Na+/H+ exchanger activity in the pig kidney epithelial cell line, LLC-PK1: inhibition by amiloride and its derivatives.
Na+/H+ exchanger activity in the pig kidney epithelial cell line, LLC-PK1: inhibition by amiloride and its derivatives.
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DOI：
10.1016/s0006-291x(85)80008-5
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发表时间：
1985-03
影响因子：
3.1
通讯作者：
J. G. Haggerty;E. Cragoe;C. Slayman;E. Adelberg
中科院分区：
文献类型：
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作者：
J. G. Haggerty;E. Cragoe;C. Slayman;E. Adelberg
快速生长的猪肾源性上皮细胞，LLC-PK1，在直接检测时缺乏可检测到的酰胺敏感的Na+/H+交换活性。在实验前，用含氯化铵或尼日利亚菌素的缓冲液孵育细胞，可诱导细胞大量摄取22na。在含有15 μM钠离子的缓冲液中，在3.5 ~ 4.5 μM范围内，钠离子对酸刺激钠摄取的抑制达到半最大值。当阿米洛利浓度低于25 μM，钠离子浓度高于20 mM时，阿米洛利与钠离子之间存在简单的竞争性相互作用。在5-氨基上携带取代基的阿米洛利衍生物的抑制作用比阿米洛利本身强35- 175倍。
Rapidly growing pig-kidney-derived epithelial cells, LLC-PK1, lack detectable amiloride-sensitive Na+/H+exchange activity when assayed directly. A large22Na uptake is induced when the cells are acid-loaded prior to assay by incubation with buffer containing ammonium chloride or nigericin. The acid-stimulated sodium uptake is sensitive to amiloride, with half-maximal inhibition at 3.5–4.5 μM in buffer containing 15 μM sodium ion. There is simple competitive interaction between amiloride and sodium ion when the amiloride concentration is below 25 μM and the sodium ion concentration is above 20 mM. Derivatives of amiloride which carry substituents on the 5-amino group are 35- to 175-fold more inhibitory than amiloride itself.