Denolle T, Plouin P F
Therapie. 1989 May-Jun;44(3):215-7.
The sodium-hydrogen (Na+/H+) antiport is electroneutral and amiloride-sensitive. It exchanges Na+ for H+ with a coupling ratio of 1:1 and therefore, it has important cellular functions: intracellular pH and cell volume regulation, control of the cell differentiation and growth. Its activity is increased in hypertension. The responsibility of the Na+/H+ antiport in essential hypertension may result in increased vascular tone and vascular hyperplasia. Amiloride is a specific inhibitor of this exchanger but under physiological conditions, very high concentrations of this drug (that are unlikely to be attained in vivo) are required to inhibit the activity of the Na+/H+ antiport. Certain of its analogues are much more potent in vitro than amiloride. Therefore, the Na+/H+ antiport may become a target for new antihypertensive drugs.
钠氢(Na+/H+)逆向转运体呈电中性且对氨氯地平敏感。它以1:1的偶联比例将Na+与H+进行交换,因此具有重要的细胞功能:调节细胞内pH值和细胞体积,控制细胞分化和生长。其活性在高血压状态下会增强。原发性高血压中Na+/H+逆向转运体的作用可能导致血管张力增加和血管增生。氨氯地平是这种交换体的特异性抑制剂,但在生理条件下,需要非常高浓度的该药物(体内不太可能达到此浓度)才能抑制Na+/H+逆向转运体的活性。其某些类似物在体外比氨氯地平的效力要强得多。因此,Na+/H+逆向转运体可能成为新型抗高血压药物的作用靶点。