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Titolo:
Polyspecific organic anion transporting polypeptides mediate hepatic uptake of amphipathic type II organic cations
Autore:
Van Montfoort, JE; Hagenbuch, B; Fattinger, KE; Muller, M; Groothuis, GMM; Meijer, DKF; Meier, PJ;
Indirizzi:
Univ Zurich Hosp, Dept Med, Div Clin Pharmacol & Toxicol, CH-8091 Zurich, Switzerland Univ Zurich Hosp Zurich Switzerland CH-8091 CH-8091 Zurich, Switzerland Univ Groningen, Inst Drug Explorat, Liver Res Ctr, Groningen, Netherlands Univ Groningen Groningen Netherlands er Res Ctr, Groningen, Netherlands
Titolo Testata:
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
fascicolo: 1, volume: 291, anno: 1999,
pagine: 147 - 152
SICI:
0022-3565(199910)291:1<147:POATPM>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
FUNCTIONAL-CHARACTERIZATION; HUMAN LIVER; UPTAKE SYSTEMS; SUBSTRATE-SPECIFICITY; RAT-KIDNEY; BILE-ACID; CLONING; EXPRESSION; IDENTIFICATION; TAUROCHOLATE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
38
Recensione:
Indirizzi per estratti:
Indirizzo: Meier, PJ Univ Zurich Hosp, Dept Med, Div Clin Pharmacol & Toxicol, CH-8091 Zurich, Switzerland Univ Zurich Hosp Zurich Switzerland CH-8091 urich, Switzerland
Citazione:
J.E. Van Montfoort et al., "Polyspecific organic anion transporting polypeptides mediate hepatic uptake of amphipathic type II organic cations", J PHARM EXP, 291(1), 1999, pp. 147-152

Abstract

Hepatic uptake of albumin-bound amphipathic organic cations has been suggested to be mediated by multispecific bile salt and organic anion transport systems. Therefore, we investigated whether the recently cloned rat organicanion transporting polypeptides 1 and 2 as well as the human organic aniontransporting polypeptide might be involved in the hepatocellular uptake ofbulky type II organic cations. In cRNA-injected Xenopus laevis oocytes, all three carriers mediated uptake of the known type II model compounds N-(4,4-azo-n-pentyl)-21-deoxy- ajmalinium and rocuronium, whereas the newly synthesized type II model compounds N- methyl-quinine and N-methyl-quinidine were transported only by the human organic anion transporting polypeptide. This carrier-mediated uptake of N-methyl-quinine and N-methyl-quinidine was sodium-independent and saturable with apparent K-m values of similar to 5 and similar to 26 mu M, respectively. In contrast to bulky type II organic cations, more hydrophilic type I organic cations such as tributylmethylammonium and choline were not transported by any of the organic anion transporting polypeptides. These findings demonstrate that organic anion transporting polypeptides can also mediate hepatocellular uptake of type II organic cations, whereas uptake of small and more water-soluble type I cations is mediated by different transport systems such as the organic cation transporters.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/09/20 alle ore 08:05:18