Schmidt W F, Asakura T, Schwartz E
Blood Cells. 1982;8(2):289-98.
We report the effects of cetiedil, a new antisickling agent, on red cell membrane permeability. With fresh red cells containing normal levels of intracellular ATP, cetiedil increases membrane permeability to both sodium and potassium. With drug concentrations from 100 to 500 microM, net sodium gain exceeds net potassium loss, and the cells quickly swell. Changes are identical with normal and sickle red cells. Membrane permeability returns to normal after washing the cells in buffer free of cetiedil. In the absence of phosphate, ouabain potentiates the cetiedil effect. With external phosphate present, the effect of cetiedil is also enhanced, but ouabain is without effect. Our findings support the idea that the antisickling effect of cetiedil observed in vitro is secondary to cell swelling.
我们报告了一种新型抗镰状细胞病药物西替地尔对红细胞膜通透性的影响。对于含有正常细胞内ATP水平的新鲜红细胞，西替地尔可增加细胞膜对钠和钾的通透性。当药物浓度为100至500微摩尔时，钠的净增加量超过钾的净损失量，细胞迅速肿胀。正常红细胞和镰状红细胞的变化相同。在不含西替地尔的缓冲液中洗涤细胞后，膜通透性恢复正常。在没有磷酸盐的情况下，哇巴因可增强西替地尔的作用。当存在外部磷酸盐时，西替地尔的作用也会增强，但哇巴因没有作用。我们的研究结果支持这样一种观点，即在体外观察到的西替地尔的抗镰状细胞病作用是细胞肿胀的继发效应。
