ArticleACS medicinal chemistry letters2012
Evaluation of [(11)C]N-Methyl Lansoprazole as a Radiopharmaceutical for PET Imaging of Tau Neurofibrillary Tangles.
Article in ACS medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 57 citations in OpenAlex.
- 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
- The Sensitivity of Tau Tracers for the Discrimination of Alzheimer's Disease Patients and Healthy Controls by PET.Biomolecules · 2023Review
- 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
- Evaluation of [ACS chemical neuroscience · 2020Article
- Development of Positron Emission Tomography Radiotracers for the GABA Transporter 1.ACS chemical neuroscience · 2018Article
- Image-Guided Development of Heterocyclic Sulfoxides as Ligands for Tau Neurofibrillary Tangles: From First-in-Man to Second-Generation Ligands.ACS omega · 2018Article
- Development of tau PET Imaging Ligands and their Utility in Preclinical and Clinical Studies.Nuclear medicine and molecular imaging · 2018Review
- New protein deposition tracers in the pipeline.EJNMMI radiopharmacy and chemistry · 2017Review
- Characteristics of Tau and Its Ligands in PET Imaging.Biomolecules · 2016Review
- Untangling tau imaging.Alzheimer's & dementia (Amsterdam, Netherlands) · 2016Review
- Comparison of New Tau PET-Tracer Candidates With [18F]T808 and [18F]T807.Molecular imaging · 2016Article
- PET Radioligands for Imaging of Tau Pathology: Current Status.Nuclear medicine and molecular imaging · 2015Review
- Synthesis and evaluation of [MedChemComm · 2015Article
- Novel PET/SPECT probes for imaging of tau in Alzheimer's disease.TheScientificWorldJournal · 2015Review
- 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.ACS chemical neuroscience · 2014Article
- Synthesis and evaluation of [(11)C]PyrATP-1, a novel radiotracer for PET imaging of glycogen synthase kinase-3β (GSK-3β).Nuclear medicine and biology · 2014Article
- In vivo evaluation of a novel tau imaging tracer for Alzheimer's disease.European journal of nuclear medicine and molecular imaging · 2014Article
- Radiosyntheses using fluorine-18: the art and science of late stage fluorination.Current topics in medicinal chemistry · 2014Review
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11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
[(11)C]N-Methyl lansoprazole ([(11)C]NML, 3) was synthesized and evaluated as a radiopharmaceutical for quantifying tau neurofibrillary tangle (NFT) burden using positron emission tomography (PET) imaging. [(11)C]NML was synthesized from commercially available lansoprazole in 4.6% radiochemical yield (noncorrected RCY, based upon [(11)C]MeI), 99% radiochemical purity, and 16095 Ci/mmol specific activity (n = 5). Log P was determined to be 2.18. A lack of brain uptake in rodent microPET imaging revealed [(11)C]NML to be a substrate for the rodent permeability-glycoprotein 1 (PGP) transporter, but this could be overcome by pretreating with cyclosporin A to block the PGP. Contrastingly, [(11)C]NML was not found to be a substrate for the primate PGP, and microPET imaging in rhesus revealed [(11)C]NML uptake in the healthy primate brain of ∼1600 nCi/cc maximum at 3 min followed by rapid egress to 500 nCi/cc. Comparative autoradiography between wild-type rats and transgenic rats expressing human tau (hTau +/+) revealed 12% higher uptake of [(11)C]NML in the cortex of brains expressing human tau. Further autoradiography with tau positive brain samples from progressive supranuclear palsy (PSP) patients revealed colocalization of [(11)C]NML with tau NFTs identified using modified Bielschowsky staining. Finally, saturation binding experiments with heparin-induced tau confirmed K d and Bmax values of [(11)C]NML as 700 pM and 0.214 fmol/μg, respectively.
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