@article{oai:repo.qst.go.jp:00048948,
 author = {Zhang, Xiaofei and Kumata, Katsushi and Yamasaki, Tomoteru and Cheng, Ran and Hatori, Akiko and Ma, Longle and Zhang, Yiding and Xie, Lin and Wang, Lu and Jin, Kang Hye and J., Sheffler Douglas and D., P. Cosford Nicholas and Zhang, Ming-Rong and H.Liang, Steven and 熊田 勝志 and 山崎 友照 and 羽鳥 晶子 and 張 一鼎 and 謝 琳 and 張 明栄},
 issue = {9},
 journal = {ACS Chemical Neuroscience},
 month = {May},
 note = {Metabotropic glutamate 2 receptors (mGlu2) are involved in the pathogenesis of several
CNS disorders and neurodegenerative diseases. Pharmacological modulation of this target represents a
potential disease-modifying approach for the treatment of substance abuse, depression, schizophrenia
and dementias. While quantification of mGlu2 receptors in the living brain by positron emission
tomography (PET) would help us better understand signaling pathways relevant to these conditions,
few successful examples have been demonstrated to image mGlu2 in vivo and a suitable PET tracer is
yet to be identified. Herein we report the design and synthesis of a radiolabeled negative allosteric
modulator (NAM) for mGlu2 PET tracer
development based on a quinoline 2-carboxamide
scaffold. The most promising candidate,
7-((2,5-dioxopyrrolidin-1-yl)methyl)-4-(2-fluoro-4-
[11C]methoxyphenyl) quinoline-2-carboxamide
([11C]QCA) was prepared in 13% radiochemical
yield (non-decay corrected at the end of synthesis) with >99% radiochemical purity and >74
GBq/μmol (2 Ci/μmol) specific activity. While the tracer showed limited brain uptake (0.3 SUV),
probably attributable to effects on PgP/Bcrp eff lux pump, in vitro autoradiography studies
demonstrated heterogeneous brain distribution and specific binding. Thus, [11C]QCA is a
chemical probe that},
 pages = {1937--1948},
 title = {Synthesis and preliminary studies of a novel negative allosteric modulator [11C]QCA for imaging of metabotropic glutamate receptor 2},
 volume = {8},
 year = {2017}
}