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Positron emitter labeled enzyme inhibitors

Patent ·
OSTI ID:867322
 [1];  [2];  [3];  [4]
  1. Bellport, NY
  2. Sag Harbor, NY
  3. Setauket, NY
  4. Upsala, SE
+ Show Author Affiliations

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:
ASSOC UNIVERSITIES INC
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

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Positron emitter labeled enzyme inhibitors
Patent · Tue Apr 03 00:00:00 EDT 1990 · OSTI ID:5664820
Positron emitter labeled enzyme inhibitors
Patent · Fri May 22 00:00:00 EDT 1987 · OSTI ID:6864415
(/sup 11/C)clorgyline and (/sup 11/C)-L-deprenyl and their use in measuring functional monoamine oxidase activity in the brain using positron emission tomography
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Related Subjects

/424/514/999/
active
activity
animal
bound
carbon-11
catalysis
clorgyline
covalently
covalently bound
distribution
emission
emission tomography
emitted
emitter
emitter-labeled
enzymatic
enzyme
enzyme activity
functionally
human
image
imaging
inactivators
inhibit
inhibitors
involves
irreversibly
l-deprenyl
labeled
living
living human
localization
map
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monoamine
obtained
oxidase
penetrating
penetrating radiation
pet
positron
positron emission
positron emitter
probes
produced
provide
radiation
radiation emitted
radioactivity
reactivity
result
selective
strategy
subtypes
suicide
tomography
vivo