Positron emitter labeled enzyme inhibitors

Patent · Fri May 22 04:00:00 EDT 1987

OSTI ID:6864415

Fowler, J S; MacGregor, R R; Wolf, A P

This invention involved 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 in activators 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. 2 figs.

• Research Organization: Brookhaven National Lab., Upton, NY (USA)
• DOE Contract Number: AC02-76CH00016
• Assignee: TIC; EDB-88-179699
• Patent Number(s): PATENTS-US-A6052921
• OSTI ID: 6864415
• Country of Publication: United States
• Language: English

Related Subjects

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550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AMINE OXIDASES
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
CARBON 11
CARBON ISOTOPES
CHEMICAL PREPARATION
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
EMISSION COMPUTED TOMOGRAPHY
ENZYME ACTIVITY
ENZYME INHIBITORS
ENZYMES
EVEN-ODD NUCLEI
INVENTIONS
ISOTOPES
LABELLING
LIGHT NUCLEI
MINUTES LIVING RADIOISOTOPES
NUCLEI
ORGANIC COMPOUNDS
OXIDOREDUCTASES
POSITRON COMPUTED TOMOGRAPHY
RADIOISOTOPES
SYNTHESIS
TOMOGRAPHY