Relation between transport maxima and inhibition of organic cation excretion in the chicken kidney.

The ability of several organic cations to inhibit differentially the renal excretion of two prototypical organic cations, tetraethylammonium (TEA) and N1-methylnicotinamide (NMN), was investigated using the Sperber technique in chickens. TEA and NMN excretion were inhibited by the following organic cations in order of decreasing potency: quinine, TEA and NMN. The respective competitive potency of these substances was related inversely to their maximum tubular transport rates (Tm). Regardless of inhibitor used (quinine, TEA or NMN), NMN excretion was always inhibited more easily than TEA excretion. In addition, TEA excretion was suppressed more easily than cimetidine excretion by the competitive inhibitor quinine. The Tm of cimetidine was determined to be less than the Tm of TEA, which in turn is less than that of NMN. These results indicate that the Tm of an organic cation is related inversely to its inhibitory potency and related directly to its susceptibility to inhibition, reflecting different affinities of organic cations for the same carrier-mediated transport system.