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来自动情间期和产后豚鼠的子宫肌层环形和纵形肌膜以及肺膜中的β-肾上腺素能受体。

Beta-adrenoceptors in circular and longitudinal myometrial membranes and in lung membranes from dioestrous and post-partum guinea-pigs.

作者信息

Handberg G M, Davis E A, Hall S, Molenaar P, Summers R J, Pennefather J N

机构信息

Department of Pharmacology, Monash University, Clayton, Victoria, Australia.

出版信息

Clin Exp Pharmacol Physiol. 1988 Sep;15(9):681-93. doi: 10.1111/j.1440-1681.1988.tb01128.x.

DOI:10.1111/j.1440-1681.1988.tb01128.x
PMID:2856065
Abstract
  1. We have examined the binding of (-)[125]-cyanopindolol ((-)[125I]-CYP) to membranes prepared from uterus and lung of dioestrous and post-partum (1-6 days) guinea-pigs. 2. The densities of beta-adrenoceptor binding sites in circular and longitudinal myometrium from dioestrous animals were similar, and approximately one-eight of those in the lung. Ascorbate and ethylenediaminetetraacetic acid in the incubation medium did not affect binding. 3. The numbers and affinities of beta-adrenoceptor binding sites in both myometrial layers and in lung parenchyma from post-partum animals were similar to those in corresponding tissues from dioestrous animals. 4. The distribution of beta-adrenoceptor binding sites in the post-partum uterus was examined using receptor autoradiography. Binding to circular and longitudinal muscle layers and to the endometrium was inhibited by (-)-propranolol (1 mumol/l), by the beta 2-adrenoceptor selective antagonist ICI 118,551 (70 nmol/l), but not by the beta 1-adrenoceptor selective antagonist CGP 20712A (100 nmol/l), indicating that the beta-adrenoceptor present was of the beta 2-subtype. 5. The ability of isoprenaline to compete for (--)[125]-CYP binding sites in uterine membranes from post-partum animals was approximately twice that in corresponding preparations from dioestrous animals. 6. Changes in the numbers or affinity of beta 2-adrenoceptors cannot account for the marked and selective enhancement of the actions of sympathomimetic amines at beta-adrenoceptors previously observed in longitudinal myometrium taken from post-partum guinea-pigs. It is suggested that enhancement of later steps in the chain of events between beta-adrenoceptor occupancy and uterine relaxation, and/or a decrease in the contribution of alpha-adrenoceptors to the net effect of the amine might provide alternative explanations.
摘要
  1. 我们研究了(-)-[125I]-氰基吲哚洛尔((-)-[125I]-CYP)与动情间期和产后(1 - 6天)豚鼠子宫及肺制备的膜的结合情况。2. 动情期动物环形和纵形子宫肌层中β-肾上腺素能受体结合位点的密度相似,约为肺中结合位点密度的八分之一。孵育培养基中的抗坏血酸和乙二胺四乙酸不影响结合。3. 产后动物子宫肌层和肺实质中β-肾上腺素能受体结合位点的数量和亲和力与动情间期动物相应组织中的相似。4. 采用受体放射自显影法研究了产后子宫中β-肾上腺素能受体结合位点的分布。(-)-普萘洛尔(1 μmol/L)、β2-肾上腺素能受体选择性拮抗剂ICI 118,551(70 nmol/L)可抑制其与环形和纵形肌层以及子宫内膜的结合,但β1-肾上腺素能受体选择性拮抗剂CGP 20712A(100 nmol/L)则无此作用,表明存在的β-肾上腺素能受体为β2亚型。5. 异丙肾上腺素竞争产后动物子宫膜中(-)-[125I]-CYP结合位点的能力约为动情期动物相应制剂中的两倍。6. β2-肾上腺素能受体数量或亲和力的变化不能解释先前在产后豚鼠纵形子宫肌层中观察到的拟交感胺对β-肾上腺素能受体作用的显著和选择性增强。提示β-肾上腺素能受体占据与子宫舒张之间事件链中后续步骤的增强和/或α-肾上腺素能受体对胺类净效应贡献的降低可能提供了其他解释。

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