| Title | ¹⁸F-labeled 2-phenylquinoxaline derivatives as potential positron emission tomography probes for in vivo imaging of β-amyloid plaques. |
| Publication Type | Journal Article |
| Year of Publication | 2012 |
| Authors | Yu P, Cui M, Wang X, Zhang X, Li Z, Yang Y, Jia J, Zhang J, Ono M, Saji H, Jia H, Liu B |
| Journal | Eur J Med Chem |
| Volume | 57 |
| Pagination | 51-8 |
| Date Published | 2012 Nov |
| ISSN | 1768-3254 |
| Keywords | Amyloid beta-Peptides, Animals, Autoradiography, Brain, Chromatography, High Pressure Liquid, Contrast Media, Fluorine Radioisotopes, Humans, Male, Mice, Mice, Transgenic, Peptide Fragments, Plaque, Amyloid, Positron-Emission Tomography, Quinoxalines, Radiography, Staining and Labeling, Tissue Distribution |
| Abstract | In continuation of our study on the 2-phenylquinoxaline scaffold as potential β-amyloid imaging probes, two [(18)F]fluoro-pegylated 2-phenylquinoxaline derivatives, 2-(4-(2-[(18)F]fluoroethoxy)phenyl)-N-methylquinoxalin-6-amine ([(18)F]4a) and 2-(4-(2-(2-(2-[(18)F]fluoroethoxy)ethoxy)ethoxy)phenyl)-N-methylquinoxalin-6-amine ([(18)F]4b) were prepared. Both of them displayed high binding affinity to Aβ(1-42) aggregates (K(i) = 10.0 ± 1.4 nM for 4a, K(i) = 5.3 ± 3.2 nM for 4b). The specific and high binding of [(18)F]4a and [(18)F]4b to Aβ plaques was confirmed by in vitro autoradiography on brain sections of AD human and transgenic mice. In biodistribution in normal mice, [(18)F]4a displayed high initial brain uptake (8.17% ID/g at 2 min) and rapid washout from the brain. These preliminary results suggest [(18)F]4a may be a potential PET imaging agent for Aβ plaques in the living human brain. |
| DOI | 10.1016/j.ejmech.2012.08.031 |
| Alternate Journal | Eur J Med Chem |
| PubMed ID | 23047223 |
Related Institute:
Molecular Imaging Innovations Institute (MI3)