Savchik E Iu, Kalinina T B, Drozd N N, Makarov V A, Zav'ialova E G, Lapsheva E N, Babiĭ A V, Mudrik N N, Pavlova G V, Golovin A V, Kopylov A M
Eksp Klin Farmakol. 2012;75(11):13-8.
DNA aptamer RA36 with a molecular weight of 10000 is direct-acting anticoagulant whose efficacy is lower than that of recombinant hirudin and unfractionated heparin (UFH) in blood clotting time (BCT), activated blood recalcification time (ABRT), recalcification time (RT), prothrombin time (PT), and activated partial thromboplastin time (APTT) tests. The anticoagulant effect of RA36 is comparable with that of UFH in the thrombin time (TT) test, but is lower than the effect of recombinant hirudin. Analysis of the blood and plasma anticoagulant activity during intravenous bolus administration of aptamer RA36 in rabbits and rats is based on the use ABRT (in blood case) and APTT/RT (in plasma case) tests. The range of doses for evaluation of pharmacodynamic parameters of RA36 during intravenous bolus administration in rabbits and rats is 3 - 34 mg/kg and 1 - 27 mg/kg, respectively. Accordingly, designed dose range for humans is 1 -29 mg/kg.
分子量为10000的DNA适配体RA36是一种直接作用的抗凝剂，在凝血时间（BCT）、活化血液复钙时间（ABRT）、复钙时间（RT）、凝血酶原时间（PT）和活化部分凝血活酶时间（APTT）测试中，其疗效低于重组水蛭素和普通肝素（UFH）。在凝血酶时间（TT）测试中，RA36的抗凝效果与UFH相当，但低于重组水蛭素。通过使用ABRT（针对血液）和APTT/RT（针对血浆）测试，对兔和大鼠静脉推注适配体RA36期间的血液和血浆抗凝活性进行分析。在兔和大鼠静脉推注期间评估RA36药效学参数的剂量范围分别为3 - 34 mg/kg和1 - 27 mg/kg。因此，为人类设计的剂量范围是1 - 29 mg/kg。
