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One-pot radiosynthesis of [18F]FEDAC as a clinically applicable PET ligand for imaging TSPO.
https://repo.qst.go.jp/records/71724
https://repo.qst.go.jp/records/7172463c075a1-d1d8-44e8-8796-64f35b799c4a
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2015-06-15 | |||||
| タイトル | ||||||
| タイトル | One-pot radiosynthesis of [18F]FEDAC as a clinically applicable PET ligand for imaging TSPO. | |||||
| 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 |
Kawamura, Kazunori
× Kawamura, Kazunori× Kumata, Katsushi× Furutsuka, Kenji× Shiomi, Satoshi× Fujishiro, Tomoya× Ryuji, Watanabe× Takei, Makoto× Hashimoto, Hiroki× Ito, Takehito× Ogawa, Masanao× Igarashi, Nobuyuki× Muto, Masatoshi× Nengaki, Nobuki× Nemoto, Kazuyoshi× Zhang, Ming-Rong× 河村 和紀× 熊田 勝志× 古塚 賢士× 潮見 聡× 藤代 智也× 渡辺 竜二× 武井 誠× 橋本 裕輝× 伊藤 岳人× 小川 政直× 五十嵐 延行× 武藤 正敏× 念垣 信樹× 根本 和義× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Objectives: Translocator protein (18 kDa) (TSPO), a nucleus-encoded mitochondrial target transmembrane protein, has been indicated as an active participant in the modulation of mitochondrial function. PET using radiolabeled TSPO probes has allowed non-invasive and reliable investigation of TSPO in neuropathological damages of experimental animals and humans. Many PET probes for TSPO imaging have been developed. Among them, [18F]FEDAC has potent binding affinity and selectivity for TSPO [1], high signal to neuroinflammation [2], and high sensitivity and specificity for detection of fatty liver diseases progression [3]. We had previously synthesized [18F]FEDAC by reaction of desmethyl-precursor with [18F]fluoroethyl bromide at two steps using a modified 18F-labelling synthesizer developed in our institute [1-3]. In this study, we simplified the synthesis of [18F]FEDAC by direct 18F-fluorination using a typical 18F-labelling synthesizer to transfer the preparation of [18F]FEDAC to other institutes toward multicenter clinical study. Methods: Tosylate-precursor for radiosynthesis of [18F]FEDAC was synthesized according to the procedures, as shown in Fig. 1. [18F]FEDAC was prepared by heating the tosylate-precursor with 18F- in DMSO at 110 ⁰C for 10-15 min. Results: Tosylate-precursor of [18F]FEDAC was successfully synthesized from desmethyl-precursor. [18F]FEDAC was obtained with sufficient radioactivity and suitable quality for injection in clinical application. The synthesis of [18 F]FEDAC was reproduceble to achieve >740 MBq, >300 GBq/μmol and >97% of radiochemical purity within 70 min of an overall synthesis time. All other analytical results were in compliance with our in-house quality control and assurance specifications. Conclusions: We successfully synthesized [18F]FEDAC by fluorination of the tosylate-precursor with 18F- using onepot 18F-labelling synthesizer. This radioligand will be used in clinical study. References: [1] Yanamoto K, et al (2009), Bioorg Med Chem Lett, 19, 1707-10. [2] Yui J, et al (2010), J Nucl Med, 51, 1301-9. [3] Xie L, et al (2012), J Hepatol, 57, 1076-82. |
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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 | 21st International Symposium on Radiopharmaceutical Sciences | |||||
| 発表年月日 | ||||||
| 日付 | 2015-05-28 | |||||
| 日付タイプ | Issued | |||||
