35272-08-3Relevant academic research and scientific papers
Development of Radiolabeled Ligands Targeting the Glutamate Binding Site of the N-Methyl-d-aspartate Receptor as Potential Imaging Agents for Brain
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.
, p. 11110 - 11119 (2016)
Abnormal activity of various N-methyl-d-aspartate receptor (NMDAR) subtypes has been implicated in a wide variety of neurological 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 analogues and measured their affinities to various NMDAR subtypes. Compounds 4a-c and 4e showed greater, nanomolar affinity for the GluN1/2A subtype versus GluN1/2B. Dicarbomethoxy (pro-drug) analogues 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 autoradiography and brain biodistribution studies. Although NMDAR-specific binding could be demonstrated for [125I]11d and [11C]11e through autoradiography and biodistribution studies, imaging of neither [124I]11d nor [11C]11e could demonstrate brain penetration sufficient for detection by PET.
HETEROCYCLES FROM NITRILE IMINES. PART I. 1,2,3,4-TETRAHYDRO-1,2,4,5-TETRAZINES
El-Abadelah, Mustafa M.,Hussein, Ahmad Q.,Kamal, Marwan R.,Al-Adhami, Khaled H.
, p. 917 - 924 (2007/10/02)
The interaction between ketohydrazones and nitrile imines provides a new and direct synthetic route to 1,2,3,4-tetrahydro-1,2,4,5-tetrazines.Elemental analysis and spectral data are consistent with the assigned tetrazine ring system.
