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新型血栓素A2受体拮抗剂KW-3635对豚鼠动脉血栓形成的抑制作用

Inhibitory effect of KW-3635, a new thromboxane A2-receptor antagonist, on arterial thrombosis in guinea pigs.

作者信息

Higo K, Karasawa A

机构信息

Department of Pharmacology, Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Shizuoka, Japan.

出版信息

Jpn J Pharmacol. 1993 Dec;63(4):521-3. doi: 10.1254/jjp.63.521.

DOI:10.1254/jjp.63.521
PMID:8121085
Abstract

The antithrombotic effects of the thromboxane (TX) A2-receptor antagonist and aspirin were determined using a photochemically-induced arterial thrombosis model in the femoral arteries of guinea pigs. KW-3635 (sodium (E)-11-[2-(5,6-dimethyl-1-benzimidazolyl)ethylidene]-6,11- dihydrodibenz[b,e]-oxepine-2-carboxylate monohydrate) and BM-13505, both of which are TXA2-receptor antagonists, and aspirin inhibited the thrombus formation at the doses that inhibited the ex vivo platelet aggregation induced by sodium arachidonate (100 microM) or collagen (3 micrograms/ml). These results support the notion that TXA2 is an important mediator in the present model of arterial thrombogenesis.

摘要

利用光化学诱导的豚鼠股动脉血栓形成模型,测定了血栓素(TX)A2受体拮抗剂和阿司匹林的抗血栓作用。KW-3635((E)-11-[2-(5,6-二甲基-1-苯并咪唑基)亚乙基]-6,11-二氢二苯并[b,e] -氧杂环庚英-2-羧酸钠一水合物)和BM-13505这两种TXA2受体拮抗剂,以及阿司匹林,在抑制花生四烯酸钠(100 microM)或胶原(3微克/毫升)诱导的体外血小板聚集的剂量下,均能抑制血栓形成。这些结果支持了TXA2在目前的动脉血栓形成模型中是重要介质这一观点。

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