@article{oai:repo.qst.go.jp:00044329,
 author = {Zhang, Ming-Rong and Kida, Takayo and Noguchi, Junko and Furutsuka, Kenji and Maeda, Jun and Suhara, Tetsuya and Suzuki, Kazutoshi and 張 明栄 and 古塚 賢士 and 前田 純 and 須原 哲也 and 鈴木 和年},
 journal = {Nuclear Medicine and Biology},
 month = {},
 note = {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.},
 pages = {513--519},
 title = {[11C]DAA1106: Radiosynthesis and in vivo binding to peripheral benzodiazepine receptors in mouse brain},
 volume = {30},
 year = {2003}
}