The purpose of this study was to synthesize a fluorine-18 labeled, highly selective aldosterone synthase (CYP11B2) inhibitor, [F]AldoView, and to assess its potential for the detection of aldosterone-producing adenomas (APAs) with positron emission tomography in patients with primary hyperaldosteronism (PHA). Using dibenzothiophene sulfonium salt chemistry, [F]AldoView was obtained in high radiochemical yield in one step from [F]fluoride. In mice, the tracer showed a favorable pharmacokinetic profile, including rapid distribution and clearance.
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May 2021
Background: The translocator protein 18 kDa is recognised as an important biomarker for neuroinflammation due to its soaring expression in microglia. This process is common for various neurological disorders. DPA-714 is a potent TSPO-specific ligand which found its use in Positron Emission Tomography following substitution of fluorine-19 with fluorine-18, a positron-emitting radionuclide.
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