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肾上腺素能受体拮抗剂对血小板聚集和血栓素生成影响的比较研究。

A comparative study of the effects of adrenoceptor antagonists on platelet aggregation and thromboxane generation.

作者信息

Greer I A, Walker J J, McLaren M, Calder A A, Forbes C D

出版信息

Thromb Haemost. 1985 Aug 30;54(2):480-4.

PMID:2867620
Abstract

Platelet aggregation and thromboxane A2 have been implicated in the pathogenesis of several forms of vascular disease. The aim of this study was to determine the effect of a wide range of adrenoceptor antagonists on platelet aggregation, and thromboxane A2 production, from normal human platelet rich plasma in vitro. Labetalol, pindolol and propranolol inhibited platelet aggregation to collagen in a dose dependent manner. Increasing the concentration of collagen "shifted" the dose response curve to the right. These 3 drugs also significantly inhibited thromboxane A2 generation in response to collagen but not to arachidonic acid. This effect was independent of any inhibitory effect of these drugs on platelet aggregation, and occurred at a drug concentration close to that obtained in vivo. Atenolol, metoprolol, prazosin and timolol were similarly assessed but had no effect on either platelet aggregation or thromboxane A2 generation. This ability of labetalol, pindolol, and propranolol to inhibit platelet aggregation and thromboxane generation, may be of clinical benefit in view of the increasing evidence implicating thromboxane A2 in the pathogenesis of vascular disease.

摘要

血小板聚集和血栓素A2与多种血管疾病的发病机制有关。本研究的目的是确定一系列肾上腺素能受体拮抗剂对正常人富含血小板血浆体外血小板聚集和血栓素A2生成的影响。拉贝洛尔、吲哚洛尔和普萘洛尔以剂量依赖方式抑制血小板对胶原的聚集。增加胶原浓度使剂量反应曲线“右移”。这三种药物也显著抑制胶原诱导的血栓素A2生成,但对花生四烯酸诱导的无此作用。这种作用独立于这些药物对血小板聚集的任何抑制作用,且发生在接近体内获得的药物浓度时。阿替洛尔、美托洛尔、哌唑嗪和噻吗洛尔经类似评估,但对血小板聚集或血栓素A2生成均无影响。鉴于越来越多的证据表明血栓素A2参与血管疾病的发病机制,拉贝洛尔、吲哚洛尔和普萘洛尔抑制血小板聚集和血栓素生成的这种能力可能具有临床益处。

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