复的收缩。在雌激素或孕激素预处理的电刺激大鼠子宫上测试了一些肾上腺素能物质的抑制作用。在雌激素预处理的子宫中,一些肾上腺素能激动剂的相对效价顺序为异肾上腺素>肾上腺素>沙丁胺醇>去甲肾上腺素>H 133/22>苯肾上腺素>氯压定;在孕激素预处理的子宫中则为异肾上腺素>沙丁胺醇>肾上腺素>去甲肾上腺素>苯肾上腺素>氯压定>H 133/22。选择性β2激动剂沙丁胺醇在孕激素处理的大鼠中比在雌激素处理的大鼠中相对更有效,而β1激动剂H 133/22在雌激素占主导的子宫中更有效。因此我们认为,β2受体在孕激素预处理的子宫中占主导,而在雌激素预处理的子宫中可同时发现β1和β2受体。在大鼠子宫中未发现异丙肾上腺素对收缩力的抑制作用与环磷酸腺苷(cAMP)增加作用之间存在解离现象。

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