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250307s2012 hu o 0|| Angol d |
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|a 1347-4367
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|a 10.2133/dmpk.DMPK-11-NT-068
|2 doi
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|a 1765884
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|a PPKE Publikáció Repozitórium
|b hun
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|a Angol
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|a Beéry Erzsébet
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|a ABCG2 modulates chlorothiazide permeability in vitro – characterization of the interaction
|h [elektronikus dokumentum] /
|c Beéry Erzsébet
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|c 2012
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|a 349-353
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|a DRUG METABOLISM AND PHARMACOKINETICS
|v 27 No. 3
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|a We are showing that chlorothiazide, a diuretic, is an ABCG2 substrate. It is a Biopharmaceutics Classification System/Biopharmaceutics Drug Distribution and Classification System (BCS/BDDCS) Class IV drug with low bioavailability. Therefore, we tested if chlorothiazide interacts with major apically located intestinal efflux transporters. Our data show that chlorothiazide is transported by ABCG2 with a Km value of 334.6 µM and does not interact with ABCB1 or ABCC2. The chlorothiazide–ABCG2 interaction results in a vectorial transport in MDCKII-BCRP and Caco-2 cells with efflux ratios of 36 and 8.1 respectively. Inhibition of ABCG2 in Caco-2 cells reduced the efflux ratio to 1.4, suggesting that ABCG2 plays a role in limiting chlorothiazide bioavailability in humans.
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|a Farmakológia és gyógyszerészet
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|a Narozsnikné Rajnai Zsuzsanna
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|a Abonyi Tibor
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|a Makai Ildikó
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|a Bánsághi Száva
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|a Erdő Franciska
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|a Sziráki István
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|a Herédi-Szabó Krisztina
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|a Kis Emese
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|a Jani Márton
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|a Márki-Zay János
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|a Tóth Gábor
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|a Krajcsi Péter
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|u https://publikacio.ppke.hu/id/eprint/2382/1/drug_metabolism2012.pdf
|z Dokumentum-elérés
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