| Title | 18F-THK523: a novel in vivo tau imaging ligand for Alzheimer's disease. |
| Publication Type | Journal Article |
| Year of Publication | 2011 |
| Authors | Fodero-Tavoletti, MT, Okamura, N, Furumoto, S, Mulligan, RS, Connor, AR, McLean, CA, Cao, D, Rigopoulos, A, Cartwright, GA, O'Keefe, G, Gong, S, Adlard, PA, Barnham, KJ, Rowe, CC, Masters, CL, Kudo, Y, Cappai, R, Yanai, K, Villemagne, VL |
| Journal | Brain |
| Volume | 134 |
| Issue | Pt 4 |
| Pagination | 1089-100 |
| Date Published | 2011 Apr |
| ISSN | 1460-2156 |
| Keywords | Alzheimer Disease, Analysis of Variance, Aniline Compounds, Animals, Autoradiography, Binding Sites, Brain, Female, Fluorodeoxyglucose F18, Humans, Immunohistochemistry, Male, Mice, Quinolines, Radiopharmaceuticals, tau Proteins |
| Abstract | While considerable effort has focused on developing positron emission tomography β-amyloid imaging radiotracers for the early diagnosis of Alzheimer's disease, no radiotracer is available for the non-invasive quantification of tau. In this study, we detail the characterization of (18)F-THK523 as a novel tau imaging radiotracer. In vitro binding studies demonstrated that (18)F-THK523 binds with higher affinity to a greater number of binding sites on recombinant tau (K18Δ280K) compared with β-amyloid(1-42) fibrils. Autoradiographic and histofluorescence analysis of human hippocampal serial sections with Alzheimer's disease exhibited positive THK523 binding that co-localized with immunoreactive tau pathology, but failed to highlight β-amyloid plaques. Micro-positron emission tomography analysis demonstrated significantly higher retention of (18)F-THK523 (48%; P |
| DOI | 10.1093/brain/awr038 |
| Alternate Journal | Brain |
| PubMed ID | 21436112 |
