Radiopharmaceuticals for diagnosis and treatment. Progress report

Technical Report · Tue Dec 01 04:00:00 EST 1992

DOI:https://doi.org/10.2172/10191678· OSTI ID:10191678

Kuhl, D E

We report on our efforts in PET basic radiochemistry, radiopharmaceutical synthesis, and preclinical radiopharmaceutical evaluation. These efforts are focused on three fronts. First predictive abilities in nucleophilic aromatic substitution with [{sup 18}F]fluorination of substituted aromatic rings. Although radiochemical yields can be predicted within a very similar group of compounds with similar leaving groups and substituent patterns, generalization to all nucleophilic substitutions with [{sup 18}F] fluoride is not warranted. Kinetic studies indicate significantly different rates of reactions, depending on ring substituents. Second, preclinical evaluation of new radiopharmaceuticals. We have synthesized and begun the preclinical evaluation of [{sup 11}C]tetrabenazine, a new radioligand based on the vesicular monoamine transport system. Third, our work, on [{sup 18}F]fluorination/decarbonylation reactions, structure-activity relationships in dopamine uptake inhibitors and effects of chronic drugs on radioligand binding is described.

• Research Organization: Michigan Univ., Ann Arbor, MI (United States). Div. of Nuclear Medicine
• Sponsoring Organization: USDOE, Washington, DC (United States)
• DOE Contract Number: FG02-88ER60639
• OSTI ID: 10191678
• Report Number(s): DOE/ER/60639--5; ON: DE93004637
• Country of Publication: United States
• Language: English

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38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
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62 RADIOLOGY AND NUCLEAR MEDICINE
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AROMATICS
BRAIN
CARBON 11
CHEMICAL PREPARATION
FLUORINE 18
IN VIVO
KETONES
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RADIOISOTOPE PRODUCTION
RADIOPHARMACEUTICALS
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UNSEALED RADIONUCLIDES IN DIAGNOSTICS
UNSEALED RADIONUCLIDES IN THERAPY