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人血小板上β-肾上腺素能受体的特性:一种β2亚型。

Characterization of the beta-adrenergic receptor on the human platelet: a beta 2-subtype.

作者信息

Klysner R, Andersen P H, Geisler A, Winther K

出版信息

Acta Pharmacol Toxicol (Copenh). 1984 Apr;54(4):265-9. doi: 10.1111/j.1600-0773.1984.tb01928.x.

DOI:10.1111/j.1600-0773.1984.tb01928.x
PMID:6145292
Abstract

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.

摘要

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。

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1
Characterization of the beta-adrenergic receptor on the human platelet: a beta 2-subtype.人血小板上β-肾上腺素能受体的特性:一种β2亚型。
Acta Pharmacol Toxicol (Copenh). 1984 Apr;54(4):265-9. doi: 10.1111/j.1600-0773.1984.tb01928.x.
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Lack of influence of short-term treatment with propranolol and terbutaline on metabolism and energy expenditure of the Na-K pump in human erythrocytes evaluated by microcalorimetry.通过微量量热法评估,普萘洛尔和特布他林短期治疗对人红细胞中钠钾泵代谢和能量消耗无影响。
Eur J Clin Pharmacol. 1993;45(6):571-6. doi: 10.1007/BF00315317.
2
Effect of metoprolol and propranolol on platelet aggregation and cAMP level in hypertensive patients.美托洛尔和普萘洛尔对高血压患者血小板聚集及环磷酸腺苷水平的影响。
Eur J Clin Pharmacol. 1986;29(5):561-4. doi: 10.1007/BF00635893.