Wang Y L, He R R
Department of Pharmacology, Hebei Medical College, Shijiazhuang, China.
Zhongguo Yao Li Xue Bao. 1994 Sep;15(5):443-6.
Dipfluzine (Dip) is a novel diphenylpiperazine calcium channel blocker first synthesized in China. Effects of Dip on experimental thrombosis and platelet aggregation were studied in vitro and in vivo compared with cinnarizine (Cin). Dip 1 and 2 mg.kg-1 i.v. and incubated in 1-100 mumol.L-1 in vitro inhibited dose- or concentration-dependent rabbit platelet aggregation induced by ADP and by arachidonic acid (AA), respectively. Dip 2.5-10 mg.kg-1 i.v. and 50-100 mg.kg-1 ip inhibited the thrombosis in rats. Dip 10 mg.kg-1 i.v. and 200 mumol.L-1 depressed the in vitro thrombosis. These results suggest that attenuation of disturbed platelet-vessel wall reaction associated with platelet activation and vasoconstriction may be a main factor involved in the antithrombotic action of Dip, and that the effects of Dip were more potent than those of Cin.
双苯氟嗪(Dip)是一种新型的二苯基哌嗪类钙通道阻滞剂,由中国首次合成。与桂利嗪(Cin)相比,在体外和体内研究了双苯氟嗪对实验性血栓形成和血小板聚集的影响。静脉注射双苯氟嗪1和2mg·kg-1,并在体外以1-100μmol·L-1孵育,分别剂量依赖性或浓度依赖性地抑制了由ADP和花生四烯酸(AA)诱导的兔血小板聚集。静脉注射双苯氟嗪2.5-10mg·kg-1和腹腔注射50-100mg·kg-1可抑制大鼠血栓形成。静脉注射双苯氟嗪10mg·kg-1和200μmol·L-1可抑制体外血栓形成。这些结果表明,减轻与血小板活化和血管收缩相关的血小板-血管壁反应紊乱可能是双苯氟嗪抗血栓作用的主要因素,且双苯氟嗪的作用比桂利嗪更强。