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Title: Positron emitter labeled enzyme inhibitors

Abstract

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.

Inventors:
 [1];  [2];  [3];  [4]
  1. Bellport, NY
  2. Sag Harbor, NY
  3. Setauket, NY
  4. Upsala, SE
Issue Date:
Research Org.:
ASSOC UNIVERSITIES INC
OSTI Identifier:
867322
Patent Number(s):
4913891
Assignee:
United States of America as represented by United States (Washington, DC)
DOE Contract Number:  
AC02-76CH00016
Resource Type:
Patent
Country of Publication:
United States
Language:
English
Subject:
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; /424/514/999/

Citation Formats

Fowler, Joanna S, MacGregor, Robert R, Wolf, Alfred P, and Langstrom, Bengt. Positron emitter labeled enzyme inhibitors. United States: N. p., 1990. Web.
Fowler, Joanna S, MacGregor, Robert R, Wolf, Alfred P, & Langstrom, Bengt. Positron emitter labeled enzyme inhibitors. United States.
Fowler, Joanna S, MacGregor, Robert R, Wolf, Alfred P, and Langstrom, Bengt. Mon . "Positron emitter labeled enzyme inhibitors". United States. https://www.osti.gov/servlets/purl/867322.
@article{osti_867322,
title = {Positron emitter labeled enzyme inhibitors},
author = {Fowler, Joanna S and MacGregor, Robert R and Wolf, Alfred P and Langstrom, Bengt},
abstractNote = {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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1990},
month = {1}
}

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