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Preliminary research on 1-(4-bromo-2-nitroimidazol-1-yl)-3-[18F]fluoropropan-2-ol as a novel brain hypoxia PET tracer in a rodent model of stroke

AuthorsNieto, Elena CSIC; Delgado, Mercedes; Sobrado, Mónica CSIC; Ceballos, María L. de CSIC ORCID; Alajarín, Ramón; García-García, Luis; Kelly, James; Lizasoain, Ignacio; Pozo, Miguel A.; Álvarez-Builla, Julio
PET imaging
Issue Date28-Aug-2015
CitationEuropean Journal of Medicinal Chemistry 101: 604-615 (2015)
Abstract© 2015 Elsevier Masson SAS. The synthesis of the new radiotracer precursor 4-Br-NITTP and the radiolabeling of the new tracer 1-(4-bromo-2-nitroimidazol-1-yl)-3-[18F]fluoropropan-2-ol (4-Br-[18F]FMISO) is reported. The cyclic voltammetry behaviour, neuronal cell toxicity, transport through the brain endothelial cell monolayer, in vivo PET imaging and preliminary calculations of the tracer uptake for a rodent model of stroke were studied for the new compound and the results were compared to those obtained with [18F]FMISO, the current gold standard PET hypoxia tracer. The new PET brain hypoxia tracer is more easily reduced, has higher CLogP than [18F]FMISO and it diffuses more rapidly through brain endothelial cells. The new compound is non-toxic to neuronal cells and it allows the in vivo mapping of stroke in mice with higher sensitivity. 4-Br-[18F]FMISO is a good candidate for further development in ischemic stroke.
Publisher version (URL)http://dx.doi.org/10.1016/j.ejmech.2015.06.023
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