| Title | (99m)Tc-labeled dibenzylideneacetone derivatives as potential SPECT probes for in vivo imaging of β-amyloid plaque. |
| Publication Type | Journal Article |
| Year of Publication | 2013 |
| Authors | Yang Y, Cui M, Jin B, Wang X, Li Z, Yu P, Jia J, Fu H, Jia H, Liu B |
| Journal | Eur J Med Chem |
| Volume | 64 |
| Pagination | 90-8 |
| Date Published | 2013 Jun |
| ISSN | 1768-3254 |
| Keywords | Amyloid beta-Peptides, Animals, Butanones, Disease Models, Animal, Fluorescent Dyes, Male, Mice, Mice, Inbred C57BL, Mice, Inbred ICR, Mice, Transgenic, Molecular Imaging, Molecular Structure, Organometallic Compounds, Peptide Fragments, Plaque, Amyloid, Rhenium, Staining and Labeling, Technetium, Tomography, Emission-Computed, Single-Photon |
| Abstract | Four (99m)Tc-labeled dibenzylideneacetone derivatives and corresponding rhenium complexes were successfully synthesized and biologically evaluated as potential imaging probes for Aβ plaques using SPECT. All rhenium complexes (5a-d) showed affinity for Aβ(1-42) aggregates (Ki = 13.6-120.9 nM), and selectively stained the Aβ plaques on brain sections of transgenic mice. Biodistribution in normal mice revealed that [(99m)Tc]5a-d exhibited moderate initial uptake (0.31%-0.49% ID/g at 2 min) and reasonable brain washout at 60 min post-injection. Although additional optimizations are still needed to facilitate it's penetration through BBB, the present results indicate that [(99m)Tc]5a may be a potential SPECT probe for imaging Aβ plaques in Alzheimer's brains. |
| DOI | 10.1016/j.ejmech.2013.03.057 |
| Alternate Journal | Eur J Med Chem |
| PubMed ID | 23644192 |
Related Institute:
Molecular Imaging Innovations Institute (MI3)