{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,9]],"date-time":"2026-03-09T11:36:31Z","timestamp":1773056191459,"version":"3.50.1"},"reference-count":17,"publisher":"MDPI AG","issue":"2","license":[{"start":{"date-parts":[[2023,2,2]],"date-time":"2023-02-02T00:00:00Z","timestamp":1675296000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Grants-in-Aid for Scientific Research from the Japan Society for the Promotion of Science","award":["21H02865"],"award-info":[{"award-number":["21H02865"]}]},{"name":"Grants-in-Aid for Scientific Research from the Japan Society for the Promotion of Science","award":["22K19504"],"award-info":[{"award-number":["22K19504"]}]},{"name":"Grants-in-Aid for Scientific Research from the Japan Society for the Promotion of Science","award":["22H03016"],"award-info":[{"award-number":["22H03016"]}]},{"name":"The Network-type Joint Usage\/Research Center for Radiation Disaster Medical Science","award":["21H02865"],"award-info":[{"award-number":["21H02865"]}]},{"name":"The Network-type Joint Usage\/Research Center for Radiation Disaster Medical Science","award":["22K19504"],"award-info":[{"award-number":["22K19504"]}]},{"name":"The Network-type Joint Usage\/Research Center for Radiation Disaster Medical Science","award":["22H03016"],"award-info":[{"award-number":["22H03016"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>We evaluated the whole-body distribution of orally-administered radioiodine-125 labeled acetaminophen (125I-AP) to estimate gastrointestinal absorption of anionic drugs. 125I-AP was added to human embryonic kidney (HEK)293 and Flp293 cells expressing human organic anion transporting polypeptide (OATP)1B1\/3, OATP2B1, organic anion transporter (OAT)1\/2\/3, or carnitine\/organic cation transporter (OCTN)2, with and without bromosulfalein (OATP and multidrug resistance-associated protein (MRP) inhibitor) and probenecid (OAT and MRP inhibitor). The biological distribution in mice was determined by oral administration of 125I-AP with and without bromosulfalein and by intravenous administration of 125I-AP. The uptake of 125I-AP was significantly higher in HEK293\/OATP1B1, OATP1B3, OATP2B1, OAT1, and OAT2 cells than that in mock cells. Bromosulfalein and probenecid inhibited OATP- and OAT-mediated uptake, respectively. Moreover, 125I-AP was easily excreted in the urine when administered intravenously. The accumulation of 125I-AP was significantly lower in the blood and urinary bladder of mice receiving oral administration of both 125I-AP and bromosulfalein than those receiving only 125I-AP, but significantly higher in the small intestine due to inhibition of OATPs and\/or MRPs. This study indicates that whole-body distribution after oral 125I-AP administration can be used to estimate gastrointestinal absorption in the small intestine via OATPs, OATs, and\/or MRPs by measuring radioactivity in the urinary bladder.<\/jats:p>","DOI":"10.3390\/pharmaceutics15020497","type":"journal-article","created":{"date-parts":[[2023,2,2]],"date-time":"2023-02-02T03:24:49Z","timestamp":1675308289000},"page":"497","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["Biological Distribution after Oral Administration of Radioiodine-Labeled Acetaminophen to Estimate Gastrointestinal Absorption Function via OATPs, OATs, and\/or MRPs"],"prefix":"10.3390","volume":"15","author":[{"given":"Kakeru","family":"Sato","sequence":"first","affiliation":[{"name":"Division of Health Sciences, Graduate School of Medical Sciences, Kanazawa University, 5-11-80 Kodatsuno, Kanazawa 920-0942, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Asuka","family":"Mizutani","sequence":"additional","affiliation":[{"name":"Faculty of Health Sciences, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, 5-11-80 Kodatsuno, Kanazawa 920-0942, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yuka","family":"Muranaka","sequence":"additional","affiliation":[{"name":"Division of Health Sciences, Graduate School of Medical Sciences, Kanazawa University, 5-11-80 Kodatsuno, Kanazawa 920-0942, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jianwei","family":"Yao","sequence":"additional","affiliation":[{"name":"Division of Health Sciences, Graduate School of Medical Sciences, Kanazawa University, 5-11-80 Kodatsuno, Kanazawa 920-0942, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5172-2626","authenticated-orcid":false,"given":"Masato","family":"Kobayashi","sequence":"additional","affiliation":[{"name":"Faculty of Health Sciences, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, 5-11-80 Kodatsuno, Kanazawa 920-0942, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3396-1145","authenticated-orcid":false,"given":"Kana","family":"Yamazaki","sequence":"additional","affiliation":[{"name":"Department of Molecular Imaging and Theranostics, Institute for Quantum Medical Science, Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage 263-8555, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2096-4611","authenticated-orcid":false,"given":"Ryuichi","family":"Nishii","sequence":"additional","affiliation":[{"name":"Department of Molecular Imaging and Theranostics, Institute for Quantum Medical Science, Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage 263-8555, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4919-7639","authenticated-orcid":false,"given":"Kodai","family":"Nishi","sequence":"additional","affiliation":[{"name":"Department of Radioisotope Medicine, Atomic Bomb Disease Institute, Nagasaki University, 1-12-4 Sakamoto, Nagasaki 852-8523, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6561-7138","authenticated-orcid":false,"given":"Takeo","family":"Nakanishi","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy, Takasaki University of Health and Welfare, 60 Nakaorui-machi, Takasaki 370-0033, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ikumi","family":"Tamai","sequence":"additional","affiliation":[{"name":"Faculty of Pharmaceutical Sciences, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kakuma, Kanazawa 920-1192, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Keiichi","family":"Kawai","sequence":"additional","affiliation":[{"name":"Faculty of Health Sciences, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, 5-11-80 Kodatsuno, Kanazawa 920-0942, Japan"},{"name":"Biomedical Imaging Research Center, University of Fukui, 23-3 Matsuokashimoaizuki, Eiheiji 910-1193, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2023,2,2]]},"reference":[{"key":"ref_1","first-page":"241","article-title":"Drug transporters as targets for cancer chemotherapy","volume":"4","author":"Nakanishi","year":"2007","journal-title":"Cancer Genom. 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