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钙通道阻滞剂硝苯地平对高血压患者红细胞膜钙泵ATP酶的抑制作用。

Inhibition of erythrocyte membrane Ca(2+)-pumping ATPase of hypertensive humans by nifedipine, a calcium entry blocker.

作者信息

Olorunsogo O O, Onatola O O, Lawal S O, Bababunmi E A, Falase A O, Okunade W G

机构信息

Department of Biochemistry, College of Medicine, University of Ibadan, Nigeria.

出版信息

Afr J Med Med Sci. 1991 Mar;20(1):61-5.

PMID:1829316
Abstract

Nifedipine, a 1,4-dihydropyridine antihypertensive drug, inhibited the basal activity of erythrocyte Ca2+,Mg(2+)-ATPase of hypertensive individuals in a concentration-dependent manner. About 50% inhibition was obtained at nifedipine concentrations greater than or equal to 300 microM. The extent of inhibition of the ATPase action was increased in the presence of calmodulin. Maximal inhibition at 400 microM was 76%. Furthermore, the activity of the partially trypsinized enzyme was inhibited by about 50% by 300 microM nifedipine. Similar results were obtained with membranes from normotensive individuals. These findings suggest that nifedipine could prevent Ca(2+)-pumping by the erythrocyte Ca2+,Mg(2+)-ATPase.

摘要

硝苯地平是一种1,4 - 二氢吡啶类抗高血压药物,它以浓度依赖的方式抑制高血压患者红细胞Ca2 +,Mg(2 +)-ATP酶的基础活性。当硝苯地平浓度大于或等于300微摩尔时,可产生约50%的抑制作用。在钙调蛋白存在的情况下,ATP酶活性的抑制程度增加。在400微摩尔时最大抑制率为76%。此外,300微摩尔硝苯地平可使部分经胰蛋白酶处理的酶活性受到约50%的抑制。血压正常者的细胞膜也得到了类似结果。这些发现表明硝苯地平可能会阻止红细胞Ca2 +,Mg(2 +)-ATP酶的Ca(2 +)泵浦作用。

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