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前列环素类似物(依洛前列素)与血栓素拮抗剂(舒洛地尔)联合应用对豚鼠和大鼠的协同抗血小板及抗血栓形成作用

Synergistic antiplatelet and antithrombotic effects of a prostacyclin analogue (iloprost) combined with a thromboxane antagonist (sulotroban) in guinea pigs and rats.

作者信息

Witt W, Stürzebecher S, Müller B

机构信息

Research Laboratories of Schering AG, Berlin, FRG.

出版信息

Thromb Res. 1988 Sep 15;51(6):607-16. doi: 10.1016/0049-3848(88)90144-2.

DOI:10.1016/0049-3848(88)90144-2
PMID:2460967
Abstract

The stable PGI2-analogue iloprost and the TXA2-receptor antagonist sulotroban were investigated for possible cooperative effects on platelet function and experimental thrombus formation in guinea pigs and rats. Iloprost and sulotroban inhibit intravascular platelet aggregation in guinea pigs and rats induced by the stable endoperoxide U 46.619 and collagen, with iloprost being the more potent and (for collagen) more efficacious drug. Combinations of both compounds show synergistic or additive effects on in vivo platelet function. Thrombus formation in rats induced by vascular damage is strongly reduced by combining doses of iloprost and sulotroban (BM 13.177) which given alone are ineffective. These results suggest a cooperative enhancement of antiplatelet and antithrombotic effects for combinations of iloprost and sulotroban. In view of disadvantages of currently used platelet inhibitors this cooperativity may offer a new approach in antiplatelet therapy.

摘要

研究了稳定的前列环素类似物伊洛前列素和血栓素A2受体拮抗剂舒洛地班对豚鼠和大鼠血小板功能及实验性血栓形成的可能协同作用。伊洛前列素和舒洛地班可抑制豚鼠和大鼠体内由稳定内过氧化物U 46.619和胶原诱导的血管内血小板聚集,其中伊洛前列素作用更强,且(对于胶原)是更有效的药物。两种化合物的组合对体内血小板功能显示出协同或相加作用。单独使用无效的伊洛前列素和舒洛地班(BM 13.177)联合给药可显著减少大鼠血管损伤诱导的血栓形成。这些结果表明伊洛前列素和舒洛地班组合具有协同增强的抗血小板和抗血栓作用。鉴于目前使用的血小板抑制剂存在的缺点,这种协同作用可能为抗血小板治疗提供一种新方法。

相似文献

1
Synergistic antiplatelet and antithrombotic effects of a prostacyclin analogue (iloprost) combined with a thromboxane antagonist (sulotroban) in guinea pigs and rats.前列环素类似物(依洛前列素)与血栓素拮抗剂(舒洛地尔)联合应用对豚鼠和大鼠的协同抗血小板及抗血栓形成作用
Thromb Res. 1988 Sep 15;51(6):607-16. doi: 10.1016/0049-3848(88)90144-2.
2
The PGI2-analogue iloprost and the TXA2-receptor antagonist sulotroban synergistically inhibit TXA2-dependent platelet activation.前列环素类似物伊洛前列素和血栓素A2受体拮抗剂舒洛地班协同抑制血栓素A2依赖性血小板活化。
Prostaglandins. 1988 Dec;36(6):751-60. doi: 10.1016/0090-6980(88)90053-6.
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Protective effects of the novel thromboxane A2 receptor antagonist sodium (E)-11-[2-(5,6-dimethyl-1-benzimidazolyl)-ethylidene]-6,11- dihydrodibenz[b,e]oxepine-2-carboxylate monohydrate against 9,11-dideoxy- 9 alpha, 11 alpha-epoxymethano-prostaglandin F2 alpha-induced sudden death in guinea-pigs and rats.新型血栓素A2受体拮抗剂(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]氧杂环庚三烯-2-羧酸钠一水合物对9,11-二脱氧-9α,11α-环氧甲撑前列腺素F2α诱导的豚鼠和大鼠猝死的保护作用
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The pharmacological profile of the thromboxane A2 antagonist BM 13.177. A new anti-platelet and anti-thrombotic drug.血栓素A2拮抗剂BM 13.177的药理学特性。一种新型抗血小板和抗血栓药物。
Thromb Res. 1984 Aug 15;35(4):379-95. doi: 10.1016/0049-3848(84)90230-5.
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The effect of substances influencing the arachidonic acid cascade on experimental cardiac arrhythmias.影响花生四烯酸级联反应的物质对实验性心律失常的作用。
Biomed Biochim Acta. 1988;47(10-11):S27-30.
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Antiaggregant and antivasospastic properties of the new thromboxane A2 receptor antagonist sodium 4-[[1-[[[(4-chlorophenyl)sulfonyl]amino]methyl]cyclopentyl] methyl]benzeneacetate.新型血栓素A2受体拮抗剂4-[[1-[[[(4-氯苯基)磺酰基]氨基]甲基]环戊基]甲基]苯乙酸钠的抗聚集和抗血管痉挛特性
Arzneimittelforschung. 1994 Nov;44(11):1196-202.
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Actions of the novel thromboxane A2 receptor antagonist sodium (E)-11-[2-(5,6-dimethyl-1-benzimidazolyl)-ethylidene]-6,11- dihydrodibenz[b,e]oxepine-1-carboxylate monohydrate on smooth muscle preparations.新型血栓素A2受体拮抗剂(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]氧杂卓-1-羧酸酯钠一水合物对平滑肌制剂的作用
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[The modification of the biosynthesis and effect of thromboxane A2 and prostacyclin by trapidil (Rocornal)].曲匹地尔(心可定)对血栓素A2和前列环素生物合成及作用的影响
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Br J Pharmacol. 1991 Jan;102(1):260-6. doi: 10.1111/j.1476-5381.1991.tb12163.x.

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2
Iloprost. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in peripheral vascular disease, myocardial ischaemia and extracorporeal circulation procedures.伊洛前列素。对其药效学和药代动力学特性以及在周围血管疾病、心肌缺血和体外循环手术中的治疗潜力的综述。
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