Kinetic measurements of the biliary excretion of metabolized compounds

Powell, Gavin; Jones, John G.; Curtis, C. G.

doi:10.1042/bj1880561

Cited by 1 publication

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“…This indicates the existence of a 'storage' compartment within the liver into which the drug may be passed, thus maintaining hepatic uptake. Kinetic models for hepatic transport which include such a compartment have been described (Powell, Jones & Curtis, 1980). BSP seems to be readily released from this store, as judged by the recovery of BSP in bile at the end of infusion, whereas this appears not to be so for SITS.…”

Section: Hepatic Transport Of Sitsmentioning

confidence: 99%

Uptake and action of a disulphonic stilbene (SITS) in the perfused guinea‐pig liver: a comparison with bromsulphthalein.

Rutishauser¹

1983

The Journal of Physiology

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SUMMARY1. Livers were perfused with a Krebs-Ringer bicarbonate buffer in a single-pass perfusion system. Bile secretion was maintained by infusion of secretin. 4-Acetamido-4'-isothiocyano-2,2'-stilbene disulphonic acid (SITS) was added to the perfusate to give concentrations ranging between 5 x 10-6 and 10-4 M.2. SITS was extracted from the perfusate by the liver (V, 0 15 ,tmol/min per g liver; Km 8X6 x 10-5 M) and excreted in bile in a modified form (bile/plasma ratio: 50-170; maximum rate of excretion: 25 nmol/min per g liver wet wt).3. The rates of uptake and excretion of bromsulphthalein (BSP) were similar to those for SITS, with the exception that the affinity of BSP for hepatic uptake was greater (Km 1-8 x 10-5 M).4. Both SITS and BSP decreased the rate of bile flow. A 50 % reduction in bile flow was attained in each case at an estimated drug content of the liver of 1-5 umol/g wet wt.5. Unlike other cells the hepatocyte appears to be readily penetrated by SITS, and it is suggested that SITS inhibits bile secretion by inhibiting an intracellular mechanism which could be mitochondrial in location.

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Section: Hepatic Transport Of Sitsmentioning

confidence: 99%

Uptake and action of a disulphonic stilbene (SITS) in the perfused guinea‐pig liver: a comparison with bromsulphthalein.

Rutishauser¹

1983

The Journal of Physiology

View full text Add to dashboard Cite

show abstract

Kinetic measurements of the biliary excretion of metabolized compounds

Cited by 1 publication

References 5 publications

Uptake and action of a disulphonic stilbene (SITS) in the perfused guinea‐pig liver: a comparison with bromsulphthalein.

Uptake and action of a disulphonic stilbene (SITS) in the perfused guinea‐pig liver: a comparison with bromsulphthalein.

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