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Title: 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.
Authors:
; ; ;
Publication Date:
OSTI Identifier:
5664820
Report Number(s):
US 4913891; A
PPN: US 7-052921A; TRN: 90-024672
Resource Type:
Patent
Resource Relation:
Patent File Date: 22 May 1987
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; 62 RADIOLOGY AND NUCLEAR MEDICINE; ENZYME INHIBITORS; CHEMICAL COMPOSITION; ENZYMES; INHIBITION; POSITRON COMPUTED TOMOGRAPHY; LABELLED COMPOUNDS; AMINES; BIOCHEMICAL REACTION KINETICS; ENZYME ACTIVITY; COMPUTERIZED TOMOGRAPHY; DIAGNOSTIC TECHNIQUES; EMISSION COMPUTED TOMOGRAPHY; KINETICS; ORGANIC COMPOUNDS; REACTION KINETICS; TOMOGRAPHY 550200* -- Biochemistry; 550601 -- Medicine-- Unsealed Radionuclides in Diagnostics