Ehlert F J, Yamamura H I
Life Sci. 1984 Jun 11;34(24):2347-55. doi: 10.1016/0024-3205(84)90421-1.
The influence of cinnarizine, flunarizine and lidoflazine on [3H]nitrendipine binding in the cerebral cortex, heart and longitudinal muscle of the ileum was investigated. When assays were run in Ca++ free Tris/HCl buffer on extensively washed tissue homogenates, cinnarizine, flunarizine and lidoflazine were approximately equipotent inhibitors of [3H] nitrendipine binding in the heart and cerebral cortex, with Ki values of approximately 10(-6) M. In contrast, the compounds were 4 to 100 times more potent in the ileum with the rank order of potency being: lidoflazine greater than flunarizine greater than cinnarizine. The same rank order of potency was observed in the ileum when assays were run in the presence of 1 mM Ca++, although all three drugs were somewhat less potent. Similarly, Ca++ inhibited the binding of the cinnarizine-like drugs in the cerebral cortex and heart as well, with all drugs being less potent than that observed in the ileum under similar assay conditions.
研究了桂利嗪、氟桂利嗪和利多氟嗪对大脑皮层、心脏及回肠纵肌中[3H]尼群地平结合的影响。当在无Ca++的Tris/HCl缓冲液中对充分洗涤的组织匀浆进行测定时，桂利嗪、氟桂利嗪和利多氟嗪在心脏和大脑皮层中对[3H]尼群地平结合的抑制作用大致相当，其Ki值约为10(-6)M。相比之下，这些化合物在回肠中的效力要强4至100倍，效力顺序为：利多氟嗪＞氟桂利嗪＞桂利嗪。当在1 mM Ca++存在的情况下进行测定时，在回肠中也观察到了相同的效力顺序，尽管所有三种药物的效力都有所降低。同样，Ca++也抑制了大脑皮层和心脏中类似桂利嗪药物的结合，在类似的测定条件下，所有药物的效力都低于在回肠中观察到的效力。
