@article{oai:repo.qst.go.jp:00080190,
 author = {Ji-yun, Sun and Kumata, Katsushi and Chen, Zhen and Zhang, Yiding and Jia-hui, Chen and Hatori, Akiko and Hua-long, Fu and Rong, Jiang and Xiao-yun, Deng and Yamasaki, Tomoteru and Xie, Lin and Kuan, Hu and Fujinaga, Masayuki and Qing-zhen, Yu and Shao, Tuo and Lee Collier, Thomas and Josephson, Lee and Yi-han, Shao and Yun-fei, Du and Lu, Wang and Xu, Hao and Ming-Rong, Zhang and Liang, Huan and Katsushi, Kumata and Zhang, Yiding and Akiko, Hatori and Tomoteru, Yamasaki and Lin, Xie and Kuan, Hu and Masayuki, Fujinaga and Lu, Wang and Zhang, Ming-Rong and Liang, Huan},
 journal = {Acta Pharmacologica Sinica},
 month = {Jul},
 note = {N-methyl-D-aspartate receptors (NMDARs) play critical roles in the physiological function of the mammalian central nervous system (CNS), including learning, memory, and synaptic plasticity, through modulating excitatory neurotransmission. Attributed to etiopathology of various CNS disorders and neurodegenerative diseases, GluN2B is one of the most well-studied subtypes in preclinical and clinical studies on NMDARs. Herein, we report the synthesis and preclinical evaluation of two 11C-labeled GluN2B-selective negative allosteric modulators (NAMs) containing N,N-dimethyl-2-(1H-pyrrolo[3,2-b]pyridin-1-yl)acetamides for positron emission tomography (PET) imaging. Two PET ligands, namely [11C]31 and [11C]37 (also called N2B-1810 and N2B-1903, respectively) were labeled with [11C]CH3I in good radiochemical yields (decay-corrected 28% and 32% relative to starting [11C]CO2, respectively), high radiochemical purity (>99%) and high molar activity (>74 GBq/μmol). In particular, PET ligand [11C]31 demonstrated moderate specific binding to GluN2B subtype by in vitro autoradiography studies. However, because in vivo PET imaging studies showed limited brain uptake of [11C]31 (up to 0.5 SUV), further medicinal chemistry and ADME optimization are necessary for this chemotype attributed to low binding specificity and rapid metabolism in vivo.},
 pages = {491--498},
 title = {Synthesis and preliminary evaluation of novel 11C-labeled GluN2B-selective NMDA receptor negative allosteric modulators},
 volume = {42},
 year = {2020}
}