ArticleMolecular imaging and biology2016
Preclinical Evaluation of [(18)F]THK-5105 Enantiomers: Effects of Chirality on Its Effectiveness as a Tau Imaging Radiotracer.
Article in Molecular imaging and biology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Human Radiation Dosimetry of [(18)F]AV-1451(T807) to Detect Tau Pathology.Molecular imaging and biology · 2016Trial
- Tau degradation in Alzheimer's disease: Mechanisms and therapeutic opportunities.Alzheimer's & dementia : the journal of the Alzheimer's Association · 2025Review
- The Sensitivity of Tau Tracers for the Discrimination of Alzheimer's Disease Patients and Healthy Controls by PET.Biomolecules · 2023Review
- Design, Synthesis, and Bioactivity of Novel Bifunctional Small Molecules for Alzheimer's disease.ACS omega · 2022Article
- Chronic traumatic encephalopathy: Diagnostic updates and advances.AIMS neuroscience · 2022Review
- PET Radiopharmaceuticals for Alzheimer's Disease and Parkinson's Disease Diagnosis, the Current and Future Landscape.Molecules (Basel, Switzerland) · 2020Review
- Development of tau PET Imaging Ligands and their Utility in Preclinical and Clinical Studies.Nuclear medicine and molecular imaging · 2018Review
- Imaging Protein Misfolding in the Brain Using β-Sheet Ligands.Frontiers in neuroscience · 2018Review
- The development and validation of tau PET tracers: current status and future directions.Clinical and translational imaging · 2018Review
- Evaluation of the Feasibility of Screening Tau Radiotracers Using an Amyloid Biomathematical Screening Methodology.Computational and mathematical methods in medicine · 2018Article
- Comparative binding properties of the tau PET tracers THK5117, THK5351, PBB3, and T807 in postmortem Alzheimer brains.Alzheimer's research & therapy · 2017Article
- In Vivo Comparison of Tau RadioligandsJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2017Article
- Tau PET imaging: present and future directions.Molecular neurodegeneration · 2017Review
- Comparability of [Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2017Article
- Imaging in-vivo tau pathology in Alzheimer's disease with THK5317 PET in a multimodal paradigm.European journal of nuclear medicine and molecular imaging · 2016Article
Corrections and comments
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeNoninvasive imaging of tau and amyloid-β pathologies would facilitate diagnosis of Alzheimer's disease (AD). Recently, we have developed [(18)F]THK-5105 for selective detection of tau pathology by positron emission tomography (PET). The purpose of this study was to clarify biological properties of optically pure [(18)F]THK-5105 enantiomers. PROCEDURES: Binding for tau aggregates in AD brain section was evaluated by autoradiography (ARG). In vitro binding assays were performed to evaluate the binding properties of enantiomers for AD brain homogenates. The pharmacokinetics in the normal mouse brains was assessed by ex vivo biodistribution assay
resultsThe ARG of enantiomers showed the high accumulation of radioactivity corresponding to the distribution of tau deposits. In vitro binding assays revealed that (S)-[(18)F]THK-5105 has slower dissociation from tau than (R)-[(18)F]THK-5105. Biodistribution assays indicated that (S)-[(18)F]THK-5105 eliminated faster from the mouse brains and blood compared with (R)-[(18)F]THK-5105.
conclusion(S)-[(18)F]THK-5105 could be more suitable than (R)-enantiomer for a tau imaging agent.
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