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吩噻嗪类药物在体外的睫状肌抑制作用及其被钙离子的拮抗作用。

Cilioinhibitory effect of phenothiazines in vitro and its antagonism by Ca++.

作者信息

Adler K B, Fand I

出版信息

Arch Int Pharmacodyn Ther. 1977 Jun;227(2):309-23.

PMID:20858
Abstract

The inhibition of ciliary beating in vitro by physiologic concentrations of chlorpromazine (CPZ) and prochlorperazine (PCP) was demonstrated in two experimental systems. CPZ had a greater cilioinhibitory effect than PCP on the rotational velocity of tissue explants from the frog palate in amphibian Ringers, and on the frequency of ciliary beating in rat tracheal rings in culture medium. Addition of calcium acetate in equal molarity to CPZ, within a time limit dependent on the drug concentration, reversed this inhibition, while dibutyryl cyclic AMP did not. Simultaneous addition of Ca++ and CPZ slowed down, but did not stop, this ciliostasis, while priming with Ca++ or cyclic AMP prior to drug addition had less of an effect. These data lend support to a prevalent theory that CPZ exerts its actions by displacing calcium ions from membrane sites.

摘要

在两个实验系统中证实了生理浓度的氯丙嗪(CPZ)和丙氯拉嗪(PCP)在体外对纤毛摆动的抑制作用。在两栖类林格氏液中,CPZ对青蛙腭部组织外植体的旋转速度,以及在培养基中对大鼠气管环的纤毛摆动频率,其纤毛抑制作用比PCP更强。在取决于药物浓度的时间限制内,加入与CPZ等摩尔浓度的醋酸钙可逆转这种抑制作用,而二丁酰环磷酸腺苷则不能。同时加入Ca++和CPZ会减缓但不会停止这种纤毛运动停滞,而在加入药物之前先用Ca++或环磷酸腺苷预处理则效果较差。这些数据支持了一种普遍的理论,即CPZ通过从膜位点置换钙离子来发挥其作用。

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