@article{oai:repo.qst.go.jp:00045760, author = {Yui, Joji and Hatori, Akiko and Yanamoto, Kazuhiko and Takei, Makoto and Nengaki, Nobuki and Kumata, Katsushi and Kawamura, Kazunori and Yamasaki, Tomoteru and Suzuki, Kazutoshi and Zhang, Ming-Rong and 由井 譲二 and 羽鳥 晶子 and 柳本 和彦 and 武井 誠 and 念垣 信樹 and 熊田 勝志 and 河村 和紀 and 山崎 友照 and 鈴木 和年 and 張 明栄}, issue = {6}, journal = {Synapse}, month = {Jun}, note = {In the central nervous system, translocator protein (TSPO) (18 kDa) (Papadopoulos et al., 2006), formerly named peripheral-type benzodiazepine receptor (PBR), is located in the microglial cells of the brain (Braestrup et al., 1977; Stephenson et al., 1995). Many studies have elucidated the relationship between TSPO and neurodegenerative diseases, such as Alzheimer's disease (Maeda et al., 2007; Yasuno et al., 2008), and stroke-induced brain injury (Rojas et al., 2007). To image TSPO in vivo, a number of new ligands have been labeled with the positron emitters 11C and 18F (Chauveau et al., 2008). We have developed [11C]DAA1106 (Zhang et al., 2003; Maeda et al., 2004), [18F]FEDAA1106 (Zhang et al., 2004), and [11C]AC-5216 (Zhang et al., 2007) for clinical imaging of TSPO in the brain. We recently synthesized and evaluated N-benzyl-N-[11C]methyl-2-(7- methyl-8-oxo-2-phenyl-7, 8-dihydro-9H-purin-9-yl)acetamide with a specific activity of 37–110 GBq/lmol for the imaging of TSPO (Yanamoto et al., 2009). The aim of this study was to synthesize N-benzyl- N-methyl-2-(7-[11C]methyl-8-oxo-2-phenyl-7,8-dihydro- 9H-purin-9-yl)acetamide ([11C]DAC) with ultra-high specific activity (average 4560 GBq/lmol), and to characterize specific binding to TSPO in the rat brain after ischemia. Using [11C]DAC of high specific activity, we expected to acquire high uptake ratios between the ipsilateral and contralateral sides and higher binding potential for TSPO from autoradiographic and PET images of infarct brains. Here, we labeled the methyl group of purine ring of DAC to achieve ultra-high specific activity using [11C]CH3I that was prepared by iodination of [11C]CH4 (Noguchi and Suzuki, 2003; Noguchi et al., 2008). We performed comparative evaluation using [11C]DAC with middle specific activity and low specific activity to elucidate the effect of specific activity on the in vitro and in vivo specific binding of [11C]DAC to TSPO in an infarct rat brain after ischemia. In this article we use the terms ''high SA,'' ''middle SA,'' and ''low SA'' to refer to specific activities of 3540–5580, 29–52, and 0.3–0.4 GBq/lmol, respectively.}, pages = {488--493}, title = {Imaging of the translocator protein (18kDa) in rat brain after ischemia using [11C]DAC with ultra-high specific Activity}, volume = {64}, year = {2010} }