@article{oai:repo.qst.go.jp:00080122,
 author = {Deng, Xiaoyun and Zhang, Yiding and Chen, Zhen and Kumata, Katsushi and Van, Richard and Rong, Jian and Shao, Tuo and Hatori, Akiko and Mori, Wakana and Yu, Qingzhen and Kuan, Hu and Fujinaga, Masayuki and Hsiao-Ying, Wey and Shao, Yihan and Josephson, Lee and Murtas, Giulia and Pollegioni, Loredano and Ming-Rong, Zhang and Liang, Huan and Zhang, Yiding and Kumata, Katsushi and Hatori, Akiko and Mori, Wakana and Kuan, Hu and Fujinaga, Masayuki and Ming-Rong, Zhang and Liang, Huan},
 issue = {16},
 journal = {Bioorganic & Medicinal Chemistry Letters},
 month = {Jun},
 note = {Selective DAAO inhibitors have demonstrated promising therapeutic effects in clinical studies, including clinically alleviating symptoms of schizophrenic patients and ameliorating cognitive function in Alzheimer’s patients with early phase. Herein we report the synthesis and preliminary evaluation of a 11C-labeled positron emission tomography ligand based on a DAAO inhibitor, DAO-1903 (8). 11C-Isotopologue of 8 was prepared in high radiochemical yield with high radiochemical purity (>99%) and high molar activity (>37 GBq/µmol). In vitro autoradiography studies indicated that the ligand possessed high in vitro specific binding to DAAO, while in vivo dynamic PET studies demonstrated that [11C]8 failed to cross the blood–brain barrier possibly due to moderate brain efflux mechanism. Further chemical scaffold optimization is necessary to overcome limited brain permeability and improve specific binding.},
 title = {Synthesis and preliminary evaluation of 4-hydroxy-6-(3-[11C]methoxyphenethyl)pyridazin-3(2H)-one, a 11C-labeled d-amino acid oxidase (DAAO) inhibitor for PET imaging},
 volume = {30},
 year = {2020}
}