新型药物5-(Z,E)-13,14-二脱氢-20-甲基-碳前列环素（FCE 22509）对血小板聚集的抑制作用

Inhibition of platelet aggregation by a new agent, 5-(Z,E)-13,14-didehydro-20-methyl-carbo PGI2 (FCE 22509).

作者信息

Bergamaschi M, Pierucci L, Ferti C, Corsi G, Branzoli U, Mandelli V

出版信息

Prostaglandins Leukot Med. 1984 Oct;16(1):19-27. doi: 10.1016/0262-1746(84)90082-9.

Abstract

FCE (+)22509, a chemically stable carboprostacyclin analogue, inhibited in vitro ADP-induced platelet aggregation in rat platelet-rich plasma (PRP) (IC50 = 7.7 ng/ml). Subcutaneous administration of the drug, inhibited both ADP-induced platelet aggregation in rat PRP (ED50 = 0.26 mg/kg) and mortality of mice induced by collagen plus adrenaline (ED50 = 0.35 mg/kg). The compound had no such preventive effects when given orally.

摘要

FCE(+)22509是一种化学性质稳定的卡前列环素类似物，在体外可抑制大鼠富血小板血浆（PRP）中由二磷酸腺苷（ADP）诱导的血小板聚集（半数抑制浓度[IC50]=7.7纳克/毫升）。皮下注射该药物可抑制大鼠PRP中由ADP诱导的血小板聚集（半数有效剂量[ED50]=0.26毫克/千克）以及由胶原蛋白加肾上腺素诱导的小鼠死亡率（ED50=0.35毫克/千克）。口服该化合物则无此预防作用。