Interaction of endogenous compounds in human and rat urine with P-glycoprotein.

Drug Metab Pharmacokinet

Department of Pharmaceutics and Therapeutics, Division of Clinical Pharmaceutical Science, Programs for Pharmaceutical Sciences, Graduate School of Biomedical Sciences, Hiroshima University, Japan.

Published: March 2005

The effect of hydrophobic extracts of human and rat urine on in-vitro P-glycoprotein (P-gp) function was examined, in terms of intra-, inter-individual variations, and physiological states. Six urine samples out of 7, obtained from one male subject on different days, suppressed P-gp function with different potencies. Similarly, 11 samples out of 15 different individuals (8 males and 7 females) inhibited P-gp function. Among them, urine from one female, obtained 1 month after delivery, showed a potent inhibitory effect. Another urine from a pregnant female, obtained 1 week before delivery, showed further potent inhibition on P-gp function. In addition, urine from normal rats strongly inhibited P-gp function at much lower concentrations than human urine, and the inhibitory potencies varied in diseased states; control (without urine extract)=experimental acute renal failure

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http://dx.doi.org/10.2133/dmpk.17.245DOI Listing

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