Raake W, Klauser R J, Elling H, Meinetsberger E
Division "Research and Development" Luitpold-Werk, München, FRG.
Thromb Res. 1989 Dec 15;56(6):719-30. doi: 10.1016/0049-3848(89)90289-2.
Sulfated bis-lactobionic acid amides, a new class of polyanions with heparin-like properties, were synthesized and their antithrombotic and anticoagulant activities were determined. Compared to heparin and Fragmin, a low molecular weight heparin, the substances exhibited moderate to low anticoagulant activities in aPTT, thrombin clotting time and Heptest assays. In amidolytic assays no anti-IIa activity and only exceedingly low anti-Xa activity was observed. The antithrombotic activity of the bis-lactobionic acid amides was determined using two thrombosis models. In rabbit and rat models thrombi were induced by a combination of endothelial damage and reduction of blood flow or only by endothelial damage. At least one of the bis-lactobionic acid amides (LW 10082) exhibited a considerable antithrombotic activity which was similar to low molecular weight heparin.
合成了具有类肝素性质的新型聚阴离子——硫酸化双乳糖醛酸酰胺，并测定了它们的抗血栓和抗凝活性。与肝素和低分子肝素法安明相比，这些物质在活化部分凝血活酶时间（aPTT）、凝血酶凝血时间和希普测试中表现出中度至低度的抗凝活性。在酰胺水解试验中，未观察到抗凝血酶IIa活性，仅观察到极低的抗Xa活性。使用两种血栓形成模型测定了双乳糖醛酸酰胺的抗血栓活性。在兔和大鼠模型中，通过内皮损伤和血流减少的联合作用或仅通过内皮损伤诱导血栓形成。至少一种双乳糖醛酸酰胺（LW 10082）表现出相当大的抗血栓活性，这与低分子肝素相似。
