| Chemical Properties | Back Directory | [Boiling point ]
432.5±45.0 °C(predicted) | [density ]
1.218±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [pka]
14.87±0.40(predicted) |
| Hazard Information | Back Directory | [Uses]
mG2N001 is a negative allosteric modulator (NAM) (IC50: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope [11C]mG2N001 can be used in PET imaging. [11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images[1]. | [in vivo]
mG2N001 (63.0-87.3 MBq [11C]mG2N001, iv.) can perform PET imaging experiments in rats and cynomolgus monkeys, showing the specific binding activity of mGluR2, clearly showing the binding activity of mGluR2 in the animal brain Biological distribution map[1].
| [References]
[1] Yuan G, et al. Synthesis and Characterization of 5-(2-Fluoro-4-[11C]methoxyphenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridine-7-carboxamide as a PET Imaging Ligand for Metabotropic Glutamate Receptor 2. J Med Chem. 2022 Feb 10;65(3):2593-2609. DOI:10.1021/acs.jmedchem.1c02004 |
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