Hongou K, Miyamae T, Hashizume H, Oshima K, Ogawa T, Hongou T, Morikawa T, Hagiwara M
Research Institute, Fuji Chemical Industries Co., Ltd., Toyama, Japan.
Arzneimittelforschung. 1997 Oct;47(10):1104-8.
3-([1:1',2':1"]-3'-Terphenyl)propanol (CAS 186835-06-3, F050) and acetylsalicylic acid (ASA) inhibited platelet aggregation induced by CaCl2, arachidonic acid, collagen, adenosine diphosphate (ADP) and thrombin in guinea pigs, rabbits and rats in vitro. However, F050 had a wider spectrum of actions than ASA. Orally administered F050 inhibited platelet aggregation ex vivo. F050 significantly reduced the thrombus formation in the extracorporeal circulation thrombosis model in guinea pigs. It inhibited erythrocyte hemolysis induced by hypotonic NaCl, while ASA did not. F050, but not ASA, inhibited increases in platelet [CA2+]i caused by thrombin in guinea pigs. F050 is a parent compound that will facilitate the development of an orally active drug for the treatment of thrombotic diseases.
3-([1:1',2':1"]-3'-三联苯)丙醇(CAS 186835-06-3,F050)和乙酰水杨酸(ASA)在体外对豚鼠、兔和大鼠由氯化钙、花生四烯酸、胶原、二磷酸腺苷(ADP)和凝血酶诱导的血小板聚集有抑制作用。然而,F050的作用谱比ASA更广。口服F050在体外能抑制血小板聚集。F050能显著减少豚鼠体外循环血栓形成模型中的血栓形成。它能抑制由低渗氯化钠诱导的红细胞溶血,而ASA则不能。F050而非ASA能抑制豚鼠中由凝血酶引起的血小板[Ca2+]i升高。F050是一种母体化合物,将有助于开发一种用于治疗血栓性疾病的口服活性药物。