Kasher J S, Holohan P D, Ross C R
J Pharmacol Exp Ther. 1983 Oct;227(1):122-9.
The relationship between the transmembrane Na+ gradient and p-aminohippurate (PAH) transport was examined in isolated rat basolateral membrane vesicles. A 100 mM Na+ gradient (o leads to i) accelerated the influx of 50 microM [3H]PAH whereas similar gradients of choline+, K+, or Li+ did not. The sodium effect was not due to a diffusion potential. The Na+ gradient (o leads to i) decreased the apparent Michaelis constant for PAH from 0.167 +/- 0.016 to 0.054 +/- 0.016 mM and increased the maximum flux rate from 116.00 +/- 13.50 to 427.34 +/- 98.96 pmol/mg/min. An "overshoot" of [3H]PAH influx (159 +/- 4% of the equilibrium value) could be demonstrated only in the presence of a Na+ gradient (o leads to i) plus an opposing gradient of unlabeled PAH (i leads to o). These results suggest that PAH transport and the Na+ gradient are functionally related. A model for cellular uptake of PAH by a Na+ gradient-dependent anion exchange mechanism is presented.
在分离的大鼠基底外侧膜囊泡中研究了跨膜钠梯度与对氨基马尿酸(PAH)转运之间的关系。100 mM的钠梯度(外向内)加速了50 μM [³H]PAH的内流,而胆碱⁺、钾⁺或锂⁺的类似梯度则没有这种作用。钠的作用并非由于扩散电位。钠梯度(外向内)使PAH的表观米氏常数从0.167±0.016 mM降至0.054±0.016 mM,并使最大通量率从116.00±13.50增加至427.34±98.96 pmol/mg/min。只有在存在钠梯度(外向内)加上未标记PAH的反向梯度(内向外)时,才能证明[³H]PAH内流出现“过冲”(为平衡值的159±4%)。这些结果表明PAH转运与钠梯度在功能上相关。本文提出了一种通过钠梯度依赖性阴离子交换机制进行细胞摄取PAH的模型。