Robert R Macgregor

US Patent:

H74, Jun 3, 1986

Filed:

Feb 24, 1983

Appl. No.:

6/469597

Inventors:

Piero A. Salvadori - Pisa, IT
Alfred P. Wolf - Setauket NY
Joanna S. Fowler - Bellport NY
Robert R. MacGregor - Sag Harbor NY

Assignee:

The United States of America as represented by The United States
Department of Energy

International Classification:

C07H 100
C07H 502
C07H 500

US Classification:

536124

Abstract:

Process for the production of 2-deoxy-2-fluoro-D-glucose and the corresponding. sup. 18 F-compound by the reaction of acetyl hypofluorite or the corresponding. sup. 18 F-compound with 3,4,6-tri-O-acetyl-D-glucal followed by hydrolysis. Process includes the production of the hypofluorite compound at ambient temperature.

US Patent:

49138910, Apr 3, 1990

Filed:

May 22, 1987

Appl. No.:

7/052921

Inventors:

Joanna S. Fowler - Bellport NY
Robert R. MacGregor - Sag Harbor NY
Alfred P. Wolf - Setauket NY
Bengt Langstrom - Upsala, SE

Assignee:

The United States of America as represented by the United States
Department of Energy - Washington DC

International Classification:

A61K 4902
A61K 31135
C07C 9306
C07C 8728

US Classification:

424 11

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.