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Radiosynthesis of [11C]disulfiram and its first in vivo PET studies
https://repo.qst.go.jp/records/72342
https://repo.qst.go.jp/records/72342a44b03d1-eac7-4ddc-8a0c-5e6440a8ca3a
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-05-25 | |||||
| タイトル | ||||||
| タイトル | Radiosynthesis of [11C]disulfiram and its first in vivo PET studies | |||||
| 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_c94f | |||||
| 資源タイプ | conference object | |||||
| 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× Yui, Joji× Zhang, Yiding× Yamasaki, Tomoteru× Hanyu, Masayuki× Ogawa, Masanao× Nengaki, Nobuki× Tsuji, Atsushi× Zhang, Ming-Rong× 石井 英樹× 由井 譲二× 張 一鼎× 山崎 友照× 破入 正行× 小川 政直× 念垣 信樹× 辻 厚至× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Objectives: Disulfiram (DSF) has been widely used to treat alcoholism for more than half a century and recent studies suggest that DSF may have potential therapeutic effect for several cancers. However, the detail reaction mechanism for the anti-cancer effect of DSF is still not clear. Therefore, the development of [11C]DSF and its in vivo and in vitro studies might be helpful for the understanding of the role of DSF. Here we present the first synthesis of [11C]DSF using [11C]carbon disulfide ([11C]CS2) as a labelling agent. Methods: [11C]DSF was synthesized via iodine (I2) oxidation of [11C]diethylcarbamodithioic acid ([11C]DETC), which was prepared by the reaction of [11C]CS2 and diethylamine in acetonitrile (MeCN) at room temperature (r.t.) Results: The (decay-corrected isolated) radiochemical yield (RCY) of [11C]DSF was greatly affected by the addition of non-radioactive carbon disulfide (CS2). In the presence of CS2, RCY was increased up to 22% with low molar radioactivity (0.27 GBq/mol). On the other hand, in the absence of CS2, [11C]DSF was obtained in 0.4% RCY with high molar radioactivity (95 GBq/mol). The radiochemical purities (determined by radio-HPLC analysis of the isolated product) of [11C]DSF were always greater than 98%. The first PET study of [11C]DSF was performed on mice. High uptake of radioactivity in the liver, kidney and gallbladder were observed and the metabolite analysis of mouse serum showed the rapid decomposition of [11C]DSF. Conclusions: [11C]DSF was successfully synthesized by the reaction of [11C]CS2 with diethylamine followed by I2 oxidation. Regardless of the molar radioactivity, PET studies of [11C]DSF showed similar uptake in mouse organ and rapid decomposition in serum. |
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| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | 22nd International symposium on radiopharmaceutical science (ISRS) | |||||
| 発表年月日 | ||||||
| 日付 | 2017-05-15 | |||||
| 日付タイプ | Issued | |||||
