ArticleACS medicinal chemistry letters2010
Fluorinated Benzofuran Derivatives for PET Imaging of β-Amyloid Plaques in Alzheimer's Disease Brains.
Article in ACS medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Ligands for Protein Fibrils of Amyloid-β, α-Synuclein, and Tau.Chemical reviews · 2025Review
- Discovery of High-Affinity Amyloid Ligands Using a Ligand-Based Virtual Screening Pipeline.Journal of the American Chemical Society · 2023Article
- Benzothiazolium Derivative-Capped Silica Nanocomposites for β-Amyloid ImagingAnalytical chemistry · 2021Article
- Amyloid-β probes: Review of structure-activity and brain-kinetics relationships.Beilstein journal of organic chemistry · 2013Article
- Development of novel 123I-labeled pyridyl benzofuran derivatives for SPECT imaging of β-amyloid plaques in Alzheimer's disease.PloS one · 2013Article
- BODIPY-based molecular probe for imaging of cerebral β-amyloid plaques.ACS chemical neuroscience · 2012Article
- (18)F-labeled phenyldiazenyl benzothiazole for in vivo imaging of neurofibrillary tangles in Alzheimer's disease brains.ACS medicinal chemistry letters · 2012Article
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A series of fluorinated benzofuran derivatives as potential tracers for positron emission tomography (PET) targeting β-amyloid plaques in the brains of patients with Alzheimer's disease (AD) were synthesized and evaluated. The derivatives were produced using an intramolecular Wittig reaction. In experiments in vitro, all displayed high affinity for Aβ(1-42) aggregates with K i values in the nanomolar range. Radiofluorinated 17, [(18)F]17, in particular labeled β-amyloid plaques in sections of Tg2576 mouse brain and displayed high uptake (5.66% ID/g) at 10 min postinjection, sufficient for PET imaging. In addition, in vivo β-amyloid plaque labeling can be clearly demonstrated with [(18)F]17 in Tg2576 mice. In conclusion, [(18)F]17 may be useful for detecting β-amyloid plaques in patients with AD.
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