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血小板肾上腺素能受体:咪唑啉药物的聚集和抗聚集活性

Blood platelet adrenoceptor: aggregatory and antiaggregatory activity of imidazoline drugs.

作者信息

Petrusewicz J, Kaliszan R

出版信息

Pharmacology. 1986;33(5):249-55. doi: 10.1159/000138223.

Abstract

The effects of seven commonly used imidazoline drugs on human blood platelet aggregation and their inhibitory activity against the adrenaline-induced process were studied. The alpha-adrenoceptor reacting drugs, prazosin and yohimbine, were used as the standards. Low agonistic properties were found in the case of antazoline, clonidine and tetryzoline, whereas those three drugs along with naphazoline, phentolamine, tolazoline and xylometazoline exhibited marked antagonistic activity against the adrenaline-induced aggregation. The results are discussed from the point of view of the existing classification of the alpha-receptors. The conclusion is that the human blood platelet alpha-adrenoceptors, although resembling the properties of the alpha 2-subtype, form either a separate subclass of the receptors or a heterogeneous population of the alpha 2-subtype and an adrenergic receptor different from both alpha 1- and alpha 2-subclasses.

摘要

研究了七种常用咪唑啉药物对人血小板聚集的影响及其对肾上腺素诱导过程的抑制活性。以α-肾上腺素受体反应药物哌唑嗪和育亨宾作为标准。发现安他唑啉、可乐定和丁苄唑啉具有低激动特性,而这三种药物与萘甲唑啉、酚妥拉明、妥拉唑啉和赛洛唑啉一起对肾上腺素诱导的聚集表现出明显的拮抗活性。从现有的α-受体分类角度对结果进行了讨论。结论是,人血小板α-肾上腺素受体虽然类似于α2亚型的特性,但要么构成受体的一个单独亚类,要么构成α2亚型的异质群体以及一种不同于α1和α2亚类的肾上腺素能受体。

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