Radiopharmaceuticals for diagnosis. Final report
In the period 1969-1986, this project was directed to the evolution of target-specific labeled chemicals useful for nuclear medical imaging, especially radioactive indicators suited to tracing adrenal functions and localizing tumors in the neuroendocrine system. Since 1986, this project research has focused on the chemistry of positron emission tomography (PET) ligands. This project has involved the evaluation of methods for radiochemical syntheses with fluorine-18, as well as the development and preliminary evaluation of new radiopharmaceuticals for positron emission tomography. In the radiochemistry area, the ability to predict fluorine-18 labeling yields for aromatic substitution reactions through the use of carbon-13 NMR analysis was studied. Radiochemical yields can be predicted for some structurally analogous aromatic compounds, but this correlation could not be generally applied to aromatic substrates for this reaction, particularly with changes in ring substituents or leaving groups. Importantly, certain aryl ring substituents, particularly methyl groups, appeared to have a negative effect on fluorination reactions. These observations are important in the future design of syntheses of complicated organic radiopharmaceuticals. In the radiopharmaceutical area, this project has supported the development of a new class of radiopharmaceuticals based on the monoamine vesicular uptake systems. The new radioligands, based on the tetrabenazine structure, offer a new approach to the quantification of monoaminergic neurons in the brain. Preliminary primate imaging studies support further development of these radioligands for PET studies in humans. If successful, such radiopharmaceuticals will find application in studies of the causes and treatment of neurodegenerative disorders such as Parkinson`s disease.
- Research Organization:
- Michigan Univ., Ann Arbor, MI (United States)
- Sponsoring Organization:
- USDOE, Washington, DC (United States)
- DOE Contract Number:
- FG02-88ER60639
- OSTI ID:
- 10191935
- Report Number(s):
- DOE/ER/60639--6; ON: DE95002200
- Country of Publication:
- United States
- Language:
- English
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62 RADIOLOGY AND NUCLEAR MEDICINE
ADRENAL GLANDS
DIAGNOSIS
DYNAMIC FUNCTION STUDIES
EXTERNAL RADIATION IN DIAGNOSTICS
FLUORINATION
FLUORINE 18
LIGANDS
NERVOUS SYSTEM DISEASES
NUCLEAR MEDICINE
POSITRON COMPUTED TOMOGRAPHY
RADIOCHEMISTRY
RADIOISOTOPE PRODUCTION
RADIOPHARMACEUTICALS
UNSEALED RADIONUCLIDES IN DIAGNOSTICS