EFFECTS OF OUABAIN ON MONO-VALENT CATION-TRANSPORT IN MAMMALIAN TISSUE

被引:2
作者
BERMAN, W
CHRISTENSEN, D
INTRESS, C
机构
来源
DEVELOPMENTAL PHARMACOLOGY AND THERAPEUTICS | 1986年 / 9卷 / 01期
关键词
D O I
10.1159/000457076
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
We measured the effects of ouabain sodium-potassium ATPase (Na-K ATPase) specific activity (SA) and rubidium (Rb) transport in newborn (NB) and adult (Ad) sheep myocardium (myo), guinea pig myo and red blood cells (RBC), and human RBC. 50% Inhibition of Na-K ATPase SA and Rb transport occurred at ouabain concentrations between 10-4.8 and 10-7.6 M in different species; within a species, 50% inhibition of Rb transport occurred at lower ouabain concentrations than 50% inhibition of Na-K ATPase SA. No differences between mature and immature tissues were found. Ouabain binding stability to Na-K ATPase extracted from myo and RBC did not vary with age. Binding studies revealed a KD .times. 10-8 M of 0.87 .+-. 0.09 for NB human RBC and 0.88 .+-. 0.14 for Ad human RBC. Calculated RBC receptor density however, was higher in the Ad (1.25 .+-. 0.08 sites/.mu.m2) than in the NB (1.03 .+-. 0.04 sites/.mu.m2, p < 0.01). Binding studies in extracted myocardial specimens showed a KD .times. 10-8 M of 1.23 .+-. 0.27 for NB and 1.09 .+-. 0.46 for Ad; mM ouabain bound .times. 10-12/Na-K ATPase unit were 355 .+-. 120 (SEM) for NB and 316 .+-. 51 for Ad. These studies of cardiac glycosides reveal few age-related differences in drug binding or inhibition of monovalent cation transport.
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页码:54 / 72
页数:19
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