Kinetics studies on the renal transport of probenecid in vitro.
1. The kinetic parameters of renal transport of probenecid have been assessed by studying the uptake of the drug in rabbit kidney tubules incubated in an electrolyte medium under various conditions. 2. The added compounds inhibited the uptake of probenecid both by kidney cortical slices and separated renal tubule preparations in the following order: p-aminohippurate less than phenol red less than bromophenol blue less than bromocresol green. A reversible competitive inhibitory effect of these organic anions on the renal accumulation of the drug was observed. 3. The Km for renal uptake of probenecid in separated tubules (0.04 mM) and the KI values calculated in this system for p-aminohippurate (0.5 mM), phenol red (0.09 mM), bromophenol blue (0.02 mM) and bromocresol green (0.015 mM) were found to be in good agreement with the corresponding KI value of probenecid and Km values of these compounds previously observed in various kidney tissue preparations. 4. On the basis of above mentioned findings, it is concluded that probenecid, p-aminohippurate and various phenolsulphonphthalein dyes are transported by the common renal organic anion transport system.
D000818:Animals; D001667:Binding, Competitive; D001693:Biological Transport, Active / Q000187:drug effects; D001961:Bromcresol Green / Q000494:pharmacology; D001978:Bromphenol Blue / Q000494:pharmacology; D005260:Female; D007684:Kidney Tubules / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D010637:Phenolsulfonphthalein / Q000494:pharmacology; D011339:Probenecid / Q000378:metabolism*; D011817:Rabbits; D010130:p-Aminohippuric Acid / Q000494:pharmacology
D001978:Bromphenol Blue; D001961:Bromcresol Green; D010637:Phenolsulfonphthalein; D011339:Probenecid; D010130:p-Aminohippuric Acid