Krupiński K, Ferber H, Breddin H K, Bielawiec M
Klinika Hematologii Akademii Medycznej w Białymstoku.
Acta Haematol Pol. 1994;25(3):235-42.
The effect of thromboxane receptor antagonist HN 11500 (Chemie Linz AG, Austria) on thrombus formation in laser thrombosis model and platelet function test has been studied. In this study HN 11500 was a potent antithrombotic agent significantly inhibiting thrombus formation in venules in doses higher than 5 mg/kg after i.v. and 10 mg/kg after oral administration. Lower doses were needed to obtain the same antithrombotic effect when arterioles were investigated. The antithrombotic effect of minimal effective doses of HN 11500 lasted longer than 8 hours in venules and more than 12 hours in arterioles. After oral feeding of this thromboxane receptor antagonist in doses 5 mg/kg, antithrombotic effect in investigated arterioles lasted longer than 16 hours but less than 20 hours. When different doses of HN 11500 were injected i.v. together with r-Hirudin or LMWH CY 216 the inhibitory effect on thrombus formation in venules was stronger and observed with lower doses of HN 11500. In vitro study HN 11500 inhibited platelet adhesion to the siliconized glass, bovine extracellular matrix as well as ADP and collagen mediated platelet aggregation. Lower concentration of this agent were needed to inhibited platelet adhesion to the extracellular matrix than platelet adhesion to the siliconised glass, and ADP and collagen induced aggregation.
研究了血栓素受体拮抗剂HN 11500(奥地利林茨化学公司)对激光血栓形成模型中血栓形成及血小板功能测试的影响。在本研究中,HN 11500是一种强效抗血栓药物,静脉注射后剂量高于5mg/kg以及口服给药后剂量高于10mg/kg时,可显著抑制小静脉中的血栓形成。在研究小动脉时,需要较低剂量就能获得相同的抗血栓效果。HN 11500最小有效剂量的抗血栓作用在小静脉中持续超过8小时,在小动脉中持续超过12小时。以5mg/kg的剂量口服这种血栓素受体拮抗剂后,在所研究的小动脉中的抗血栓作用持续超过16小时但少于20小时。当将不同剂量的HN 11500与重组水蛭素或低分子肝素CY 216一起静脉注射时,对小静脉中血栓形成的抑制作用更强,且在较低剂量的HN 11500时即可观察到。体外研究中,HN 11500抑制血小板黏附于硅化玻璃、牛细胞外基质以及ADP和胶原介导的血小板聚集。抑制血小板黏附于细胞外基质所需的该药物浓度低于抑制血小板黏附于硅化玻璃以及ADP和胶原诱导的聚集所需的浓度。