@article{oai:repo.qst.go.jp:00046172,
 author = {Kumata, Katsushi and Yui, Joji and Hatori, Akiko and Fujinaga, Masayuki and Yanamoto, Kazuhiko and Yamasaki, Tomoteru and Kawamura, Kazunori and Wakizaka, Hidekatsu and Nengaki, Nobuki and Yoshida, Yuichirou and Ogawa, Masanao and Fukumura, Toshimitsu and Zhang, Ming-Rong and 熊田 勝志 and 由井 譲二 and 羽鳥 晶子 and 藤永 雅之 and 柳本 和彦 and 山崎 友照 and 河村 和紀 and 脇坂 秀克 and 念垣 信樹 and 吉田 勇一郎 and 小川 政直 and 福村 利光 and 張 明栄},
 issue = {17},
 journal = {Journal of Medicinal Chemistry},
 month = {Sep},
 note = {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.},
 pages = {6040--6049},
 title = {Synthesis and Evaluation of Novel Carbon-11 Labeled Oxopurine Analogues for Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Peripheral Organs},
 volume = {54},
 year = {2011}
}