Milicevic Sephton, Selena; Vetterli, Peter T.; Pedani, Valentina; Cermak, Stjepko; Chiotellis, Aristeidis; Roscales, Sylvia; Mueller Herde, Adrienne; Schibli, Roger; Auberson, Yves P.; Ametamey, Simon M. published an article in 2017, the title of the article was Synthesis and Biological Evaluation of Quinoxaline Derivatives for PET Imaging of the NMDA Receptor.Recommanded Product: 2-Chloro-4-methyl-1-nitrobenzene And the article contains the following content:
Due to the biol. complexity of the N-methyl-D-aspartate receptor (NMDAR), the development of a positron emission tomog. radiotracer for the imaging of NMDAR has met with limited success. Recent studies have established the presence of GluN2A subunit of the NMDAR in the heart and its role in the regulation of intracellular calcium levels. In our efforts to develop an imaging agent for the GluN2A subunit, we designed three new compounds based on a quinoxaline scaffold. The synthesis of the analogs was based on a two-step Kabachnik-Fields reaction in sequence with Suzuki cross-coupling and acid hydrolysis. They exhibited comparable high binding affinity values below 5 nM. A two-step radiolabeling procedure was successfully developed for the synthesis of [18F]I. [18F]I was obtained in a modest overall radiochem. yield of 5.5 ± 4.2%, a good specific radioactivity of 254 ± 158 GBq/μmol, and a radiochem. purity > 99%. While two compounds showed comparable binding affinity towards NMDAR, sluggish radiolabeling, prevented their further evaluation. For [18F]I, in vitro autoradiog. on rat heart slices demonstrated heterogeneous but unspecific accumulation, whereas for the brain a high in vitro specificity towards NMDAR, could be demonstrated. The experimental process involved the reaction of 2-Chloro-4-methyl-1-nitrobenzene(cas: 38939-88-7).Recommanded Product: 2-Chloro-4-methyl-1-nitrobenzene
The Article related to quinoxaline preparation pet imaging, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 2-Chloro-4-methyl-1-nitrobenzene
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