Udvardy M, Posan E, Harsfalvi J, Dinya Z
2nd Department of Medicine, Debrecen University Medical School, Hungary.
Blood Coagul Fibrinolysis. 1996 Mar;7(2):256-8. doi: 10.1097/00001721-199603000-00037.
Pentamidine, a highly toxic drug, possesses RGD-peptide (Arg-Gly-Asp)-like antiplatelet actions. The objective of this investigation was to study the anticipated profibrinolytic and antiplatelet actions of pentamidine and of pentamidine (bearing guanidino-like groups)-related synthetic peptidomimetic compounds. Platelet aggregation inhibition was assessed using ADP, thrombin, collagen, arachidonic acid and epinephrine as inducers, by aggregometry. In vitro chromogenic plasmin generation tests and clot lysis assays were also performed. Two (assigned as D-2 and D-3) of the synthetic pentamidine-guanidino related molecules were able to inhibit platelet aggregation and simultaneously accelerate in vitro plasmin generation and clot-lysis in the nM range. These dual action antithrombotic agents now need to be tested further to assess their antithrombotic actions in vivo.
喷他脒是一种剧毒药物，具有类RGD肽（精氨酸-甘氨酸-天冬氨酸）的抗血小板作用。本研究的目的是研究喷他脒以及与喷他脒（带有类胍基）相关的合成拟肽化合物预期的纤溶和抗血小板作用。使用ADP、凝血酶、胶原蛋白、花生四烯酸和肾上腺素作为诱导剂，通过凝集测定法评估血小板聚集抑制情况。还进行了体外显色纤溶酶生成试验和血凝块溶解试验。两种与喷他脒-胍基相关的合成分子（分别命名为D-2和D-3）能够在纳摩尔范围内抑制血小板聚集，同时加速体外纤溶酶生成和血凝块溶解。这些具有双重作用的抗血栓药物现在需要进一步测试，以评估它们在体内的抗血栓作用。
