Radiopharmaceuticals for diagnosis and treatment. Progress report
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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62 RADIOLOGY AND NUCLEAR MEDICINE
ALDEHYDES
AROMATICS
BRAIN
CARBON 11
CHEMICAL PREPARATION
FLUORINE 18
IN VIVO
KETONES
LABELLING
MICE
NITRILES
NITRO COMPOUNDS
POSITRON COMPUTED TOMOGRAPHY
PRIMATES
PROGRESS REPORT
RADIOISOTOPE PRODUCTION
RADIOPHARMACEUTICALS
TRANQUILIZERS
UNSEALED RADIONUCLIDES IN DIAGNOSTICS
UNSEALED RADIONUCLIDES IN THERAPY