The main focus of this report is the MR spectroscopy of the changes in the concentration of fluorine labeled photosensitizer that occur following the IP administration. This process is studied by (19)F in vivo MR methodology in a murine tumor model. The animal model used in these studies was mice bearing radiation induced fibrosarcoma (RIF) tumor on the foot dorsum. The mice were injected with a solution of approximately 100 micro-moles of the fluorinated photosensitizer and the (19)F MR examination of the photosensitizer in the tumor or the muscle was performed. The pharmacokinetic (PK) profile for each labeled compound was generated using the (19)F MR data at various time points post photosensitizer administration. The pharmacokinetic parameters were analyzed and the relationship of these results to photodynamic therapy is discussed. The (19)F MR methods clearly demonstrate utility in measuring the pharmacokinetic profiles and provide a new approach in the evaluation of appropriate photosensitizers for use in preclinical mammalian systems.
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http://dx.doi.org/10.2174/157016307781483423 | DOI Listing |
Background: Different PET tracers can be used to measure neuritic amyloid plaque deposition in human brain. While mean cortical-to-cerebellar standard uptake value ratios (SUVRs) generated using different radiotracer methods can be transformed into Centiloid measurements to facilitate comparisons among the resulting amyloid plaque measurements, the level of agreement as measured by the strength of the correlation between the measurements does not change. In this study, paired 18F-labeled (i.
View Article and Find Full Text PDFJ Med Chem
January 2025
Gordon Center for Medical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Boston, Massachusetts 02114, United States.
Carfentanil, a highly potent synthetic opioid, paradoxically serves as a crucial positron emission tomography (PET) imaging tool in neurobiological studies of the mu-opioid receptor (MOR) system when labeled with carbon-11 ([C]CFN). However, its clinical research use is hindered by extreme potency and the limited availability of short-lived carbon-11 ( = 20.4 min).
View Article and Find Full Text PDFPharmaceuticals (Basel)
December 2024
N. P. Bechtereva Institute of the Human Brain, Russian Academy of Sciences, 197022 St. Petersburg, Russia.
-succinimidyl-[F]fluorobenzoate ([F]SFB) is commonly prepared through a three-step procedure starting from [F]fluoride ion. A number of methods for the single-step radiosynthesis of [F]SFB have been introduced recently, including the radiofluorination of diaryliodonium salts and the Cu-mediated F-fluorination of pinacol aryl boronates and aryl tributyl stannanes, but they still have the drawbacks of lengthy product purification procedures. In the present work, two approaches for the direct labeling of [F]SFB from diaryliodonium (DAI) salt () and pinacol aryl boronate () are evaluated, with a major focus on developing a fast and simple SPE-based purification procedure.
View Article and Find Full Text PDFAppl Radiat Isot
December 2024
Department of Isotope Application Research, National Atomic Research Institute, Taoyuan City, Taiwan, ROC.
Histone deacetylase 6 (HDAC6) is an enzyme crucial in epigenetic regulation and protein degradation, with implications in various cancers and neurodegenerative disorders. While HDAC6 is recognized as a promising therapeutic target for Parkinson's and Alzheimer's diseases, its involvement in spinocerebellar ataxias (SCAs) remains underexplored. Currently, there are no direct methods available for characterizing HDAC6 in the brains of living subjects.
View Article and Find Full Text PDFACS Chem Neurosci
January 2025
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, 10 Center Drive, Bethesda, Maryland 20892, United States.
Receptor interacting protein kinase 1 (RIPK1) crucially upregulates necroptosis and is a key driver of inflammation. An effective PET radioligand for imaging brain RIPK1 would be useful for further exploring the role of this enzyme in neuroinflammation and for assisting drug discovery. Here, we report our progress on developing a PET radioligand for RIPK1 based on the phenyl-1-dihydropyrazole skeleton of a lead RIPK1 inhibitor, GSK'963.
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