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Synthesis and Evaluation of Novel Carbon-11 Labeled Oxopurine Analogues for Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Peripheral Organs
https://repo.qst.go.jp/records/46172
https://repo.qst.go.jp/records/4617285f214fa-ce73-4afd-8395-44d1035c3363
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2011-09-20 | |||||
| タイトル | ||||||
| タイトル | Synthesis and Evaluation of Novel Carbon-11 Labeled Oxopurine Analogues for Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Peripheral Organs | |||||
| 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 |
Kumata, Katsushi
× Kumata, Katsushi× Yui, Joji× Hatori, Akiko× Fujinaga, Masayuki× Yanamoto, Kazuhiko× Yamasaki, Tomoteru× Kawamura, Kazunori× Wakizaka, Hidekatsu× Nengaki, Nobuki× Yoshida, Yuichirou× Ogawa, Masanao× Fukumura, Toshimitsu× Zhang, Ming-Rong× 熊田 勝志× 由井 譲二× 羽鳥 晶子× 藤永 雅之× 柳本 和彦× 山崎 友照× 河村 和紀× 脇坂 秀克× 念垣 信樹× 吉田 勇一郎× 小川 政直× 福村 利光× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | To develop a PET ligand for imaging TSPO in peripheral organs, we designed three novel oxopurine analogues [11C]3a–c (LogD: 1.81–2.17) by introducing a pyridine ring in place of a benzene ring in the lead compound [11C]2 (LogD: 3.48). The desmethyl precursors 10 for radiosynthesis were synthesized by reacting glycine 7 with picolylamines 4, followed by hydrolysis and by Curtius rearrangement with diphenylphosphoryl azide. Methylation of 10a–c with methyl iodide produced unlabeled compounds 3a–c. The radiosynthesis of [11C]3a–c was performed by reacting 10a–c with [11C]methyl iodide. Compounds 3a–c displayed high or moderate in vitro binding affinities (Ki: 5–40 nM) for TSPO. PET with [11C]3a–c in rats showed high uptake in the lung, heart, and kidney, which are organs with high TSPO expression. Metabolite analysis with [11C]3a showed that radioactivity in these organs mainly corresponded with unchanged [11C]3a. PET with [11C]3a using a rat model of lung inflammation showed a significant signal in the lipopolysaccharide-treated lung. | |||||
| 書誌情報 |
Journal of Medicinal Chemistry 巻 54, 号 17, p. 6040-6049, 発行日 2011-09 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0022-2623 | |||||
