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Radiosynthesis of [thiocarbonyl-11C]disulfiram and its first PET study in mice
https://repo.qst.go.jp/records/79415
https://repo.qst.go.jp/records/79415633dc68e-fd25-427d-91c3-e0f19f81d64e
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2020-03-13 | |||||
| タイトル | ||||||
| タイトル | Radiosynthesis of [thiocarbonyl-11C]disulfiram and its first PET study in mice | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 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 | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Ishii, Hideki
× Ishii, Hideki× Yamasaki, Tomoteru× Yui, Joji× Zhang, Yiding× Hanyu, Masayuki× Ogawa, Masanao× Nengaki, Nobuki× Tsuji, Atsushi× Terashima, Yuya× Matsushima, Kouji× Ming-Rong, Zhang× Hideki, Ishii× Tomoteru, Yamasaki× Joji, Yui× Zhang, Yiding× Masayuki, Hanyu× Masanao, Ogawa× Nobuki, Nengaki× Atsushi, Tsuji× Zhang, Ming-Rong |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | [Thiocarbonyl-11C]disulfiram ([11C]DSF) was synthesized via iodine oxidation of [11C]diethylcarbamodithioic acid ([11C]DETC), which was prepared from [11C]carbon disulfide and diethylamine. The decay-corrected isolated radiochemical yield (RCY) of [11C]DSF was greatly affected by the addition of unlabeled carbon disulfide. In the presence of carbon disulfide, the RCY was increased up to 22% with low molar activity (Am, 0.27 GBq/μmol). On the other hand, [11C]DSF was obtained in 0.4% RCY with a high Am value (95 GBq/μmol) in the absence of carbon disulfide. The radiochemical purity of [11C]DSF was always >98%. The first PET study on [11C]DSF was performed in mice. A high uptake of radioactivity was observed in the liver, kidneys, and gallbladder. The uptake level and distribution pattern in mice were not significantly affected by the Am value of the [11C]DSF sample used. In vivo metabolite analysis showed the rapid decomposition of [11C]DSF in mouse plasma. | |||||
| 書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 30, 号 6, p. 126998, 発行日 2020-01 |
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| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0960-894X | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.bmcl.2020.126998 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://www.sciencedirect.com/science/article/pii/S0960894X20300615?via%3Dihub | |||||
