Evidence map›Paper›PMID 32483763›Full record

ArticlePharmaceutical research2020

Investigation of Fluorescent Substrates and Substrate-Dependent Interactions of a Drug Transporter Organic Anion Transporting Polypeptide 2B1 (OATP2B1).

Tatsuya Kawasaki, Yuichi Shiozaki, Naoki Nomura, Kumi Kawai, Yuichi Uwai, Tomohiro Nabekura

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Article in Pharmaceutical research, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

2 citing papers in PubMed.

  1. Review
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors.

Tatsuya KawasakiDepartment of Pharmaceutics, School of Pharmacy, Aichi Gakuin University, 1-100 Kusumoto, Chikusa-ku, Nagoya, 464-8650, Japan.
Yuichi ShiozakiDepartment of Pharmaceutics, School of Pharmacy, Aichi Gakuin University, 1-100 Kusumoto, Chikusa-ku, Nagoya, 464-8650, Japan.
Naoki NomuraDepartment of Pharmaceutics, School of Pharmacy, Aichi Gakuin University, 1-100 Kusumoto, Chikusa-ku, Nagoya, 464-8650, Japan.
Kumi KawaiDepartment of Pharmaceutics, School of Pharmacy, Aichi Gakuin University, 1-100 Kusumoto, Chikusa-ku, Nagoya, 464-8650, Japan.
Yuichi UwaiDepartment of Pharmaceutics, School of Pharmacy, Aichi Gakuin University, 1-100 Kusumoto, Chikusa-ku, Nagoya, 464-8650, Japan.
Tomohiro NabekuraDepartment of Pharmaceutics, School of Pharmacy, Aichi Gakuin University, 1-100 Kusumoto, Chikusa-ku, Nagoya, 464-8650, Japan. nabekura@dpc.agu.ac.jp.ORCID http://orcid.org/0000-0002-7139-2270

Funding

Furukawa Academic Research Promotion Fund H30FurukawaB2
6 · The paper itself

Abstract

purposeIn this study, we investigated organic anion transporting polypeptide 2B1 (OATP2B1)-mediated uptake of fluorescent anions to better identify fluorescent substrates for in vitro OATP2B1 assays. The OATP2B1 is involved in the intestinal absorption and one of the pharmacokinetic determinants of orally administered drugs.

methodsA microplate reader was used to determine the cellular accumulation of the fluorescent compounds into the OATP2B1 or the empty vector-transfected HEK293 cells.

resultsTwo types of derivatives were found to be OATP2B1 substrates: heavy halogenated derivatives, such as 4',5'-dibromofluorescein (DBF), and carboxylated derivatives, such as 5-carboxyfluorescein (5-CF). The DBF and 5-CF were transported in a time and concentration-dependent manner. The DBF was transported at a broad pH (pH 6.5-8.0) while 5-CF was transported at an acidic pH (pH 5.5-6.5). The K

conclusionWe found two fluorescein analogs, DBF and 5-CF as the OATP2B1 substrates that exhibited substrate-dependent interactions.

Indexed as

Biological TransportDrug InteractionsFluorescent DyesHEK293 CellsHumansIntestinal AbsorptionOrganic Anion TransportersFluorescent DyesOrganic Anion Transportersdrug−drug interaction (DDI)fluorescent substratefood–drug interaction (FDI)inhibition assayorganic anion transporting polypeptide 2B1 (OATP2B1)

Identifiers

PMID32483763

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.