Purpose: N-benzyl-N-methyl-2-[7, 8-dihydro-7-(2-[F] fluoroethyl) -8-oxo-2-phenyl-9H-purin-9-yl] acetamide ([F] FEDAC) is a novel positron emission tomography (PET) tracer that targets the translocator protein (TSPO; 18 kDa) in the mitochondrial outer membrane, which is known to be upregulated in various diseases such as malignant tumors, neurodegenerative diseases, and neuroinflammation. This study presents the first attempt to use [F]FEDAC PET/CT and evaluate its biodistribution as well as the systemic radiation exposure to the radiotracer in humans.
Materials And Methods: Seventeen whole-body [F]FEDAC PET/CT (injected dose, 209.1 ± 6.2 MBq) scans with a dynamic scan of the upper abdomen were performed in seven participants. Volumes of interest were assigned to each organ, and a time-activity curve was created to evaluate the biodistribution of the radiotracer. The effective dose was calculated using IDAC-Dose 2.1.
Results: Immediately after the intravenous injection, the radiotracer accumulated significantly in the liver and was subsequently excreted into the gastrointestinal tract through the biliary tract. It also showed high levels of accumulation in the kidneys, but showed minimal migration to the urinary bladder. Thus, the liver was the principal organ that eliminated [F] FEDAC. Accumulation in the normal brain tissue was minimal. The effective dose estimated from biodistribution in humans was 19.47 ± 1.08 µSv/MBq, and was 3.60 mSV for 185 MBq dose.
Conclusion: [F]FEDAC PET/CT provided adequate image quality at an acceptable effective dose with no adverse effects. Therefore, [F]FEDAC may be useful in human TSPO-PET imaging.
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http://dx.doi.org/10.1007/s12149-023-01895-0 | DOI Listing |
Ann Nucl Med
April 2024
Department of Radiology, Keio University School of Medicine, 35 Shinanomachi, Shinjuku-Ku, Tokyo, 160-8582, Japan.
Atherosclerosis
October 2021
Department of Pathology, Faculty of Medicine, University of Miyazaki, 889-1692, 5200, Kihara, Kiyotake, Miyazaki City, Miyazaki, Japan.
Background And Aims: This study aimed to investigate whether N-benzyl-N-methyl-2-[7,8-dihydro-7-(2-[F]fluoroethyl)-8-oxo-2-phenyl-9H-purin-9-yl]acetamide (F-FEDAC), a probe for translocator protein (TSPO), can visualize atherosclerotic lesions in rabbits and whether TSPO is localized in human coronary plaques.
Methods: F-FEDAC-PET of a rabbit model of atherosclerosis induced by a 0.5% cholesterol diet and balloon injury of the left carotid artery (n = 7) was performed eight weeks after the injury.
Ann Nucl Med
August 2021
Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, 68 Changle Road, Nanjing, 210006, China.
Background: This study aimed to evaluate the biodistribution and kinetics of [F]FEDAC targeting the translocator protein TSPO in the myocardium, and to explore its use for the identification of mitochondrial dysfunction. We also assessed the feasibility of [18F]FEDAC for the early detection of mitochondrial dysfunction associated with myocardial ischemia (MI).
Methods: The radiochemical purity and stability of [F]FEDAC were analyzed by radio-high-performance liquid chromatography (radio-HPLC).
Appl Radiat Isot
March 2021
Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-855, Japan.
Recently, a straightforward one-pot method for F-fluoroethylation without azeotropic drying of cyclotron-produced [F]F was developed. In this study, we have attempted to simplify the automated radiosynthesis of two [F]fluoroethylated tracers, [F]FEDAC and [F]FET, using a desmethyl labeling precursor and [F]fluoroethyl tosylate, based on the above-mentioned method. The radiochemical yields of [F]FEDAC and [F]FET were 26 ± 3.
View Article and Find Full Text PDFStem Cells Transl Med
April 2020
Department of Physiology, Keio University School of Medicine, Tokyo, Japan.
Transplantation of human-induced pluripotent stem cell-derived neural stem/progenitor cells (hiPSC-NS/PCs) is a promising treatment for a variety of neuropathological conditions. Although previous reports have indicated the effectiveness of hiPSC-NS/PCs transplantation into the injured spinal cord of rodents and nonhuman primates, long-term observation of hiPSC-NS/PCs post-transplantation suggested some "unsafe" differentiation-resistant properties, resulting in disordered overgrowth. These findings suggest that, even if "safe" NS/PCs are transplanted into the human central nervous system (CNS), the dynamics of cellular differentiation of stem cells should be noninvasively tracked to ensure safety.
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