Cytoplasmic binding and disposition kinetics of diclofenac in the isolated perfused rat liver

Imatinib metabolism and disposition in isolated rat perfused liver

Imatinib is an orally administered tyrosine kinase inhibitor which inhibits the Bcr-Abl protein-tyrosine kinase with high selectivity. Imatinib is rapidly absorbed from the gut, after oral intake and has an almost absolute bioavailability of 98%. The metabolism of imatinib is mediated by the cytochrome P450 (CYP) isoenzymes in the liver and gut wall. CGP74588 is a major active metabolite of ima...

imatinib metabolism and disposition in isolated rat perfused liver

imatinib is an orally administered tyrosine kinase inhibitor which inhibits the bcr-abl protein-tyrosine kinase with high selectivity. imatinib is rapidly absorbed from the gut, after oral intake and has an almost absolute bioavailability of 98%. the metabolism of imatinib is mediated by the cytochrome p450 (cyp) isoenzymes in the liver and gut wall. cgp74588 is a major active metabolite of ima...

Disposition kinetics of propranolol isomers in the perfused rat liver.

The aim of this study was to define the determinants of the linear hepatic disposition kinetics of propranolol optical isomers using a perfused rat liver. Monensin was used to abolish the lysosomal proton gradient to allow an estimation of propranolol ion trapping by hepatic acidic vesicles. In vitro studies were used for independent estimates of microsomal binding and intrinsic clearance. Hepa...

Disposition and covalent binding of diflunisal and diflunisal acyl glucuronide in the isolated perfused rat liver.

Acyl glucuronides are intrinsically reactive metabolites of carboxylate drugs, capable of undergoing hydrolysis, intramolecular rearrangement (isomerization via acyl migration), and intermolecular transacylation reactions. Transacylation with nucleophilic groups located on protein molecules leads to covalent drug-protein adducts. Protein adducts can also form from the rearrangement isomers via ...

study on hepatobiliary disposition of etoposide in an isolated perfused rat liver model (iprl)