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Synthesis and evaluation of an 18F-labeled imidazoline I2 receptor ligand as a PET probe
https://repo.qst.go.jp/records/71531
https://repo.qst.go.jp/records/71531426e9349-37cd-4e50-aa29-4ab5af1b1aee
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2014-10-28 | |||||
| タイトル | ||||||
| タイトル | Synthesis and evaluation of an 18F-labeled imidazoline I2 receptor ligand as a PET probe | |||||
| 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× Yamasaki, Tomoteru× Shimoda, Yoko× Kumata, Katsushi× Fujinaga, Masayuki× Yui, Joji× Xie, Lin× Hatori, Akiko× Wakizaka, Hidekatsu× Yusuke, Kurihara× Ogawa, Masanao× Nengaki, Nobuki× Zhang, Ming-Rong× 河村 和紀× 山崎 友照× 下田 陽子× 熊田 勝志× 藤永 雅之× 由井 譲二× 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 | Aim: The density of the imidazoline I2 receptors (I2Rs) has been shown to change in psychiatric conditions such as depression and addiction, along with neurodegenerative disorders such as Alzheimer’s disease and Huntington’s chorea. However, functions associated with I2Rs are not known. Previously we developed a new PET probe (11C-FTIMD) for imaging of I2Rs (NMB 2010;37:625), although the specific binding of this probe appears to be low. Recently, Kealey et al. developed another new PET probe (11C-BU99008) which has high selective affinity for I2R and relatively high specific binding in brain (JNM 2013;54:139). Also, Tyacke et al. synthesized a fluorine analog of BU99008 (BU99018, Ki for I2Rs = 2.6 nM, Synapse 2012;66:542). However, they had not labeled the fluro compound, because this compound had poor stability in methanol and slowly conversed to a cyclized product. In this study, we synthesized 18F-BU99018 (18F-FEBU), and evaluated its stability and in vivo potentials as an imaging agent for I2Rs. Methods: 18F-FEBU was synthesized by the reaction of its precursor and 18F-fluoroethyl triflate. Biodistribution in mice was performed and PET studies were conducted in rat brains. Results: 18F-FEBU was successfully synthesized with a suitable radioactivity for the injection. The radiochemical yields based on 18F- was 16-21%. The specific activity at end of synthesis (EOS) was 62–89 TBq/mmol. The radiochemical purity of 18F-FEBU injection was over 95% at EOS, and remained unchanged at 1 hour after EOS. In mice, the brain uptake was relatively high and gradually decreased after initial phase. In the blocking study by co-injection of the high-affinity I2R ligand BU224 (1 mg/kg), the brain uptake was significantly decreased at 30 min after injection (56 % of control). In the PET studies, the radioactivity was accumulated in rat brain regions existing I2Rs in control. By pretreatment with BU224 (1 mg/kg), the radioactivity accumulated in the rat brains from 60 to 90 min after injection was significantly decreased as compared with control (23% of control). Conclusions: 18F-FEBU showed the suitable stability as a PET probe and relatively high specific binding to I2Rs in rats and mice. PET study using 18F-FEBU could be used to elucidate the pharmacological role of I2R in the brain. \n(Abstracts should not exceed 400 words (excluding title and authors) and should be well structured stating the aim, materials and methods, results and conclusion of your chosen topic.) |
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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 | EANM Congress 2014 | |||||
| 発表年月日 | ||||||
| 日付 | 2014-10-19 | |||||
| 日付タイプ | Issued | |||||
