ArticleJournal of nuclear medicine : official publication, Society of Nuclear Medicine2012
Quantitative preclinical imaging of TSPO expression in glioma using N,N-diethyl-2-(2-(4-(2-18F-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide.
Article in Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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38 citing papers in PubMed, 61 citations in OpenAlex.
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- Imaging of the glioma microenvironment by TSPO PET.European journal of nuclear medicine and molecular imaging · 2021Review
- Unconventional non-amino acidic PET radiotracers for molecular imaging in gliomas.European journal of nuclear medicine and molecular imaging · 2021Review
- A perspective on the radiopharmaceutical requirements for imaging and therapy of glioblastoma.Theranostics · 2021Review
- Imaging temozolomide-induced changes in the myeloid glioma microenvironment.Theranostics · 2021Article
- TSPO-targeted PET and Optical Probes for the Detection and Localization of Premalignant and Malignant Pancreatic Lesions.Clinical cancer research : an official journal of the American Association for Cancer Research · 2020Article
- Visualization of translocator protein (18 kDa) (TSPO) in the retina of diabetic retinopathy rats using fluorine-18-DPA-714.Annals of nuclear medicine · 2020Article
- N-[Bioorganic & medicinal chemistry letters · 2020Article
- Pyrazoles as Key Scaffolds for the Development of Fluorine-18-Labeled Radiotracers for Positron Emission Tomography (PET).Molecules (Basel, Switzerland) · 2020Review
- Article
- A unified structural model of the mammalian translocator protein (TSPO).Journal of biomolecular NMR · 2019Article
- TSPO-PET and diffusion-weighted MRI for imaging a mouse model of infiltrative human glioma.Neuro-oncology · 2019Article
- Preclinical Evaluation of a Novel TSPO PET Ligand 2-(7-Butyl-2-(4-(2-[Molecular imaging and biology · 2019Article
- TSPO PET for glioma imaging using the novel ligandEuropean journal of nuclear medicine and molecular imaging · 2017Article
- TSPO PET usingEuropean journal of nuclear medicine and molecular imaging · 2017Article
- Evaluation of TSPO PET Ligands [Molecular imaging and biology · 2017Article
- Optimized Translocator Protein Ligand for Optical Molecular Imaging and Screening.Bioconjugate chemistry · 2017Article
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12 authors at 2 institutions in 1 country.
Funding
Abstract
unlabelledThere is a critical need to develop and rigorously validate molecular imaging biomarkers to aid diagnosis and characterization of primary brain tumors. Elevated expression of translocator protein (TSPO) has been shown to predict disease progression and aggressive, invasive behavior in a variety of solid tumors. Thus, noninvasive molecular imaging of TSPO expression could form the basis of a novel, predictive cancer imaging biomarker. In quantitative preclinical PET studies, we evaluated a high-affinity pyrazolopyrimidinyl-based TSPO imaging ligand, N,N-diethyl-2-(2-(4-(2-(18)F-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide ((18)F-DPA-714), as a translational probe for quantification of TSPO levels in glioma.
methodsGlioma-bearing rats were imaged with (18)F-DPA-714 in a small-animal PET system. Dynamic images were acquired simultaneously on injection of (18)F-DPA-714 (130-200 MBq/0.2 mL). Blood was collected to derive the arterial input function (AIF), with high-performance liquid chromatography radiometabolite analysis performed on selected samples for AIF correction. Compartmental modeling was performed using the corrected AIF. Specific tumor cell binding of DPA-714 was evaluated by radioligand displacement of (3)H-PK 11195 with DPA-714 in vitro and displacement of (18)F-DPA-714 with an excess of DPA-714 in vivo. Immediately after imaging, tumor and healthy brain tissues were harvested for validation by Western blotting and immunohistochemistry.
results(18)F-DPA-714 was found to preferentially accumulate in tumors, with modest uptake in the contralateral brain. Infusion with DPA-714 (10 mg/kg) displaced (18)F-DPA-714 binding by greater than 60% on average. Tumor uptake of (18)F-DPA-714 was similar to another high-affinity TSPO imaging ligand, (18)F-N-fluoroacetyl-N-(2,5-dimethoxybenzyl)-2-phenoxyaniline, and agreed with ex vivo assay of TSPO levels in tumor and healthy brain.
conclusionThese studies illustrate the feasibility of using (18)F-DPA-714 for visualization of TSPO-expressing brain tumors. Importantly, (18)F-DPA-714 appears suitable for quantitative assay of tumor TSPO levels in vivo. Given the relationship between elevated TSPO levels and poor outcome in oncology, these studies suggest the potential of (18)F-DPA-714 PET to serve as a novel predictive cancer imaging modality.
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