Mestre M, Clairefond P, Mardiguian J, Trillou M, Le Fur G, Uzan A
Thromb Res. 1985 May 15;38(4):389-99. doi: 10.1016/0049-3848(85)90137-9.
The comparative properties of heparin and PK 10169, a low molecular weight fraction, were studied using an antithrombotic test in anaesthetized dogs. The antithrombotic properties of the two compounds were evaluated by measuring inhibition of thrombus formation following transluminar stimulation of coronary artery with anodal current and by measuring anticoagulant properties, anti Xa and anti IIa activities. The results show that PK 10169 displayed significant antithrombotic activities above 0.625 mg/kg and was equipotent at 2.5 mg/kg s.c. with heparin 10 mg/kg s.c. No correlation could be observed between antithrombotic/anti Xa ratio of both compounds. Moreover it was shown that, unlike heparin, PK 10169 s.c. was devoid of obvious anticoagulant properties and induced a negligible anti IIa activity contrasting with a high anti Xa level. A similar dissociation between anti Xa and anti IIa activities was observed following i.v. administration of 2.5 mg/kg of PK 10169 but not with heparin. This low molecular weight heparin fraction might thus be regarded as a potential arterial antithrombotic agent devoid of appreciable anticoagulant effect.
使用麻醉犬的抗血栓形成试验，研究了肝素和低分子量组分PK 10169的比较特性。通过测量阳极电流经冠状动脉腔内刺激后血栓形成的抑制情况以及测量抗凝特性、抗Xa和抗IIa活性，来评估这两种化合物的抗血栓形成特性。结果表明，PK 10169在剂量高于0.625 mg/kg时显示出显著的抗血栓形成活性，且在皮下注射2.5 mg/kg时与皮下注射10 mg/kg的肝素等效。两种化合物的抗血栓形成/抗Xa比值之间未观察到相关性。此外，研究表明，与肝素不同，皮下注射PK 10169没有明显的抗凝特性，诱导的抗IIa活性可忽略不计，而抗Xa水平较高。静脉注射2.5 mg/kg的PK 10169后观察到了类似的抗Xa和抗IIa活性解离情况，但肝素未出现这种情况。因此，这种低分子量肝素组分可能被视为一种潜在的动脉抗血栓形成药物，且没有明显的抗凝作用。
