Abstract

SummaryTreatment of rats with benziodarone (50 mg/kg ip) 1 hr prior to infusion of BSP resulted in marked impairment of the biliary excretion of BSP. Total BSP concentration was decreased and this was due to a decrease in the BSP-GSH component, while unconjugated BSP concentration was increased. Benziodarone is a potent inhibitor of the S-arylglutathione transferase enzyme system which catalyses BSP conjugation with GSH. Benziodarone was found to inhibit the biliary excretion of synthetic BSP-GSH conjugates, although not that of DBSP, a BSP analog excreted without conjugation. It is proposed that benziodarone exerts its influence on BSP excretion by a combination of effects on conjugation and BSP-GSH transport, and that the results have uncovered the possibility that separate mechanisms may exist for the biliary excretion of conjugated and unconjugated dyes.The technical assistance of Mrs. M.-Y. Guillaume is gratefully acknowledged. We are indebted to Doctor H. A. Brown Dunning, Jr. of Hynson Westcott and...

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