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Inhibition of the Hepatic Uptake of 99mTc-Tetrofosmin Using an Organic Cation Transporter Blocker
http://hdl.handle.net/10069/00041037
http://hdl.handle.net/10069/00041037549c7c06-814d-4e72-a2a8-76d9cf894c79
名前 / ファイル | ライセンス | アクション |
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Pharmaceutics13_1073.pdf (2.0 MB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2021-11-18 | |||||
タイトル | ||||||
タイトル | Inhibition of the Hepatic Uptake of 99mTc-Tetrofosmin Using an Organic Cation Transporter Blocker | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | 99mTc-tetrofosmin | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | small-animal SPECT/CT | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | hepatic uptake | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | transport mechanism | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | OCT1 | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
著者 |
Nishi, Kodai
× Nishi, Kodai× Kobayashi, Masato× Kikuchi, Minori× Mizutani, Asuka× Muranaka, Yuka× Tamai, Ikumi× Kawai, Keiichi× Kudo, Takashi |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | The accumulation of high levels of 99mTc-tetrofosmin (99mTc-TF) in the hepatobiliary system can lead to imaging artifacts and interference with diagnosis. The present study investigated the transport mechanisms of 99mTc-TF and attempted to apply competitive inhibition using a specific inhibitor to reduce 99mTc-TF hepatic accumulation. In this in vitro study, 99mTc-TF was incubated in HEK293 cells expressing human organic anion transporting polypeptide 1B1 (OATP1B1), OATP1B3, OATP2B1, organic anion transporter 2 (OAT2), organic cation transporter 1 (OCT1), OCT2, and Na+-taurocholate cotransporting polypeptide with or without each specific inhibitor to evaluate the contribution of each transporter to 99mTc-TF transportation. In vivo studies, dynamic planar imaging, and single photon emission computed tomography (SPECT) experiments with rats were performed to observe alterations to 99mTc-TF pharmacokinetics using cimetidine (CMT) as an OCT1 inhibitor. Time–activity curves in the liver and heart were acquired from dynamic data, and the 99mTc-TF uptake ratio was calculated from SPECT. From the in vitro study, 99mTc-TF was found to be transported by OCT1 and OCT2. When CMT-preloaded rats and control rats were compared, the hepatic accumulation of the 99mTc-TF was reduced, and the time to peak heart count shifted to an earlier stage. The hepatic accumulation of 99mTc-TF was markedly suppressed, and the heart-to-liver ratio increased 1.6-fold. The pharmacokinetics of 99mTc-TF were greatly changed by OCT1 inhibitor. Even in humans, the administration of OCT1 inhibitor before cardiac SPECT examination may reduce 99mTc-TF hepatic accumulation and contribute to the suppression of artifacts and the improvement of SPECT image quality. | |||||
書誌情報 |
Pharmaceutics 巻 13, 号 7, p. 1073, 発行日 2021-07-13 |
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出版者 | ||||||
出版者 | MDPI | |||||
EISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 1999-4923 | |||||
DOI | ||||||
関連タイプ | isIdenticalTo | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.3390/pharmaceutics13071073 | |||||
権利 | ||||||
権利情報 | © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). | |||||
著者版フラグ | ||||||
出版タイプ | VoR | |||||
出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||
引用 | ||||||
内容記述タイプ | Other | |||||
内容記述 | Pharmaceutics, 13(7), art. no. 1073; 2021 |