ArticleScientific reports2015
Preliminary Characterization and In Vivo Studies of Structurally Identical (18)F- and (125)I-Labeled Benzyloxybenzenes for PET/SPECT Imaging of β-Amyloid Plaques.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 19 citations in OpenAlex.
- 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
- Computational Chemistry for the Identification of Lead Compounds for Radiotracer Development.Pharmaceuticals (Basel, Switzerland) · 2023Review
- [Current radiopharmaceuticals · 2019Article
- Efficient and Site-SpecificACS omega · 2018Article
- Highly specific noninvasive photoacoustic and positron emission tomography of brain plaque with functionalized croconium dye labeled by a radiotracer.Chemical science · 2017Article
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
With the assistance of molecular docking and 3D-QSAR models established previously, structurally identical (18)F- and (125)I-labeled benzyloxybenzene derivatives were designed to achieve the early detection of Aβ plaques by PET/SPECT imaging. In competition binding assay, ligands 7a and 12a displayed high binding affinities to Aβ42 aggregates with Ki values of 19.5 nM and 23.9 nM, respectively. Specific plaque labeling was observed on the in vitro autoradiography of brain sections from AD patients and Tg mice. In biodistribution, [(125)I]7a, [(18)F]7a, [(125)I]12a and [(18)F]12a all exhibited high initial brain uptakes (>5% ID/g at 2 min). [(125)I]7a and [(125)I]12a cleared fast from the normal brain regions, while corresponding [(18)F]7a and [(18)F]12a showed slow washout rates. Dynamic microPET/CT and microSPECT/CT imaging data in normal ICR mice were in accordance with in vivo biodistribution results. In vivo metabolism results indicated that the different clearance profiles between the structurally identical (18)F- and (125)I-labeled tracers could be attributed to different biochemical characteristics of the radiometabolites. Radioiodinated benzyloxybenzene derivatives exhibited good in vivo biostability in brain. Ex vivo autoradiography further confirmed the strong in vivo Aβ labeling ability of [(125)I]7a. These new fluorinated and iodinated benzyloxybenzenes can develop into PET/SPECT dual imaging agents targeting Aβ plaques.
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