Amiloride and 5-N,N-dimethylamiloride inhibit the carrier mediated uptake of choline in Ehrlich ascites tumor cells.

Amiloride and 5-N,N-dimethylamiloride (DMA) inhibit the choline uptake of Ehrlich ascites tumor cells. The inhibition by DMA is competitive with a KI value of 20 microM. The apparent KM value for choline was determined as 15 microM. Amiloride is approximately three times less potent. Amiloride uptake is not antagonized by choline or impaired in cells characterized by a deficient choline carrier. This indicates that amiloride is not transported into the cell by the choline carrier. The inhibition of the choline uptake by DMA cannot be attributed to a depression of choline kinase (EC 2.7.1.32) and is therefore considered to be due to a direct interaction between DMA and the choline carrier. DMA does not compete with sodium ions for its effect on the choline carrier. It is suggested that the choline carrier of Ehrlich ascites tumor cells exhibits a binding site for DMA similar to the one on the Na+/H+ antiporter.