Giedrojc J, Fellier H, Breddin H K
Department of Internal Medicine, J.W. Goethe University, Frankfurt am Main, FRG.
Haemostasis. 1992;22(6):322-9. doi: 10.1159/000216342.
The antithrombotic effect of a thromboxane A2 receptor antagonist (HN-11501:5-[2-(4-chlorophenylsulfonylamino)-ethyl]-2-thienylox y-acetic acid) alone and in combination with other antithrombotic agents has been studied in an experimental thrombosis model in which laser lesions are used to induce a defined thrombosis in rat mesenteric venules. The thromboxane receptor antagonist showed a significant and dose-dependent antithrombotic effect if given orally. The strongest additive thrombosis-inhibiting effect was observed after oral administration of HN-11501 at a dose of 2.5 mg/kg together with an intravenous infusion of 1 microgram/kg/h of a prostacyclin analogue (cicaprost). An additive antithrombotic effect was also observed after oral application of 2.5 mg/kg of HN-11501 and intravenous injection of 0.2 mg/kg of a low molecular weight heparin (Fraxiparine). The combination of 2.5 mg/kg of HN-11501 orally with an intravenous injection of 0.1 mg/kg molsidomine also had a significant additive effect. No significant additive effect was observed when 2.5 mg/kg of HN-11501 and 10 mg/kg of acetylsalicylic acid were orally administered simultaneously.
在一个实验性血栓形成模型中，研究了血栓素A2受体拮抗剂（HN-11501：5-[2-(4-氯苯基磺酰氨基)-乙基]-2-噻吩氧基乙酸）单独以及与其他抗血栓药物联合使用时的抗血栓作用。该模型利用激光损伤在大鼠肠系膜小静脉中诱导特定的血栓形成。如果口服给予血栓素受体拮抗剂，可显示出显著的剂量依赖性抗血栓作用。口服2.5mg/kg的HN-11501并静脉输注1μg/kg/h的前列环素类似物（西卡前列素）后，观察到最强的相加性血栓形成抑制作用。口服2.5mg/kg的HN-11501并静脉注射0.2mg/kg的低分子量肝素（速避凝）后，也观察到相加性抗血栓作用。口服2.5mg/kg的HN-11501并静脉注射0.1mg/kg的吗多明的组合也有显著的相加作用。当同时口服2.5mg/kg的HN-11501和10mg/kg的乙酰水杨酸时，未观察到显著的相加作用。
