@article{oai:repo.qst.go.jp:00080110,
 author = {Deng, Xiaoyun and Zhang, Yiding and Rong, Jian and Kumata, Katsushi and Shao, Tuo and Wang, Gangqiang and Hatori, Akiko and Mori, Wakana and Yu, Qingzhen and Kuan, Hu and Fujinaga, Masayuki and Shao, Yihan and Josephson, Lee and Sun, Shaofa 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 = {27},
 journal = {Tetrahedron Letters},
 month = {May},
 note = {Positive allosteric modulators of muscarinic acetylcholine receptor subtype 4 have been identified as promising activators for the treatment of neurological disorders and neurodegenerative diseases, including schizophrenia, Alzheimer's disease (AD) and dementia with Lewy bodies (DLB). Herein we report the synthesis and preliminary evaluation of a 18F-labeled positron emission tomography ligand based on a M4 activator (7). 18F-Isotopologue of 7 was prepared in a reasonable radiochemical yield with high radiochemical purity (>99%) and high molar activity (>37 GBq/µmol). In vitro autoradiography studies indicated that the ligand possessed moderate in vitro specific binding. Dynamic PET studies in vivo demonstrated that [18F]7 (also named as [18F]M4R-1911) failed to cross the blood–brain barrier. Therefore, further chemical scaffold optimization in chemotype of 7 is necessary to overcome limited brain permeability and improve specific binding.},
 title = {Synthesis and preliminary evaluation of 18F-labeled 1-(6,7-dimethyl-4-(methylamino)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-yl)-2-(trans-2-(6-fluoropyridin-3-yl)cyclopropyl)ethan-1-one for imaging muscarinic acetylcholine receptor subtype 4},
 volume = {61},
 year = {2020}
}