Klysner R, Andersen P H, Geisler A, Winther K
Acta Pharmacol Toxicol (Copenh). 1984 Apr;54(4):265-9. doi: 10.1111/j.1600-0773.1984.tb01928.x.
The human platelet beta-adrenergic receptor was characterized by using the ability of different drugs to stimulate the adenylate cyclase activity and the effects of various beta-antagonists to block the isoprenaline-stimulated adenylate cyclase activity. Isoprenaline was found 10 times more potent than adrenaline and 1000 times more potent than noradrenaline in stimulating the adenylate cyclase activity in these cells. Isoprenaline-stimulated activity was blocked by the non-selective beta-antagonists propranolol and alprenolol and by the beta 2-selective antagonist IPS 339 and prenalterol. Metoprolol, a beta 1-selective blocker, was without effect on the isoprenaline-stimulated adenylate cyclase activity. We conclude from our findings that the beta-adrenergic receptor type on the human platelet is mainly of the beta 2-subtype.
通过利用不同药物刺激腺苷酸环化酶活性的能力以及各种β拮抗剂阻断异丙肾上腺素刺激的腺苷酸环化酶活性的作用,对人血小板β肾上腺素能受体进行了表征。发现在刺激这些细胞中的腺苷酸环化酶活性方面,异丙肾上腺素的效力比肾上腺素高10倍,比去甲肾上腺素高1000倍。异丙肾上腺素刺激的活性被非选择性β拮抗剂普萘洛尔和阿普洛尔以及β2选择性拮抗剂IPS 339和普瑞特罗阻断。β1选择性阻滞剂美托洛尔对异丙肾上腺素刺激的腺苷酸环化酶活性没有影响。我们从研究结果得出结论,人血小板上的β肾上腺素能受体类型主要是β2亚型。