ArticleScientific reports2016
A Novel PET Imaging Probe for the Detection and Monitoring of Translocator Protein 18 kDa Expression in Pathological Disorders.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 48 citations in OpenAlex.
- Synthesis and evaluation of TSPO-targeting radioligand [Acta pharmaceutica Sinica. B · 2025Article
- Translocator Protein 18 kDa (TSPO): A Promising Molecular Target for Image-Guided Surgery of Solid Cancers.Advanced pharmaceutical bulletin · 2024Review
- Targeting the Translocator Protein (18 kDa) in Cardiac Diseases: State of the Art and Future Opportunities.Journal of medicinal chemistry · 2024Review
- Sigma-2 Receptor Ligand Binding Modulates Association between TSPO and TMEM97.International journal of molecular sciences · 2023Article
- Review
- Essential Principles and Recent Progress in the Development of TSPO PET Ligands for Neuroinflammation Imaging.Current medicinal chemistry · 2022Review
- The 18-kDa Translocator Protein PET Tracers as a Diagnostic Marker for Neuroinflammation: Development and Current Standing.ACS omega · 2022Review
- Novel PET Imaging of Inflammatory Targets and Cells for the Diagnosis and Monitoring of Giant Cell Arteritis and Polymyalgia Rheumatica.Frontiers in medicine · 2022Review
- Radiosynthesis and characterization of [European journal of nuclear medicine and molecular imaging · 2021Article
- Unconventional non-amino acidic PET radiotracers for molecular imaging in gliomas.European journal of nuclear medicine and molecular imaging · 2021Review
- Feasibility of TSPO-Specific Positron Emission Tomography Radiotracer for Evaluating Paracetamol-Induced Liver Injury.Diagnostics (Basel, Switzerland) · 2021Article
- The Pharmaceutical Technology Approach on Imaging Innovations from Italian Research.Pharmaceutics · 2021Review
- A brief review of non-invasive brain imaging technologies and the near-infrared optical bioimaging.Applied microscopy · 2021Review
- Physiological Imaging Methods for Evaluating Response to Immunotherapies in Glioblastomas.International journal of molecular sciences · 2021Review
- Membrane-Mediated Ligand Unbinding of the PK-11195 Ligand from TSPO.Biophysical journal · 2021Article
- A perspective on the radiopharmaceutical requirements for imaging and therapy of glioblastoma.Theranostics · 2021Review
- Dexmedetomidine alleviates LPS‑induced acute lung injury via regulation of the p38/HO‑1 pathway.Molecular medicine reports · 2020Article
- Molecular and Cellular Complexity of Glioma. Focus on Tumour Microenvironment and the Use of Molecular and Imaging Biomarkers to Overcome Treatment Resistance.International journal of molecular sciences · 2020Review
- [Theranostics · 2020Article
- Sleep fragmentation, microglial aging, and cognitive impairment in adults with and without Alzheimer's dementia.Science advances · 2019Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A new fluorine-substituted ligand, compound 1 (CB251), with a very high affinity (Ki = 0.27 ± 0.09 nM) and selectivity for the 18-kDa translocator protein (TSPO), is presented as an attractive biomarker for the diagnosis of neuroinflammation, neurodegeneration and tumour progression. To test compound 1 as a TSPO PET imaging agent in vivo, 2-(2-(4-(2-[(18)F]fluoroethoxy)phenyl)-6,8-dichloroimidazo[1,2-a]pyridin-3-yl)-N,N-dipropylacetamide ([(18)F]1; [(18)F]CB251) was synthesized by nucleophilic aliphatic substitution in a single-step radiolabelling procedure with a 11.1 ± 3.5% (n = 14, decay corrected) radiochemical yield and over 99% radiochemical purity. In animal PET imaging studies, [(18)F]CB251 provided a clearly visible image of the inflammatory lesion with the binding potential of the specifically bound radioligand relative to the non-displaceable radioligand in tissue (BPND 1.83 ± 0.18), in a neuroinflammation rat model based on the unilateral stereotaxic injection of lipopolysaccharide (LPS), comparable to that of [(11)C]PBR28 (BPND 1.55 ± 0.41). [(18)F]CB251 showed moderate tumour uptake (1.96 ± 0.11%ID/g at 1 h post injection) in human glioblastoma U87-MG xenografts. These results suggest that [(18)F]CB251 is a promising TSPO PET imaging agent for neuroinflammation and TSPO-rich cancers.
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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.