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In vivo evaluation of a new 18F-labeled PET ligand, [18F]FEBU, for the imaging of I2-imidazoline receptors
https://repo.qst.go.jp/records/47076
https://repo.qst.go.jp/records/47076947d164b-5795-4efd-9666-b7fbe5f7b725
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2015-04-07 | |||||
| タイトル | ||||||
| タイトル | In vivo evaluation of a new 18F-labeled PET ligand, [18F]FEBU, for the imaging of I2-imidazoline receptors | |||||
| 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 |
Kawamura, Kazunori
× Kawamura, Kazunori× Shimoda, Yoko× Kumata, Katsushi× Fujinaga, Masayuki× Yui, Joji× Yamasaki, Tomoteru× Xie, Lin× Hatori, Akiko× Wakizaka, Hidekatsu× Yusuke, Kurihara× Ogawa, Masanao× Nengaki, Nobuki× Zhang, Ming-Rong× 河村 和紀× 下田 陽子× 熊田 勝志× 藤永 雅之× 由井 譲二× 山崎 友照× 謝 琳× 羽鳥 晶子× 脇坂 秀克× 栗原 雄祐× 小川 政直× 念垣 信樹× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Introduction: The functions of I2-imidazoline receptors (I2Rs) are unknown, but evidence exists for their involvement in various neuropsychiatric disorders. Although a few positron emission tomography (PET) I2R ligands have been developed, of which [11C]FTIMD and [11C]BU99008 were evaluated as PET I2R imaging ligands in monkeys, no human PET imaging study using an I2R-selective PET ligand has been conducted yet. Thus, we synthesized an 18F-labeled I2R-selective ligand (BU99018 or FEBU, Ki for I2Rs = 2.6 nM), and evaluated its application using rodents in PET imaging in vivo toward the development of a clinically-useful I2R PET imaging ligand. Methods: [18F]FEBU was synthesized by the reaction of its precursor and [18F]fluoroethyl bromide. A biodistribution and brain PET study were conducted in mice and rats, respectively. Results: [18F]FEBU was successfully synthesized, yielding a radioactivity suitable for injection (10.1 ± 5.3% at the end of the irradiation (n = 10) based on 18F-). The specific activity at end of synthesis (EOS) was 40-147 TBq/mmol (n = 10). The radiochemical purity was >99% at EOS and remained >99% for 90 min after EOS. In mice, brain uptake was relatively high. In the blocking study with the coinjection of the high-affinity I2R ligand BU224 (1 mg/kg b.w.), brain uptake was significantly decreased 30 min post-injection. In the PET studies, the radioactivity was highly accumulated in the I2R-rich hypothalamus. Pretreatment with BU224 (1 mg/kg b.w.) significantly decreased the radioactivity in the hypothalamus to 23% of that of the control from 60 to 90 min post-injection. Conclusion: [18F]FEBU was sufficiently stable as a PET ligand and had a relatively high specific binding affinity for I2Rs in rats and mice. |
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| 書誌情報 |
Nuclear Medicine and Biology 巻 42, 号 4, p. 406-412, 発行日 2015-04 |
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| 出版者 | ||||||
| 出版者 | Elsevier | |||||
