On March 31, 2021, Sun, Ji-yun; Kumata, Katsushi; Chen, Zhen; Zhang, Yi-ding; Chen, Jia-hui; Hatori, Akiko; Fu, Hua-long; Rong, Jian; Deng, Xiao-yun; Yamasaki, Tomoteru; Xie, Lin; Hu, Kuan; Fujinaga, Masayuki; Yu, Qing-zhen; Shao, Tuo; Collier, Thomas Lee; Josephson, Lee; Shao, Yi-han; Du, Yun-fei; Wang, Lu; Xu, Hao; Zhang, Ming-rong; Liang, Steven H. published an article.Electric Literature of 1820711-82-7 The title of the article was Synthesis and preliminary evaluation of novel 11C-labeled GluN2B-selective NMDA receptor negative allosteric modulators. And the article contained the following:
Abstract: N-methyl-D-aspartate receptors (NMDARs) play critical roles in the physiol. function of the mammalian central nervous system (CNS), including learning, memory, and synaptic plasticity, through modulating excitatory neurotransmission. Attributed to etiopathol. of various CNS disorders and neurodegenerative diseases, GluN2B is one of the most well-studied subtypes in preclin. and clin. studies on NMDARs. Herein, we report the synthesis and preclin. evaluation of two 11C-labeled GluN2B-selective neg. allosteric modulators (NAMs) containing N,N-dimethyl-2-(1H-pyrrolo[3,2-b]pyridin-1-yl)acetamides for positron emission tomog. (PET) imaging. Two PET ligands, namely [11C]31 and [11C]37 (also called N2B-1810 and N2B-1903, resp.) were labeled with [11C]CH3I in good radiochem. yields (decay-corrected 28% and 32% relative to starting [11C]CO2, resp.), high radiochem. 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 autoradiog. studies. However, because in vivo PET imaging studies showed limited brain uptake of [11C]31 (up to 0.5 SUV), further medicinal chem. and ADME optimization are necessary for this chemotype attributed to low binding specificity and rapid metabolism in vivo. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Electric Literature of 1820711-82-7
The Article related to glun2b receptor neg allosteric modulator pet imaging radiotracer brain, glun2b subunit, nmdars, carbon-11, ionotropic glutamate receptors (iglurs), positron emission tomography (pet) and other aspects.Electric Literature of 1820711-82-7