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苯达松对凝血、纤维蛋白溶解及血小板功能的体外作用

In vitro effects of bencyclan on coagulation, fibrinolysis and platelet function.

作者信息

Ponari O, Civardi E, Dettori G, Magha A, Potì R, Bulletti G

出版信息

Arzneimittelforschung. 1976;26(8):1532-8.

PMID:12770
Abstract

The in vitro effects of N-3-(1-benzyl-cycloheptyloxy)-propyl-N,N-dimethylammonium-hydrogenfumarate (bencyclan) on clotting, fibrinolytic and platelet function test were investigated by adding the drug to normal human plasma. An anticoagulant activity, mainly of an antithromboplastin nature (directed against later stages of intrinsic thromboplastin formation and against tissue thromboplastin), was observed, while thrombin phase was unaffected. No effect was found in the fibrinolytic system tested (euglobulin lysis, UK-activated fibrinolysis, "hanging clot" method). The drug, although capable of aggregating platelets by itself at very high concentrations, showed a striking inhibitory effect, over a wide range of concentrations, both on platelet aggregation induced by ADP, epinephrine or collagen and on platelet adhesiveness to glass or collagen. Clot retraction was also clearly inhibited. PF3 availability was influenced with a peculiar two-phase behaviour dose-dependently. High concentrations showed a promoting action, while the lower were obviously inhibitory. It is suggested that the effects on platelet function may be due to an influence of the drug on cell membrane.

摘要

通过将N-3-(1-苄基-环庚氧基)-丙基-N,N-二甲基铵氢富马酸盐(苄环烷)添加到正常人血浆中,研究了其对凝血、纤维蛋白溶解和血小板功能测试的体外作用。观察到一种抗凝活性,主要具有抗凝血活酶性质(针对内源性凝血活酶形成的后期阶段以及组织凝血活酶),而凝血酶阶段未受影响。在所测试的纤维蛋白溶解系统(优球蛋白溶解、尿激酶激活的纤维蛋白溶解、“悬凝块”法)中未发现作用。该药物虽然在非常高的浓度下自身能够使血小板聚集,但在很宽的浓度范围内,对由ADP、肾上腺素或胶原诱导的血小板聚集以及血小板与玻璃或胶原的黏附性均表现出显著的抑制作用。凝块回缩也明显受到抑制。PF3可用性受到剂量依赖性的特殊双相行为影响。高浓度表现出促进作用,而低浓度则明显具有抑制作用。提示对血小板功能的影响可能是由于该药物对细胞膜的作用。

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