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:
-
- Bellport, NY
- Sag Harbor, NY
- Setauket, NY
- Upsala, SE
- Issue Date:
- Research Org.:
- Associated Universities, Inc., Upton, NY (United States)
- OSTI Identifier:
- 867322
- Patent Number(s):
- 4913891
- Assignee:
- United States of America as represented by United States (Washington, DC)
- Patent Classifications (CPCs):
-
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
- 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 = {Mon Jan 01 00:00:00 EST 1990},
month = {Mon Jan 01 00:00:00 EST 1990}
}