The effect of organic solvents on the in vitro transport activity of three OATP isoforms

The uptake activities of OATPs were reduced by methanol and ethanol in a concentration-dependent manner, with IC<sub>20</sub> values of 2.4-3.4 % and 0.51-3.8 % respectively. In contrast, DMSO did not affect the OATP2B1-mediated uptake at the maximum concentration (10 %) of DMSO whereas it exhibited concentration-dependent inhibition for OATP1B1 and 1A2 with IC<sub>20</sub> values of approximately 3 % and 0.7 %, respectively. This study provides useful information regarding experimental conditions for evaluating OATPs activity in vitro.

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Publication Details

Journal
Toxicology in Vitro
Published
2025-03-30
DOI
https://doi.org/10.1016/j.tiv.2025.106059
Citations
1
Primary Topic
Drug Transport and Resistance Mechanisms
Type
article
Field-Weighted Citation Impact
1.05
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article

The effect of organic solvents on the in vitro transport activity of three OATP isoforms

Rie Takahashi, Kazunari Tsujii, Hisakazu Ohtani, Rina Saito et al.
1 citations
Toxicology in Vitro
Drug Transport and Resistance Mechanisms
1.05
article

The effect of organic solvents on the in vitro transport activity of three OATP isoforms

Rie Takahashi, Kazunari Tsujii, Hisakazu Ohtani, Rina Saito, Ayuko Imaoka, Takeshi Akiyoshi, Hiroki Kataoka
article en
1 citations

Abstract

The uptake activities of OATPs were reduced by methanol and ethanol in a concentration-dependent manner, with IC<sub>20</sub> values of 2.4-3.4 % and 0.51-3.8 % respectively. In contrast, DMSO did not affect the OATP2B1-mediated uptake at the maximum concentration (10 %) of DMSO whereas it exhibited concentration-dependent inhibition for OATP1B1 and 1A2 with IC<sub>20</sub> values of approximately 3 % and 0.7 %, respectively. This study provides useful information regarding experimental conditions for evaluating OATPs activity in vitro.

Toxicology in VitroVol. 107
Keio University (JP), Keio University Hospital (JP)
Openalex Percentile: Top 24%
Drug Transport and Resistance Mechanisms
1.05
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