On December 22, 2016, Tamborini, Lucia; Chen, Ying; Foss, Catherine A.; Pinto, Andrea; Horti, Andrew G.; Traynelis, Stephen F.; De Micheli, Carlo; Mease, Ronnie C.; Hansen, Kasper B.; Conti, Paola; Pomper, Martin G. published an article.Product Details of 98946-18-0 The title of the article was Development of Radiolabeled Ligands Targeting the Glutamate Binding Site of the N-Methyl-D-aspartate Receptor as Potential Imaging Agents for Brain. And the article contained the following:
Abnormal activity of various N-methyl-D-aspartate receptor (NMDAR) subtypes has been implicated in a wide variety of neurol. disorders such as Alzheimer’s disease, schizophrenia, and epilepsy. Imaging agents for PET and SPECT that target NMDARs in a subtype-selective fashion may enable better characterization of those disorders and enhance drug development. On the basis of a pyrazoline derivative that demonstrated neuroprotective effects in vivo, we synthesized a series of para-substituted analogs and measured their affinities to various NMDAR subtypes. Compounds 4a-c and 4e showed greater, nanomolar affinity for the GluN1/2A subtype vs. GluN1/2B. Dicarbomethoxy (pro-drug) analogs of [124/125I]4d and [11C]4e (i.e., [124/125I]11d and [11C]11e) were generated and tested for NMDAR binding specificity in ex vivo autoradiog. and brain biodistribution studies. Although NMDAR-specific binding could be demonstrated for [125I]11d and [11C]11e through autoradiog. and biodistribution studies, imaging of neither [124I]11d nor [11C]11e could demonstrate brain penetration sufficient for detection by PET. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Product Details of 98946-18-0
The Article related to preparation nmda receptor targeting radiolabeled ligand brain imaging, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Product Details of 98946-18-0
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