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雌激素和孕酮会改变兔血小板上α-肾上腺素能受体和5-羟色胺受体的结合特性。

Oestrogen and progesterone change the binding characteristics of alpha-adrenergic and serotonin receptors on rabbit platelets.

作者信息

Elliott J M, Peters J R, Grahame-Smith D G

出版信息

Eur J Pharmacol. 1980 Aug 22;66(1):21-30. doi: 10.1016/0014-2999(80)90291-5.

Abstract

The binding characteristics of the alpha-adrenergic and serotonin receptors on intact rabbit platelets were identified using [3H]-dihydroergocryptine and [3H]-5-hydroxytryptamine respectively. In untreated female rabbits a single slpha-adrenoceptor and two serotonin receptors were identified with ligand affinities similar to those in human platelets. The effects of oestrogen and/or progesterone on the alpha-adrenergic and serotonin receptors of rabbit platelets were studied. Oestrogen alone increased the capacity of serotonin receptors but reduced that of the alpha-adrenoceptor. Oestrogen plus progesterone reduced the capacity of both receptors and reduced the affinity of the alpha-adrenoceptor. The possible mechanisms of the steroid-induced changes and the implications of these with regard to the effects of the oral contraceptive pill are discussed.

摘要

分别使用[3H]-二氢麦角隐亭和[3H]-5-羟色胺来鉴定完整兔血小板上α-肾上腺素能受体和5-羟色胺受体的结合特性。在未经处理的雌性兔中,鉴定出单一的α-肾上腺素能受体和两种5-羟色胺受体,其配体亲和力与人血小板中的相似。研究了雌激素和/或孕酮对兔血小板α-肾上腺素能受体和5-羟色胺受体的影响。单独使用雌激素可增加5-羟色胺受体的容量,但降低α-肾上腺素能受体的容量。雌激素加孕酮可降低两种受体的容量,并降低α-肾上腺素能受体的亲和力。讨论了类固醇诱导变化的可能机制以及这些机制与口服避孕药作用的关系。

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