Anticoagulant and antithrombotic properties of synthetic sulfated bis-lactobionic acid amides.
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.
Raake
W
W
Division "Research and Development" Luitpold-Werk, München, FRG.
Klauser
R J
RJ
Elling
H
H
Meinetsberger
E
E
D000818:Animals; D000925:Anticoagulants; D004187:Disaccharides / Q000494:pharmacology*; D004195:Disease Models, Animal; D065427:Factor Xa Inhibitors; D005343:Fibrinolytic Agents; D006493:Heparin / Q000494:pharmacology; D006495:Heparin, Low-Molecular-Weight / Q000494:pharmacology; D008297:Male; D015394:Molecular Structure; D010314:Partial Thromboplastin Time; D011516:Prothrombin / Q000037:antagonists & inhibitors; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D013918:Thrombin Time; D013924:Thrombophlebitis / Q000188:drug therapy
D000925:Anticoagulants; D004187:Disaccharides; D065427:Factor Xa Inhibitors; D005343:Fibrinolytic Agents; D006495:Heparin, Low-Molecular-Weight; D011516:Prothrombin; C025337:Factor IIa; D006493:Heparin