Positron emitter labeled enzyme inhibitors

Patent · Fri May 22 00:00:00 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 Laboratory (BNL), Upton, NY (United States)
• DOE Contract Number: AC02-76CH00016
• Assignee: TIC; EDB-88-179699
• Patent Number(s): PATENTS-US-A6052921
• OSTI ID: 6864415
• Resource Relation: Other Information: Portions of this document are illegible in microfiche products
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
AMINE OXIDASES
ENZYME INHIBITORS
ENZYME ACTIVITY
DISTRIBUTION
LABELLING
CARBON 11
CHEMICAL PREPARATION
INVENTIONS
ORGANIC COMPOUNDS
POSITRON COMPUTED TOMOGRAPHY
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
CARBON ISOTOPES
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
EMISSION COMPUTED TOMOGRAPHY
ENZYMES
EVEN-ODD NUCLEI
ISOTOPES
LIGHT NUCLEI
MINUTES LIVING RADIOISOTOPES
NUCLEI
OXIDOREDUCTASES
RADIOISOTOPES
SYNTHESIS
TOMOGRAPHY
550201* - Biochemistry- Tracer Techniques
550200 - Biochemistry