Drozd N N, Makarov V A, Miftakhova N T, Kalugin S A, Stroeva O G, Akberova S I
Laboratory of Hemostasis Pathology and Pharmacology, Russian Academy of Medical Sciences, Moscow, Russia.
Eksp Klin Farmakol. 2000 May-Jun;63(3):40-4.
Mechanisms of the anticoagulant activity of p-aminobenzoic acid (PABA) were studied. The specific antithrombin activity of PABA is aIIa = 7.00 +/- 0.32 IU/mg and the specific antiactivated factor Xa activity is aXa = 6.70 +/- 0.12 IU/mg. Study of the antithrombotic activity of PABA in rats with a model of venous stasis showed that intravenous injection of PABA at a dose of 1.5 mg/kg prevented the experimental thrombosis development 1.5 h after injection. The activity exhibited a peak 3 h after drug injection and ceased by the 5th hour. Equal antithrombotic activity in the rat blood plasma was observed for fraxiparin at a dose of 40 aXa IU/kg and PABA at 25 aXa IE/kg (1.5 mg/kg). At the same time, PABA affected neither the number of thrombocytes nor their response to the thrombocyte aggregation factors (ADP or adrenaline).
对对氨基苯甲酸(PABA)抗凝活性的机制进行了研究。PABA的特异性抗凝血酶活性为抗凝血酶IIa = 7.00±0.32 IU/mg,特异性抗活化因子Xa活性为抗活化因子Xa = 6.70±0.12 IU/mg。在静脉淤滞模型大鼠中对PABA的抗血栓形成活性进行研究,结果表明,以1.5 mg/kg的剂量静脉注射PABA可在注射后1.5小时预防实验性血栓形成。该活性在药物注射后3小时达到峰值,并在第5小时消失。观察到,对于剂量为40抗活化因子Xa IU/kg的达肝素和剂量为25抗活化因子Xa IE/kg(1.5 mg/kg)的PABA,大鼠血浆中的抗血栓形成活性相同。同时,PABA既不影响血小板数量,也不影响其对血小板聚集因子(ADP或肾上腺素)的反应。