| Title | Preliminary research on 1-(4-bromo-2-nitroimidazol-1-yl)-3-[(18)F]fluoropropan-2-ol as a novel brain hypoxia PET tracer in a rodent model of stroke. |
| Publication Type | Journal Article |
| Year of Publication | 2015 |
| Authors | Nieto E, Delgado M, Sobrado M, de Ceballos ML, Alajarín R, García-García L, Kelly J, Lizasoain I, Pozo MA, Álvarez-Builla J |
| Journal | Eur J Med Chem |
| Volume | 101 |
| Pagination | 604-15 |
| Date Published | 2015 Aug 28 |
| ISSN | 1768-3254 |
| Keywords | Animals, Cell Line, Disease Models, Animal, Hypoxia, Brain, Male, Mice, Molecular Structure, Nitroimidazoles, Positron-Emission Tomography, Propanols, Rats, Rats, Inbred F344, Stroke |
| Abstract | 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-[(18)F]fluoropropan-2-ol (4-Br-[(18)F]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 [(18)F]FMISO, the current gold standard PET hypoxia tracer. The new PET brain hypoxia tracer is more easily reduced, has higher CLogP than [(18)F]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-[(18)F]FMISO is a good candidate for further development in ischemic stroke. |
| DOI | 10.1016/j.ejmech.2015.06.023 |
| Alternate Journal | Eur J Med Chem |
| PubMed ID | 26204508 |
Related Institute:
Molecular Imaging Innovations Institute (MI3)