WEKO3
アイテム
Synthesis and evaluation of PET probes for the imaging of I2 imidazoline receptors in peripheral tissues
https://repo.qst.go.jp/records/46275
https://repo.qst.go.jp/records/4627542fdc06a-f96d-4ac8-aa23-a2dc911670b1
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2012-02-24 | |||||
| タイトル | ||||||
| タイトル | Synthesis and evaluation of PET probes for the imaging of I2 imidazoline receptors in peripheral tissues | |||||
| 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× Yui, Joji× Konno, Fujiko× Yamasaki, Tomoteru× Hatori, Akiko× Wakizaka, Hidekatsu× Fujinaga, Masayuki× Kumata, Katsushi× Yoshida, Yuichirou× Ogawa, Masanao× Nengaki, Nobuki× Yanamoto, Kazuhiko× Fukumura, Toshimitsu× Zhang, Ming-Rong× 河村 和紀× 由井 譲二× 昆野 富士子× 山崎 友照× 羽鳥 晶子× 脇坂 秀克× 藤永 雅之× 熊田 勝志× 吉田 勇一郎× 小川 政直× 念垣 信樹× 柳本 和彦× 福村 利光× 張 明栄 |
|||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Introduction: To explore the possible use of positron emission tomography (PET) probes for imaging of I2-imidazoline receptors (I2Rs) in peripheral tissues, we labeled two new I2R ligands, 2-[2-(o-tolyl)vinyl]-4,5-dihydro-1H-imidazole (Ki for I2Rs, 3.7 nM) and 2-[2-(o-tolyl) ethyl]-4,5-dihydro-1H-imidazole (Ki for I2Rs, 1.7 nM) with 11C ([11C]metrazoline and [11C]TEIMD), respectively, and evaluated these ligands and the recently developed I2R ligand 2-[3-fluoro-[4-11C]tolyl]-4,5-dihydro-1H-imidazole ([11C]FTIMD) by in vivo studies. Methods: [11C]Metrazoline and [11C]TEIMD were prepared by a palladium-promoted cross-coupling reaction of the tributylstannyl precursor and [11C]methyl iodide. Their biodistribution in mice was investigated by tissue dissection. In addition, PET scans and metabolite analysis were performed. Results: [11C]Metrazoline and [11C]TEIMD were successfully synthesized with a suitable radioactivity for injection. In the liver and pancreas expressing I2Rs, coinjection with the high-affinity I2R ligand, BU224, induced a reduction in the radioactivity level at 30 min after injection of [11C]metrazoline and [11C]FTIMD. However, the radioactivity level after injection of [11C]TEIMD was unchanged. In the PET study, coinjection with BU224 induced a decrease in the radioactivity level in the liver and pancreas after more than 15 min of injection of [11C]metrazoline and [11C]FTIMD as compared with the results obtained for controls. In metabolite analysis, coinjection with BU224 induced a significant reduction in the percentage of unchanged [11C]metrazoline at 30 min after injection as compared with that in the control, although no significant difference was observed in the percentage of unchanged [11C]FTIMD. Conclusion: [11C]Metrazoline may be a more useful PET probe than [11C]FTIMD for imaging of I2Rs in peripheral tissues. |
|||||
| 書誌情報 |
Nuclear Medicine and Biology 巻 39, 号 1, p. 89-99, 発行日 2012-01 |
|||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0969-8051 | |||||
