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乙酰毒毛旋花子苷元变力作用的线性剂量反应及钾对其的定量衰减

Linear dose response and quantitative attenuation by potassium of the inotropic action of acetylstrophanthidin.

作者信息

Lee G, Zelis R, Mason D T

出版信息

Clin Pharmacol Ther. 1977 Jul;22(1):34-41. doi: 10.1002/cpt197722134.

Abstract

To evaluate the nature of the inotropic dose response of digitalis and to determine the effects of potassium on this response, isometrically contracting isolated supported right ventricular cat papillary muscles were studied relative to their peak tension and peak dT/dt increases to physiologic cumulative doses of acetylstrophanthidin (ACS) in different extracellular potassium concentrations in the muscle bath. The inotropic dose response to ACS was observed to be linear in cumulative glycoside concentrations ranging from 0.40 to 4.23 X 10(-7) M ACS in 3.5 mM K+ medium and from 1.22 to 7.47 X 10(-7) M ACS in 7.0 mM K+ medium. The influence of potassium alterations in the muscle bath from the low to the high K+ concentrations prior to ACS resulted in marked attenuation of the positive inotropic property of ACS. From these data, it is concluded that the dose inotropic response of digitalis is linear, with small doses producing proportionally the same effects as larger doses, and that extracellular potassium markedly influences this linear dose response such that higher K+ concentrations considerably attenuate the positive inotropic response of digitalis.

摘要

为评估洋地黄的变力剂量反应特性,并确定钾对该反应的影响,研究了在肌肉浴中不同细胞外钾浓度下,等长收缩的离体支持右心室猫乳头肌对生理累积剂量毒毛花苷(ACS)的峰值张力和峰值dT/dt增加情况。在3.5 mM K⁺ 培养基中,当累积糖苷浓度在0.40至4.23×10⁻⁷ M ACS范围内,以及在7.0 mM K⁺ 培养基中,当累积糖苷浓度在1.22至7.47×10⁻⁷ M ACS范围内时,观察到对ACS的变力剂量反应呈线性。在加入ACS之前,将肌肉浴中的钾浓度从低浓度改变为高浓度,导致ACS的正性变力特性明显减弱。从这些数据得出结论,洋地黄的剂量变力反应是线性的,小剂量产生的效果与大剂量成比例相同,并且细胞外钾显著影响这种线性剂量反应,使得较高的K⁺ 浓度会大大减弱洋地黄的正性变力反应。

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