Rong, Jian published the artcileNovel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold, Recommanded Product: 2-Fluoro-4-iodo-6-methylpyridine, the main research area is piperazinyl azetidine PET ligand preparation imaging monoacylglycerol lipase.
Monoacylglycerol lipase (MAGL) is a 33 kDa serine protease primarily responsible for hydrolyzing 2-arachidonoylglycerol into the proinflammatory eicosanoid precursor arachidonic acid in the central nervous system. Inhibition of MAGL constitutes an attractive therapeutic concept for treating psychiatric disorders and neurodegenerative diseases. Herein, we present the design and synthesis of multiple reversible MAGL inhibitor candidates based on a piperazinyl azetidine scaffold. Compounds 10 and 15 were identified as the best-performing reversible MAGL inhibitors by pharmacol. evaluations, thus channeling their radiolabeling with fluorine-18 in high radiochem. yields and favorable molar activity. Furthermore, evaluation of [18F]10 and [18F]15 ([18F]MAGL-2102) by autoradiog. and positron emission tomog. (PET) imaging in rodents and nonhuman primates demonstrated favorable brain uptakes, heterogeneous radioactivity distribution, good specific binding, and adequate brain kinetics, and [18F]15 demonstrated a better performance. In conclusion, [18F]15 was found to be a suitable PET radioligand for the visualization of MAGL, harboring potential for the successful translation into humans.
Journal of Medicinal Chemistry published new progress about Homo sapiens. 884494-45-5 belongs to class iodides-buliding-blocks, name is 2-Fluoro-4-iodo-6-methylpyridine, and the molecular formula is C6H5FIN, Recommanded Product: 2-Fluoro-4-iodo-6-methylpyridine.
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com