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哇巴因在分离心肌细胞中的摄取时间进程:对细胞外钾和钙浓度的依赖性。

Time course of ouabain uptake in isolated myocardial cells: dependence on extracellular potassium and calcium concentration.

作者信息

Meldgaard L, Steiness E, Waldorff S

出版信息

Br J Pharmacol. 1981 Jun;73(2):341-5. doi: 10.1111/j.1476-5381.1981.tb10427.x.

Abstract

1 Spontaneously beating myocardial cells isolated from newborn rats have been used to evaluate the time course of cellular ouabain uptake. 2 The rate of cellular uptake and the amount of ouabain bound at equilibrium were computed by fitting the experimental data to the conventional exponential equation for receptor binding of drugs. 3 At normal extracellular potassium and calcium concentrations a biexponential equation was the best fit to the experimental data, indicating two receptor sites of ouabain with different rates of uptake. 4 Increasing extracellular potassium or calcium concentrations decreased the amounts of ouabain bound at equilibrium. 5 High and low extracellular concentrations of potassium or calcium decreased the rate of ouabain uptake. 6 It is well known that ouabain changes ionic fluxes. Changes in the extracellular potassium and calcium concentrations also influence the amount of ouabain taken up by myocardial cells, as demonstrated in the present study.

摘要
  1. 从新生大鼠分离出的自发性搏动心肌细胞已被用于评估细胞摄取哇巴因的时间进程。2. 通过将实验数据拟合到药物受体结合的传统指数方程来计算细胞摄取速率和平衡时结合的哇巴因量。3. 在正常细胞外钾和钙浓度下,双指数方程最适合实验数据,表明存在两个摄取速率不同的哇巴因受体位点。4. 增加细胞外钾或钙浓度会降低平衡时结合的哇巴因量。5. 细胞外高钾或高钙浓度以及低钾或低钙浓度均会降低哇巴因摄取速率。6. 众所周知,哇巴因会改变离子通量。如本研究所示,细胞外钾和钙浓度的变化也会影响心肌细胞摄取的哇巴因量。

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