@article{oai:repo.qst.go.jp:00080545,
 author = {Kumata, Katsushi and Zhang, Yiding and Ogawa, Masanao and Kurihara, Yusuke and Mori, Wakana and Kuan, Hu and Fujinaga, Masayuki and Nengaki, Nobuki and Ming-Rong, Zhang and Katsushi, Kumata and Zhang, Yiding and Masanao, Ogawa and Kurihara, Yusuke and Wakana, Mori and Kuan, Hu and Masayuki, Fujinaga and Nobuki, Nengaki and Zhang, Ming-Rong},
 issue = {23},
 journal = {Bioorganic & Medicinal Chemistry Letters},
 month = {Sep},
 note = {Selective metabotropic glutamate receptor 2 (mGluR2) inhibitors have been demonstrated to show therapeutic effects by improving alleviating symptoms of schizophrenic patients in clinical studies. Herein we report the synthesis and preliminary evaluation of a 11C-labeled positron emission tomography (PET) tracer originating from a mGluR2 inhibitor, 3-(cyclopropylmethyl)-7-((4-(4-methoxyphenyl)piperidin-1-yl)methyl)-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine (CMTP, 1a). [11C]CMTP ([11C]1a) was synthesized by O-[11C]methylation of desmethyl precursor 1b with [11C]methyl iodide in 19.7 ± 8.9% (n = 10) radiochemical yield (based on [11C]CO2) with >98% radiochemical purity and >74 GBq/μmol molar activity. Autoradiography study showed that [11C]1a possessed moderate in vitro specific binding to mGluR2 in the rat brain, with a heterogeneous distribution of radioactive accumulation in the mGluR2-rich brain tissue sections, such as the cerebral cortex and striatum. PET study indicated that [11C]1a was able to cross the blood–brain barrier and enter the brain, but had very low specific binding in the rat brain. Further optimization for the chemical structure of 1a is necessary to increase binding affinity to mGluR2 and then improve in vivo specific binding in brain.},
 title = {3-(Cyclopropylmethyl)-7-((4-(4-[11C]methoxyphenyl)piperidin-1-yl)methyl)-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine: Synthesis and preliminary evaluation for PET imaging of metabotropic glutamate receptor subtype 2},
 volume = {30},
 year = {2020}
}