Van Nueten J M, Van Beek J, Janssen P A
Arch Int Pharmacodyn Ther. 1978 Mar;232(1):42-52.
Flunarizine, a difluoro derivative of cinnarizine, is a potent inhibitor of Ca2+-induced constriction of isolated arteries; this inhibition has a gradual onset and a prolonged duration. The present study demonstrates that flunarizine inhibits Ca2+-induced responses in the rat tail and the rabbit ear arteries, but not in isolated cat papillary muscle; flunarizine does not depress the spontaneous rhythmic activity of the rat portal-mesenteric vein. This dissociation between the arterial preparations on the one hand, was less pronounced with cinnarizine, and was not seen with verapamil and papaverine. The present experiments thus suggest that flunarizine inhibits peripheral vasoconstriction by selectively decreasing the rate of stimulated Ca2+-influx, without affecting the myogenic activity of the vascular smooth muscle cells.
氟桂利嗪是桂利嗪的二氟衍生物,是离体动脉钙诱导收缩的有效抑制剂;这种抑制作用起效缓慢且持续时间长。本研究表明,氟桂利嗪可抑制大鼠尾部和兔耳动脉的钙诱导反应,但对离体猫乳头肌无此作用;氟桂利嗪不抑制大鼠门静脉-肠系膜静脉的自发节律性活动。一方面,这种动脉制剂之间的差异在桂利嗪作用时不太明显,而维拉帕米和罂粟碱则无此差异。因此,本实验提示氟桂利嗪通过选择性降低刺激的钙内流速率来抑制外周血管收缩,而不影响血管平滑肌细胞的肌源性活动。