This article deals with the analysis of drug transport systems in the plasma membranes of the intestinal and renal epithelial cells. Aminocephalosporins such as cephradine and cephalexin, possessing an α-amino group and a carboxyl group, can be transported via common carrier system with dipeptides in the intestinal and renal brush border membranes, and that this process is driven by an inward H
+ gradient (H
+ cotransport system). The tubular secretion involves transport across basolateral membranes, and accumulation in the epithelial cells followed by efflux from the cells across brush border membranes into the urine. Tetraethylammonium (TEA), a prototype cation, is transported across basolateral membranes via carrier-mediated system, which is stimulated by an inside-negative membrane potential. TEA transport across brush border membranes is driven by an H
+ gradient via electroneutral H
+/ TEA antiport system. In contrast,
p-aminohippurate is transported by an anion exchange mechanism in basolateral membranes. Thus, the vesicle studies have provided a great deal of information about the coupled transport of drugs in the intestine and renal tubule.
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