Accumulation of cimetidine by kidney cortex slices.

摘要: The mechanisms involved in the excretion of histamine H2-receptor antagonist cimetidine are as yet incompletely understood. purpose this study was to examine interaction with incubated slices dog kidney cortex. results time and concentration-dependent experiments by using 3H-labeled demonstrated that drug accumulated without metabolism against a concentration gradient saturable process. Inhibition uptake cyanide incubation under nitrogen atmosphere indicated energy dependence. Uptake active cationic transport likely inasmuch both cyanine 863 quinine blocked accumulation. However, probenecid-sensitive component, accounting for about 20% steady-state accumulation, also identified. lack inhibitory action p-aminohippuric acid nature molecule suggest probenecid-sensitivity not related renal organic anion mechanism. Further, probenecid inhibition due generalized cellular toxicity because maximally concentrations did interfere cation tetraethylammonium.