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Radiosynthesis and evaluation of [11C]BU99008 with ultra-high specific activity as a PET ligand for imaging I2-imidazoline receptors.
https://repo.qst.go.jp/records/71725
https://repo.qst.go.jp/records/71725ddc388e8-4985-4794-92d1-0d2cc73bddcb
| 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 | Radiosynthesis and evaluation of [11C]BU99008 with ultra-high specific activity as a PET ligand for imaging 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_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× Shimoda, Yoko× Yui, Joji× Fujinaga, Masayuki× Yamasaki, Tomoteru× Hatori, Akiko× Xie, Lin× Zhang, Yiding× Kumata, Katsushi× Ogawa, Masanao× Yusuke, Kurihara× Nengaki, Nobuki× Wakizaka, Hidekatsu× Zhang, Ming-Rong× 河村 和紀× 下田 陽子× 由井 譲二× 藤永 雅之× 山崎 友照× 羽鳥 晶子× 謝 琳× 張 一鼎× 熊田 勝志× 小川 政直× 栗原 雄祐× 念垣 信樹× 脇坂 秀克× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Objectives: The I2-imidazoline receptor (I2R) is involved in various neuropsychiatric disorders, but the these function are unknown. In addition, selective I2R ligands promote food intake and may therefore alter eating behavior. The carrier dose of PET ligand may modify both binding and pharmacokinetics in small animal imaging studies. Ultra-high specific activity (SA) is a useful tool to investigate a receptor with low density and small region in the brain [1]. We recently reported that [11C]FTIMD with ultra-high SA (mean 4470 GBq/μmol) for imaging of I2Rs showed higher specific-binding than [11C]FTIMD with conventional SA (about 100 GBq/μmol) in the hypothalamus, which is highly expressed I2Rs [2]. More recently, Kealey et al. developed [11C]BU99008 as a more potent PET ligand for I2R imaging [3]. [11C]BU99008 displayed a relatively high brain penetration and specific binding in the porcine and rhesus brain [3,4]. In this study, to image I2Rs in extremely small region such as hypothalamus, we synthesized and evaluated [11C]BU99008 with ultra-high SA as a PET ligand. Methods: [11C]BU99008 was prepared by methylation of the BU-precursor and [11C]methyl iodide. In case of ultrahigh SA, [11C]methyl iodide was produced by iodination of [11C]methane using the single-pass method [1,2]. Biodistribution and brain PET studies were conducted in rats. Results: [11C]BU99008 with conventional and ultra-high SA were successfully synthesized in the range of SA at 55∼220 [n = 8] and 5400∼16600 [n = 7] GBq/μmol at the end of synthesis, respectivery, yielding a radioactivity suitable for injection. In PET studies, the radioactivity after injection of [11C]BU99008 with conventional or ultra-high SA was highly accumulated in the hypothalamus. Pretreatment with BU224 (an high affinity I2R ligand; 1 mg/kg) significantly decreased the radioactivity (AUC30-60 min) of conventional or ultra-high SA in the hypothalamus to 76% or 86% of the correspoding control radioactivity (AUC30-60 min), respectively. Conclusions: [11C]BU99008 with ultra-high SA showed high specific binding in rat brain. PET study using [11 C]BU99008 with ultra-high SA would contribute to the detection of I2Rs expression in small regions or with small change. References: [1] Noguchi J, et al (2003), Nucl Med Biol, 30, 335-43. [2] Kawamura K, et al (2012), Nucl Med Biol, 39, 199-206. [3] Kealey S, et al (2013), J Nucl Med, 54, 139-44. [4] Parker CA, et al (2014), J Nucl Med, 55, 838-44. (No Image Selected) |
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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 | 2015-05-27 | |||||
| 日付タイプ | Issued | |||||
