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The effects of amiloride and a series of amiloride analogs have been tested on the Na(+)/H(+) antiport activity in intact vacuoles and tonoplast vesicles isolated from sugar beet cell suspension cultures. There is a competitive interaction between amiloride analogs and sodium. Substitution of one or both H-atoms of the 5-amino group of amiloride (apparent K(i) about 150 micromolar) resulted in a 3- to 200-fold increase in inhibitory potency of the antiport activity.
Blumwald et al. (Tue,) studied this question.