WEKO3
アイテム
[11C]DAA1106: Radiosynthesis and in vivo binding to peripheral benzodiazepine receptors in mouse brain
https://repo.qst.go.jp/records/44329
https://repo.qst.go.jp/records/44329a9bf11a4-3f08-4dba-8958-f46de58f6645
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2006-06-23 | |||||
| タイトル | ||||||
| タイトル | [11C]DAA1106: Radiosynthesis and in vivo binding to peripheral benzodiazepine receptors in mouse brain | |||||
| 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 |
Zhang, Ming-Rong
× Zhang, Ming-Rong× Kida, Takayo× Noguchi, Junko× Furutsuka, Kenji× Maeda, Jun× Suhara, Tetsuya× Suzuki, Kazutoshi× 張 明栄× 古塚 賢士× 前田 純× 須原 哲也× 鈴木 和年 |
|||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | DAA1106 (N-(2,5-Dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide), is a potent and selective ligand for peripheral benzodiazepine receptors (PBR) in mitochondrial fractions of rat (Ki=0.043 nM) and monkey (Ki=0.188 nM) brains. This compound was labeled by [11C]methylation of a corresponding desmethyl precursor (DAA1123) with [11C]CH3I in the presence of NaH, with a 72+/-16% (corrected for decay) incorporation yield of radioactivity. After HPLC purification, [11C]DAA1106 was obtained with >98% radiochemical purity and specific activity of 90-156 GBq/mumol at the end of synthesis. After iv injection of [11C]DAA1106 into mice, high accumulations of radioactivity were found in the olfactory bulb and cerebellum, the high PBR density regions in the brain. Coinjection of [11C]DAA1106 with unlabeled DAA1106 and PBR-selective PK11195 displayed a significant reduction of radioactivity, suggesting a high specific binding of [11C]DAA1106 to PBR. Although this tracer was rapidly metabolized in the plasma, only [11C]DAA1106 was detected in the brain tissues, suggesting the specific binding in the brain due to the tracer itself. These findings revealed that [11C]DAA1106 is a potential and selective positron emitting radioligand for PBR. | |||||
| 書誌情報 |
Nuclear Medicine and Biology 巻 30, p. 513-519, 発行日 2003 |
|||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0969-8051 | |||||
