The polymer supported phosphazene bases PS-P₂(tBu) and the novel PS-P₂(PEG) allowed for efficient extraction of [¹⁸F]F⁻ from proton irradiated [¹⁸O]H₂O and subsequent radiofluorination of a broad range of substrates directly on the resin. The highest radiochemical yields were obtained with aliphatic sulfonates (69%) and bromides (42%); the total radiosynthesis time was 35-45 min. The multivariate analysis showed that the radiochemical yields and purities were controlled by the resin load, reaction temperature, and column packing effects. The resins could be reused several times with the same or different substrates. The fully automated on-column radiofluorination methodology was applied to the radiosynthesis of the important PET radiotracers [¹⁸F]FLT and [¹⁸F]FDG. The latter was produced with 40% yield on a 120 GBq scale and passed GMP-regulated quality control required for commercial production of [1¹⁸F]FDG. The combination of compact form factor, simplicity of [¹⁸F]F⁻ recovery and processing, and column reusability can make solid phase radiofluorination an attractive radiochemistry platform for the emerging dose-on-demand instruments for bedside production of PET radiotracers.
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http://dx.doi.org/10.3390/molecules180910531 | DOI Listing |
Open Heart
January 2025
Department of Cardiology, University Hospital Basel, Basel, Switzerland.
Background: The majority of functional ischemia tests in patients with suspected chronic coronary syndromes (CCS) yield normal results. Implementing gatekeepers for patient preselection, such as pretest probability (PTP) and/or coronary artery calcium score (CACS), could reduce the number of normal scan results, radiation exposure and costs. However, the efficacy and safety of these approaches remain unclear.
View Article and Find Full Text PDFBiomaterials
January 2025
Department of Nuclear Medicine, Xiangya Hospital, Central South University, No. 87 Xiangya Road, Changsha, Hunan, 410008, China; Key Laboratory of Biological Nanotechnology, NHC, No. 87 Xiangya Road, Changsha, Hunan, 410008, China. Electronic address:
Osteoarthritis (OA) is a prevalent and debilitating condition characterized by cartilage destruction and inflammation. Traditional pharmacotherapies for OA are limited by their short-term efficacy and systemic side effects. Radiosynoviorthesis (RSO), involving intra-articular injection of radiopharmaceuticals, has shown promise for OA treatment but is hindered by the toxicity and rapid clearance of radioisotopes.
View Article and Find Full Text PDFMolecules
December 2024
Laboratory of Veterinary Microbiology, Joint Graduate School of Veterinary Medicine, Yamaguchi University, 1677-1 Yoshida, Yamaguchi 753-8511, Japan.
No effective vaccines or treatments are currently available for severe fever with thrombocytopenia syndrome (SFTS), a fatal tick-borne infectious disease caused by the SFTS virus (SFTSV). This study evaluated the potential of In-labeled anti-SFTSV antibodies targeting SFTSV structural proteins as single-photon emission computed tomography (SPECT) imaging agents for the selective visualization of SFTSV-infected sites. This study used nuclear medicine imaging to elucidate the pathology of SFTS and assess its therapeutic efficacy.
View Article and Find Full Text PDFEJNMMI Radiopharm Chem
January 2025
Division of Nuclear Medicine, Department of Biomedical Imaging and Image-Guided Therapy, Medical University of Vienna, Vienna, Austria.
Background: Poly (ADP-ribose) polymerase (PARP) enzymes are crucial for the repair of DNA single-strand breaks and have become key therapeutic targets in homologous recombination-deficient cancers, including prostate cancer. To enable non-invasive monitoring of PARP-1 expression, several PARP-1-targeting positron emission tomography (PET) tracers have been developed. Here, we aimed to preclinically investigate [carbonyl-C]DPQ as an alternative PARP-1 PET tracer as it features a strongly distinct chemotype compared to the frontrunners [F]FluorThanatrace and [F]PARPi.
View Article and Find Full Text PDFIndian J Nucl Med
November 2024
Department of Neuroimaging and Interventional Radiology, National Institute of Mental Health and Neurosciences, Bengaluru, Karnataka, India.
Background: Fluorine-18 (F) flumazenil (FMZ) has been synthesized using various precursors, and its role has been explored in imaging Gamma-aminobutyric acid-A receptors.
Aim And Objective: The main objective was to synthesize (F) FMZ using isotopic substitution.
Materials And Methods: Around 18 ± 2 GBq was added to the module, dried, and radiolabeling was standardized with 3.
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