WEKO3
アイテム
Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain
https://repo.qst.go.jp/records/47564
https://repo.qst.go.jp/records/47564398627de-5e2f-4f2c-a836-235c8bfceff0
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2016-10-12 | |||||
| タイトル | ||||||
| タイトル | Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain | |||||
| 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 |
Hanyu, Masayuki
× Hanyu, Masayuki× Kawamura, Kazunori× Takei, Makoto× Furutsuka, Kenji× Shiomi, Satoshi× Fujishiro, Tomoya× Ogawa, Masanao× Nengaki, Nobuki× Hashimoto, Hiroki× Fukumura, Toshimitsu× Zhang, Ming-Rong× 破入 正行× 河村 和紀× 武井 誠× 古塚 賢士× 潮見 聡× 藤代 智也× 小川 政直× 念垣 信樹× 橋本 裕輝× 福村 利光× 張 明栄 |
|||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Introduction: Recently, 6-[(1-cyclobutylpiperidin-4-yl)oxy]- 1-(6-[11C]methoxypyridin-3-yl)-3,4-dihydroquinolin-2(1H)-one ([11C]TASP457, [11C]2) has been developed as a novel PET ligand for histamine H3 receptors in brain. [11C]2 is potentially suitable for imaging H3 receptors in rat and monkey brains, which has motivated us to perform first-in-human study of [11C]2 for qualifying H3 receptors in human brain. In this paper, we report efficient radiosynthesis of [11C]2 to obtain sufficient radioactivity and high quality for clinical application. Methods: In manual synthesis, we optimized the reaction conditions of desmethyl precursor 2, which contains a 2-hydroxypyridine moiety, with [11C]MeI or [11C]MeOTf. After optimization, we performed automated synthesis and quality control of [11C]2. Results: Bubbling [11C]MeOTf into a heated mixture of precursor 1 and cesium carbonate in DMF at 100 °C for 90 sec produced [11C]2 with 7.9 ± 1.8 % (n = 78) of the radiochemical yields (decay-corrected, based on [11C]CO2). The specific activity of [11C]2 was 156 ± 52 GBq/mol (n = 78) at the end of synthesis. The total synthesis time was approximately 35 min from the end of bombardment. All the quality control results of [11C]2 were in compliance with our in-house quality control/assurance specifications. Conclusion: We radiosynthesized [11C]TASP457 ([11C]2) with sufficient amounts of radioactivity and high quality for clinical usefulness. This radioligand is being used for PET assessment of H3 receptors in human brain in our facility. |
|||||
| 書誌情報 |
Nuclear Medicine and Biology 巻 43, 号 11, p. 679-684, 発行日 2016-10 |
|||||
| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.nucmedbio.2016.08.004 | |||||
