{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["10(3)"],"submitter":["Gilibili RR"],"pubmed_abstract":["Previously we reported that coproporphyrin-I (CP-I) is an optimal probe substrate for multidrug resistance-associated protein 2 (MRP2), and stimulation of MRP2-mediated transport is probe substrate-dependent. In the present investigation, we assessed if the in vitro stimulation is physiologically relevant. Similar to human MRP2 transport, CP-I was transported by rat Mrp2 in a typical Michaelis-Menten kinetics with apparent K<sub>m</sub> and V<sub>max</sub> values of 15 ± 6 µM and 161 ± 20 pmol/min/mg protein, respectively. In vivo Mrp2 functions were monitored by biliary and renal secretion of CP-I and its isomer CP-III, in bile-duct cannulated rats before and after treatment with mitoxantrone, progesterone, and verapamil. These compounds stimulated Mrp2-mediated CP-I transport in vitro. N"],"journal":["Pharmaceutics"],"pagination":["E125"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC6161027"],"repository":["biostudies-literature"],"pubmed_title":["In Vitro Stimulation of Multidrug Resistance-Associated Protein 2 Function Is Not Reproduced In Vivo in Rats."],"pmcid":["PMC6161027"],"pubmed_authors":["Lai Y","Kurawattimath V","Gilibili RR","Chatterjee S","Murali BV","Mariappan TT","Shen H"],"additional_accession":[]},"is_claimable":false,"name":"In Vitro Stimulation of Multidrug Resistance-Associated Protein 2 Function Is Not Reproduced In Vivo in Rats.","description":"Previously we reported that coproporphyrin-I (CP-I) is an optimal probe substrate for multidrug resistance-associated protein 2 (MRP2), and stimulation of MRP2-mediated transport is probe substrate-dependent. In the present investigation, we assessed if the in vitro stimulation is physiologically relevant. Similar to human MRP2 transport, CP-I was transported by rat Mrp2 in a typical Michaelis-Menten kinetics with apparent K<sub>m</sub> and V<sub>max</sub> values of 15 ± 6 µM and 161 ± 20 pmol/min/mg protein, respectively. In vivo Mrp2 functions were monitored by biliary and renal secretion of CP-I and its isomer CP-III, in bile-duct cannulated rats before and after treatment with mitoxantrone, progesterone, and verapamil. These compounds stimulated Mrp2-mediated CP-I transport in vitro. N","dates":{"release":"2018-01-01T00:00:00Z","publication":"2018 Aug","modification":"2026-06-14T05:18:02.263Z","creation":"2019-03-26T23:58:29Z"},"accession":"S-EPMC6161027","cross_references":{"pubmed":["30096834"],"doi":["10.3390/pharmaceutics10030125"]}}