ArticleArthritis research & therapy2014
Promising potential of new generation translocator protein tracers providing enhanced contrast of arthritis imaging by positron emission tomography in a rat model of arthritis.
Article in Arthritis research & therapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers, 1 of them a synthesis that pooled it.
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Who cites it
20 citing papers in PubMed, 1 synthesis or guideline pooled it, 43 citations in OpenAlex.
- Synovial Macrophages: Past Life, Current Situation, and Application in Inflammatory Arthritis.Frontiers in immunology · 2022Pooled it
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- PET-MRI: The promise of multi-tissue imaging of early disease mechanisms in osteoarthritis.Osteoarthritis and cartilage · 2025Article
- Evaluation ofJournal of clinical medicine · 2022Article
- Evaluation of [Molecular imaging and biology · 2022Article
- Imaging of Synovial Inflammation in Osteoarthritis, From theAJR. American journal of roentgenology · 2022Review
- Assessing organ-level immunoreactivity in a rat model of sepsis using TSPO PET imaging.Frontiers in immunology · 2022Article
- LongitudinalFrontiers in chemistry · 2022Article
- EANM recommendations based on systematic analysis of small animal radionuclide imaging in inflammatory musculoskeletal diseases.EJNMMI research · 2021Article
- Preclinical Evaluation of a NovelACS omega · 2020Article
- Specificity of translocator protein-targeted positron emission tomography in inflammatory joint disease.EJNMMI research · 2020Article
- Quantitative Assessment of Arthritis Activity in Rheumatoid Arthritis Patients Using [International journal of molecular sciences · 2020Article
- Pyrazoles as Key Scaffolds for the Development of Fluorine-18-Labeled Radiotracers for Positron Emission Tomography (PET).Molecules (Basel, Switzerland) · 2020Review
- The folate receptor β as a macrophage-mediated imaging and therapeutic target in rheumatoid arthritis.Drug delivery and translational research · 2019Review
- Imaging and Methotrexate Response Monitoring of Systemic Inflammation in Arthritic Rats Employing the Macrophage PET Tracer [Contrast media & molecular imaging · 2018Article
- TSPO PET Imaging: From Microglial Activation to Peripheral Sterile Inflammatory Diseases?Contrast media & molecular imaging · 2017Review
- The macrophage marker translocator protein (TSPO) is down-regulated on pro-inflammatory 'M1' human macrophages.PloS one · 2017Article
- 68Ga-DOTA-Siglec-9--a new imaging tool to detect synovitis.Arthritis research & therapy · 2015Article
- Mapping neuroinflammation in frontotemporal dementia with molecular PET imaging.Journal of neuroinflammation · 2015Review
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9 authors at 2 institutions in 3 countries.
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No grant is acknowledged in the PubMed record.
Abstract
introductionEarly diagnosis of and subsequent monitoring of therapy for rheumatoid arthritis (RA) could benefit from detection of (sub)clinical synovitis. Imaging of (sub)clinical arthritis by targeting the translocator protein (TSPO) on activated macrophages is feasible using (R)-[¹¹C] PK11195-based positron emission tomography (PET), but clinical applications are limited by background uptake in peri-articular bone/bone marrow. The purpose of the present study was to evaluate two other TSPO ligands with potentially lower background uptake in neurological studies, [¹¹C]DPA-713 and [¹⁸F]DPA-714, in a rat model of arthritis.
methodsTSPO binding of DPA-713, DPA-714 and PK11195 were assessed by in vitro competition studies with [³H]DPA-713 using human macrophage THP-1 cells and CD14⁺ monocytes from healthy volunteers. In vivo studies were performed in rats with methylated bovine serum albumin-induced knee arthritis. Immunohistochemistry with anti-TSPO antibody was performed on paraffin-embedded sections. Rats were imaged with [¹¹C]DPA-713 or [¹⁸F]DPA-714 PET, followed by ex vivo tissue distribution studies. Results were compared with those obtained with the tracer (R)-[¹¹C]PK11195, the established ligand for TSPO.
resultsIn THP-1 cells, relative TSPO binding of DPA-713 and DPA-714 were 7-fold and 25-fold higher, respectively, than in PK11195. Comparable results were observed in CD14⁺ monocytes from healthy volunteers. In the arthritis rat model, immunohistochemistry confirmed the presence of TSPO-positive inflammatory cells in the arthritic knee. PET images showed that uptake of [¹¹C]DPA-713 and [¹⁸F]DPA-714 in arthritic knees was significantly increased compared with contralateral knees and knees of normal rats. Uptake in arthritic knees could be largely blocked by an excess of PK11195. [¹¹C]DPA-713 and [¹⁸F]DPA-714 provided improved contrast compared with (R)-[¹¹C]PK11195, as was shown by significantly higher arthritic knee-to-bone ratios of [¹¹C]DPA-713 (1.60 ± 0.31) and [¹⁸F]DPA-714 (1.55 ± 0.10) compared with (R)-[¹¹C]PK11195 (1.14 ± 0.19).
conclusions[¹¹C]DPA-713 and [¹⁸F]DPA-714 clearly visualized arthritis and exhibited lower (peri-articular) bone/bone marrow uptake than (R)-[¹¹C]PK11195. These features merit further investigation of these tracers for early diagnosis and therapy monitoring of RA in a clinical setting.
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