Cholesterol modulates organic cation transport activity and lipid fluidity in rat renal brush-border membranes.

The role of cholesterol in organic cation transport was studied in rat renal brush-border membranes. H+ gradient-dependent uptake of the organic cation tetraethylammonium in brush-border membrane vesicles was stimulated by cholesterol enrichment in a dose-dependent manner. The dissipation rate of the H+ gradient, a driving force for organic cation transport in brush-border membranes, was reduced by cholesterol enrichment. Tetraethylammonium uptake in the absence of H+ gradient was also stimulated by cholesterol enrichment. These findings indicate that cholesterol modulates tetraethylammonium uptake by affecting the intrinsic activity of the organic cation transporter and the H+ gradient dissipation rate. Therefore, cholesterol content should be an important determinant for organic cation transport in renal brush-border membranes.