Yamada K, Shuto K, Nakamizo N
Thromb Res. 1983 Jan 15;29(2):197-206. doi: 10.1016/0049-3848(83)90141-x.
KF4939, 2,2'-dithiobis-(N-2-hydroxypropylbenzamide), is a potent inhibitor of platelet aggregation in vitro in rabbit and human PRP. This agent inhibited both cyclooxygenase product-dependent (collagen and arachidonate) and independent (ADP and thrombin)-platelet aggregations. This action carried over to ex vivo situation following intraduodenal dosing as demonstrated in rabbits. KF4939 inhibited experimentally induced thrombocytopenias in rats and pulmonary thrombosis in mice following oral doses in a range of 25-300mg/kg. These results indicate that KF4939 is a new orally active inhibitor of platelet aggregation possessing a different mode of action from cyclooxygenase inhibition.
KF4939,即2,2'-二硫代双-(N-2-羟丙基苯甲酰胺),是一种在体外对兔和人富血小板血浆中血小板聚集有强效抑制作用的物质。该药物既能抑制依赖环氧化酶产物的(胶原和花生四烯酸)血小板聚集,也能抑制非依赖环氧化酶产物的(二磷酸腺苷和凝血酶)血小板聚集。如在兔身上所证实的那样,十二指肠给药后,这种作用在体内环境中依然存在。口服剂量在25至300毫克/千克范围内时,KF4939可抑制大鼠实验性诱导的血小板减少以及小鼠的肺血栓形成。这些结果表明,KF4939是一种新型的口服活性血小板聚集抑制剂,其作用方式与抑制环氧化酶不同。