首页> 美国卫生研究院文献>The Journal of Physiology >Kinetics of the inhibition of the Na-K pump by tetrapropylammonium chloride.
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Kinetics of the inhibition of the Na-K pump by tetrapropylammonium chloride.

机译:氯化四丙基铵对Na-K泵的抑制动力学。

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摘要

1. The tetrapropylammonium ion (TPA) acts as a mixed-type (with K) inhibitor of the Na-K pump. The kinetics of the process suggest that combination of the pump with a single TPA ion is sufficient for inhibition. 2. TPA inhibits the partial reactions of the Na-K pump (the uncoupled Na outflux, the Na-Na exchange, and K-K exchange). 3. TPA inhibits ouabain binding to the pump and this inhibitory effect is enhanced by external Na. The inhibitory effect of TPA on the pump rate is also promoted by external Na. 4. A Lineweaver-Burk plot of the reciprocal of the ouabain-sensitive K influx versus the reciprocal of the external K concentration is approximately a straight line if the measurements are made in Na-free solutions. TPA increases the apparent Michaelis constant (K 1/2) for K and the plot remains straight. 5. The Lineweaver-Burk plot is parabolic when the measurements are made in solutions which contain Na. TPA both increases the apparent K 1/2 for K and makes the curve more parabolic. 6. The characteristics of pump inhibition by TPA are similar to those for strophanthidin. In both cases the kinetic behaviour is consistent with a model in which the inhibitor binds: with greatest affinity to the pump form free of K; with less affinity to the pump form with a single bound K; and with least affinity to the pump form with two bound K.
机译:1.四丙基铵离子(TPA)作为Na-K泵的混合型(含K)抑制剂。该过程的动力学表明,泵与单个TPA离子的结合足以抑制。 2. TPA抑制Na-K泵的部分反应(未耦合的Na流出,Na-Na交换和K-K交换)。 3. TPA抑制哇巴因与泵的结合,外部Na增强了这种抑制作用。 TPA对泵速的抑制作用也由外部Na促进。 4.如果在无钠溶液中进行测量,则哇巴因敏感的K流入量的倒数与外部K浓度倒数的Lineweaver-Burk图近似为一条直线。 TPA增加了K的表观米氏常数(K 1/2),并且曲线保持直线。 5.当在含有Na的溶液中进行测量时,Lineweaver-Burk图是抛物线的。 TPA既增加了K的视在K 1/2,又使曲线更加抛物线。 6. TPA抑制泵浦的特性与鸟菊磷脂相似。在这两种情况下,动力学行为都与抑制剂结合的模型一致:对无K的泵浦形式具有最大亲和力;对具有单键K的泵浦形式的亲和力较小;对具有两个绑定K的泵浦形式的亲和力最低。

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