ArticleACS chemical neuroscience2014
High affinity radiopharmaceuticals based upon lansoprazole for PET imaging of aggregated tau in Alzheimer's disease and progressive supranuclear palsy: synthesis, preclinical evaluation, and lead selection.
Article in ACS chemical neuroscience, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
43 citing papers in PubMed, 87 citations in OpenAlex.
- Widespread brain tau and its association with ageing, Braak stage and Alzheimer's dementia.Brain : a journal of neurology · 2018Trial
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- Trifluoromethylation of alkyl electrophiles withScience (New York, N.Y.) · 2025Article
- Ligands for Protein Fibrils of Amyloid-β, α-Synuclein, and Tau.Chemical reviews · 2025Review
- Strategies of positron emission tomography (PET) tracer development for imaging of tau and α-synuclein in neurodegenerative disorders.RSC medicinal chemistry · 2025Review
- Isotopologues of potassium 2,2,2-trifluoroethoxide for applications in positron emission tomography and beyond.Nature communications · 2024Article
- Peptidoglycan-Targeted [JACS Au · 2024Article
- Discovery of High-Affinity Amyloid Ligands Using a Ligand-Based Virtual Screening Pipeline.Journal of the American Chemical Society · 2023Article
- The Sensitivity of Tau Tracers for the Discrimination of Alzheimer's Disease Patients and Healthy Controls by PET.Biomolecules · 2023Review
- Fluorine-18: Radiochemistry and Target-Specific PET Molecular Probes Design.Frontiers in chemistry · 2022Review
- Quantitative analysis of regional distribution of tau pathology with 11C-PBB3-PET in a clinical setting.PloS one · 2022Article
- Advances in [Molecules (Basel, Switzerland) · 2021Review
- Clinical Relevance of [Molecules (Basel, Switzerland) · 2021Article
- Synthesis of [ACS chemical neuroscience · 2021Article
- Synthesis and Evaluation of a Fluorine-18 Radioligand for Imaging Huntingtin Aggregates by Positron Emission Tomographic Imaging.Frontiers in neuroscience · 2021Article
- Positron Emission Tomography in Animal Models of Tauopathies.Frontiers in aging neuroscience · 2021Review
- Molecular Imaging of Fluorinated Probes for Tau Protein and Amyloid-β Detection.Molecules (Basel, Switzerland) · 2020Review
- Imaging biomarkers in neurodegeneration: current and future practices.Alzheimer's research & therapy · 2020Review
- Tau-positron emission tomography correlates with neuropathology findings.Alzheimer's & dementia : the journal of the Alzheimer's Association · 2020Article
- PET Radiopharmaceuticals for Alzheimer's Disease and Parkinson's Disease Diagnosis, the Current and Future Landscape.Molecules (Basel, Switzerland) · 2020Review
Corrections and comments
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Authors and funding
13 authors at 1 institution in 1 country.
Funding
Abstract
Abnormally aggregated tau is the hallmark pathology of tauopathy neurodegenerative disorders and is a target for development of both diagnostic tools and therapeutic strategies across the tauopathy disease spectrum. Development of carbon-11- or fluorine-18-labeled radiotracers with appropriate affinity and specificity for tau would allow noninvasive quantification of tau burden using positron emission tomography (PET) imaging. We have synthesized [(18)F]lansoprazole, [(11)C]N-methyl lansoprazole, and [(18)F]N-methyl lansoprazole and identified them as high affinity radiotracers for tau with low to subnanomolar binding affinities. Herein, we report radiosyntheses and extensive preclinical evaluation with the aim of selecting a lead radiotracer for translation into human PET imaging trials. We demonstrate that [(18)F]N-methyl lansoprazole, on account of the favorable half-life of fluorine-18 and its rapid brain entry in nonhuman primates, favorable kinetics, low white matter binding, and selectivity for binding to tau over amyloid, is the lead compound for progression into clinical trials.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.