Positron emitter labeled enzyme inhibitors
This invention involves a new strategy for imaging and mapping enzyme activity in the living human and animal body using positron emitter-labeled suicide enzyme inactivators or inhibitors which become covalently bound to the enzyme as a result of enzymatic catalysis. Two such suicide inactivators for monoamine oxidase have been labeled with carbon-11 and used to map the enzyme subtypes in the living human and animal body using PET. By using positron emission tomography to image the distribution of radioactivity produced by the body penetrating radiation emitted by carbon-11, a map of functionally active monoamine oxidase activity is obtained. Clorgyline and L-deprenyl are suicide enzyme inhibitors and irreversibly inhibit monoamine oxidase. When these inhibitors are labeled with carbon-11 they provide selective probes for monoamine oxidase localization and reactivity in vivo using positron emission tomography.
- Assignee:
- Dept. of Energy, Washington, DC
- Patent Number(s):
- A; US 4913891
- Application Number:
- PPN: US 7-052921A
- OSTI ID:
- 5664820
- Country of Publication:
- United States
- Language:
- English
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Positron emitter labeled enzyme inhibitors
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Related Subjects
550601 -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AMINES
BIOCHEMICAL REACTION KINETICS
CHEMICAL COMPOSITION
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
EMISSION COMPUTED TOMOGRAPHY
ENZYME ACTIVITY
ENZYME INHIBITORS
ENZYMES
INHIBITION
KINETICS
LABELLED COMPOUNDS
ORGANIC COMPOUNDS
POSITRON COMPUTED TOMOGRAPHY
REACTION KINETICS
TOMOGRAPHY