Positron emitter labeled enzyme inhibitors

Patent · Mon Jan 01 00:00:00 EST 1990

OSTI ID:867322

Fowler, Joanna S ^[1]; MacGregor, Robert R ^[2]; Wolf, Alfred P ^[3]; Langstrom, Bengt ^[4]

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1. Bellport, NY
2. Sag Harbor, NY
3. Setauket, NY
4. Upsala, SE

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.

• Research Organization: Associated Universities, Inc., Upton, NY (United States)
• DOE Contract Number: AC02-76CH00016
• Assignee: United States of America as represented by United States (Washington, DC)
• Patent Number(s): US 4913891
• OSTI ID: 867322
• Country of Publication: United States
• Language: English

Related Subjects

positron
emitter
labeled
enzyme
inhibitors
involves
strategy
imaging
mapping
activity
living
human
animal
emitter-labeled
suicide
inactivators
covalently
bound
result
enzymatic
catalysis
monoamine
oxidase
carbon-11
map
subtypes
pet
emission
tomography
image
distribution
radioactivity
produced
penetrating
radiation
emitted
functionally
active
obtained
clorgyline
l-deprenyl
irreversibly
inhibit
provide
selective
probes
localization
reactivity
vivo
enzyme activity
covalently bound
penetrating radiation
emission tomography
positron emission
radiation emitted
positron emitter
living human
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