@article{oai:repo.qst.go.jp:00080793,
 author = {Yamasaki, Tomoteru and Zhang, Xiaofei and Kumata, Katsushi and Zhang, Yiding and Deng, Xiaoyun and Fujinaga, Masayuki and Chen, Zhen and Mori, Wakana and Kuan, Hu and Wakizaka, Hidekatsu and Hatori, Akiko and Xie, Lin and Ogawa, Masanao and Nengaki, Nobuki and Van, Richard and Shao, Yihan and J. Sheffler, Douglas and D. P. Cosford, Nicholas and Liang, Huan and Ming-Rong, Zhang and Tomoteru, Yamasaki and Katsushi, Kumata and Zhang, Yiding and Masayuki, Fujinaga and Wakana, Mori and Kuan, Hu and Hidekatsu, Wakizaka and Akiko, Hatori and Lin, Xie and Masanao, Ogawa and Nobuki, Nengaki and Liang, Huan and Zhang, Ming-Rong},
 issue = {63},
 journal = {Journal of Medicinal Chemistry},
 month = {Sep},
 note = {Metabotropic glutamate receptor 2 (mGlu2) is a known target for treating several central nervous system (CNS) disorders. To develop a viable positron emission tomography (PET) ligand for mGlu2, we identified new candidates 5a–i that are potent negative allosteric modulators (NAMs) of mGlu2. Among these candidates, 4-(2-fluoro-4-methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide (5i, also named as [11C]MG2-1812) exhibited high potency, high subtype selectivity, and favorable lipophilicity. Compound 5i was labeled with positron-emitting carbon-11 (11C) to obtain [11C]5i in high radiochemical yield and high molar activity by O-[11C]methylation of the phenol precursor 12 with [11C]CH3I. In vitro autoradiography with [11C]5i showed heterogeneous radioactive accumulation in the brain tissue sections, ranked in the order: cortex > striatum > hippocampus > cerebellum ≫ thalamus > pons. PET study of [11C]5i indicated in vivo specific binding of mGlu2 in the rat brain. Based on the [11C]5i scaffold, further optimization for new candidates is underway to identify a more suitable ligand for imaging mGlu2.},
 pages = {11469--11483},
 title = {Identification and Development of a New Positron Emission Tomography Ligand 4-(2-Fluoro-4-[11C]methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide for Imaging Metabotropic Glutamate Receptor Subtype 2 (mGlu2)},
 volume = {2020},
 year = {2020}
}