Transport hepatic

The liver plays an important role in determining the oral bioavailability of drags. Drag molecules absorbed into the portal vein are taken up by hepatocytes, and then metabolized and/or excreted into the bile. For hydrophilic drugs, transporters located on the sinusoidal membrane are responsible for the hepatic uptake [1, 2]. Biliary excretion of many drags is also mediated by the primary active transporters, referred to as ATP-binding cassette transmembrane (ABC) transporters, located on the bile canalicular membrane [1, 3-5], Recently, many molecular biological 

Area under the (plasma concentration-time) curve 

Cell line human colon carcinoma cells 

Drug Bioavailability Estimation of SolubilityPermeability Absorption and Bioavailability. Edited by Han van de Waterbeemd, Hans Lennemas and Per Artursson Copyright 2003 WILEY-VCH Verlag GmbH Co. KGaA, Weinheim ISBN 3-527-30438-X 

Kazuya Maeda, Hiroshi Suzuki, and Yuichi Sugiyama 

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Bohan, A., Boyer, J. L., Mechanism of hepatic transport of drugs implications for cholestatic drug reactions, Semin. Liv. Dis. 2002, 22, 123-136. 

The synthesis, glucuronidation and hepatic transport of new aromatic congeners of bilirubin have also been followed by an RP-HPLC method. The chemical strucutres of bilirubin derivatives are shown in Fig. 2.160. 

J.O. Brower, D.A. Lightner and A.F. McDonagh, Aromatic congeners of bilirubin synthesis, stereochemistry, glucuronidation and hepatic transport. Tetrahedron 57 (2001) 7813-7827. 

These results also indicate that human hepatocytes are an appropriate model in which to study inter-species differences and the mechanisms of hepatic transport in man. 

LIVER Use of isolated perfused liver in studies of biological transport processes, 192, 485 measurement of unidirectional calcium ion fluxes in liver, 192, 495 preparation and specific applications of isolated hepatocyte couplets, 192, 501 characterizing mechanisms of hepatic bile acid transport utilizing isolated membrane vesicles, 192, 517 preparation of basolateral (sinusoidal) and canalicular plasma membrane vesicles for the study of hepatic transport processes, 192, 534. 

B14. Billing, B. H., Williams, R., and Richards, T. G., Defects in hepatic transport of bilirubin in congenital hyperbilirubinaemia an analysis of plasma bilirubin disappearance curves. Clin. Sci. 27, 245-257 (1964). 

Boyer JL, Graf J, and Meier PJ. Hepatic transport systems regulating pH, cell volume, and bile secretion. Ann Rev Physiol 1992 54 415-438. 

The hepatic transport of bilirubin from plasma to bile involves three independent, but related mechanisms, i.e., uptake, conjugation, and... 

Meier PJ, Boyer JL. Preparation of basolateral (sinusoidal) and canahcular plasma membrane vesicles for the study of hepatic transport processes. Methods Enzymol 1990 192 534-545. 

Moffit JS, Aleksunes LM, Maher JM, et al. Induction of hepatic transporters multidrug resistance-associated proteins (Mrp) 3 and 4 by clofibrate is regulated by peroxisome proliferator-activated receptor alpha. J Pharmacol Exp Ther 2006 317 537-545. 

Runnegar, M.T., Bemdt, N., Kaplowitz, N. (1995). Microcystin uptake and inhibition of protein phosphatases effects of chemoprotectants and self-inhibition in relation to known hepatic transporters. Toxicol. Appl. Pharmacol. 134 264-72. 

Klaassen, C.D., Slitt, A.L. (2005). Regulation of hepatic transporters by xenobiotic receptors. Curr. Drug. Metab. 6 309-28. 

Yoon, YJ., Hagey, L.R., Hofmann, AJ ., Gurantz, D., Michelotti, E.L., Steinbach, J. H. Effect of side-chain shortening on the physiologic properties of bile acids Hepatic transport and effect on bihary secretion of 23-nor-ursodeoxycholate in rodents. Gastroenterology 1986 90 837-852... 

Kullak-Ublick, G.A., Stieger, B., Hagenbuch, B., Meier, P.J. Hepatic transport of bile salts. Semin. Liver Dis. 2000 20 273—292... 

Forker, E.L. Luxon, B. Hepatic transport kinetics and plasma disappearance curves distributed modeling versus conventional approach. Am. J. Physiol. 1978, 235, E648-E660. 

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