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Titolo:
Canalicular membrane transport is primarily responsible for the differencein hepatobiliary excretion of triethylmethylammonium and tributylmethylammonium in rats
Autore:
Han, YH; Chung, SJ; Shim, CK;
Indirizzi:
Seoul Natl Univ, Coll Pharm, Dept Pharmaceut, Kwanak Gu, Seoul 151742, South Korea Seoul Natl Univ Seoul South Korea 151742 k Gu, Seoul 151742, South Korea
Titolo Testata:
DRUG METABOLISM AND DISPOSITION
fascicolo: 8, volume: 27, anno: 1999,
pagine: 872 - 879
SICI:
0090-9556(199908)27:8<872:CMTIPR>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
ORGANIC CATION TRANSPORTER; BILIARY-EXCRETION; HEPATIC-UPTAKE; KINETIC-ANALYSIS; UPTAKE SYSTEM; LIVER; VESICLES; HEPATOCYTES; DRUGS; PHARMACOKINETICS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Chung, SJ Seoul Natl Univ, Coll Pharm, Dept Pharmaceut, Kwanak Gu, San 56-1 Shinlim Dong, Seoul 151742, South Korea Seoul Natl Univ San 56-1 Shinlim Dong Seoul South Korea 151742
Citazione:
Y.H. Han et al., "Canalicular membrane transport is primarily responsible for the differencein hepatobiliary excretion of triethylmethylammonium and tributylmethylammonium in rats", DRUG META D, 27(8), 1999, pp. 872-879

Abstract

Two structurally similar quaternary ammonium compounds, triethylmethylammonium (TEMA, M-r 116) and tributylmethylammonium (TBuMA, M-r 200) were used as model compounds to identify the unit process of hepatobiliary excretion that is responsible for markedly different biliary excretion of organic cations (OCs). Cumulative biliary excretion (in percentage of dose; i.v., 12 mu mol/kg) was 0.17 for TEMA and 34.5 for TBuMA. In vivo uptake clearance into the liver was 0.686 +/- 0.020 ml/min for TEMA and 0.421 +/- 0.028 ml/minfor TBuMA. When the uptake clearance was examined in an isolated hepatocyte system, comparable clearance between TEMA and TBuMA was obtained, consistent with the in vivo result. These observations suggest that uptake into the liver is not the major determinant for the difference in biliary excretion of the OCs. Co-administration of colchicine, an inhibitor of microtubule formation, had no effect on biliary excretion of the model compounds, and the primary site of subcellular distribution of the OCs appears to be the cytosol, suggesting that intracellular movement does not play a major role inthe markedly different biliary excretion of the OCs. In contrast, in vivo excretion clearance across the canalicular membrane for TBuMA was 180-fold greater than that for TEMA, and in vitro efflux clearance of TBuMA was smaller than that of TEMA (p < .01), indicative of involvement of these processes in the markedly different biliary excretion of the OCs. Therefore, thesedata indicate that canalicular transport is primarily responsible for the markedly different biliary excretion of TEMA and TBuMA.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/07/20 alle ore 19:52:16