Drug transporter - enzyme crossroads: Does OATP2B1 shape Cyp3a-driven midazolam metabolism in rats?

OATP2B1, encoded by SLCO2B1, is an uptake transporter in liver. Humanized SLCO2B1+/+ rats showed increased hepatic Cyp3a1 expression compared to rSlco2b1−/− rats. To assess the impact of humanization on Cyp3a activity, we conducted a phenotyping study applying midazolam in SLCO2B1+/+ and rSlco2b1−/-...

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Bibliographic Details
Published in:	European journal of pharmaceutical sciences Vol. 215; p. 107343
Main Authors:	Paloumpis, Nikolaos, Rysz, Marta, Bianchi, Noemi, Seibert, Isabell, Kinzi, Jonny, Schäfer, Anima M., Brecht, Karin, Ricklin, Daniel, Meyer zu Schwabedissen, Henriette E.
Format:	Journal Article
Language:	English
Published:	Netherlands Elsevier B.V 01.12.2025
Subjects:	Animals Cyp3a1 Cyp3a2 Cytochrome P-450 CYP3A - genetics Cytochrome P-450 CYP3A - metabolism Humans Liver - metabolism Male Microsomes, Liver - metabolism Midazolam Midazolam - analogs & derivatives Midazolam - blood Midazolam - metabolism Midazolam - pharmacokinetics OATP2B1 Organic Anion Transporters - genetics Organic Anion Transporters - metabolism Rat model Rats Rats, Sprague-Dawley Cyp3a1 Rat model Midazolam Cyp3a2 OATP2B1
ISSN:	0928-0987, 1879-0720, 1879-0720
Online Access:	Get full text
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