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Title: 4-fluoroalkyl-3-halophenyl nortropanes

Abstract

A series of compounds in the 4-fluoroalkyl-3-halophenyl nortropanes family are described as diagnostic and therapeutic agents for diseases associated with serotonin transporter dysfunction. These compounds bind to serotonin transporter protein with high affinity and selectivity. The invention provides methods of synthesis which incorporate radioisotopic halogens at a last step which permit high radiochemical yield and maximum usable product life. The radiolabeled compounds of the invention are useful as imaging agents for visualizing the location and density of serotonin transporter by PET and SPECT imaging.

Inventors:
 [1];  [2]
  1. Atlanta, GA
  2. Indianapolis, IN
Issue Date:
Research Org.:
Oak Ridge National Lab. (ORNL), Oak Ridge, TN (United States)
OSTI Identifier:
874483
Patent Number(s):
6399042
Application Number:
10/558916
Assignee:
Emory University (Atlanta, GA)
Patent Classifications (CPCs):
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07D - HETEROCYCLIC COMPOUNDS
DOE Contract Number:  
FG02-97ER62367
Resource Type:
Patent
Country of Publication:
United States
Language:
English
Subject:
4-fluoroalkyl-3-halophenyl; nortropanes; series; compounds; family; described; diagnostic; therapeutic; agents; diseases; associated; serotonin; transporter; dysfunction; bind; protein; affinity; selectivity; provides; methods; synthesis; incorporate; radioisotopic; halogens; step; permit; radiochemical; yield; maximum; usable; product; life; radiolabeled; useful; imaging; visualizing; location; density; pet; provides methods; therapeutic agent; /424/999/

Citation Formats

Goodman, Mark M, and Chen, Ping. 4-fluoroalkyl-3-halophenyl nortropanes. United States: N. p., 2002. Web.
Goodman, Mark M, & Chen, Ping. 4-fluoroalkyl-3-halophenyl nortropanes. United States.
Goodman, Mark M, and Chen, Ping. Tue . "4-fluoroalkyl-3-halophenyl nortropanes". United States. https://www.osti.gov/servlets/purl/874483.
@article{osti_874483,
title = {4-fluoroalkyl-3-halophenyl nortropanes},
author = {Goodman, Mark M and Chen, Ping},
abstractNote = {A series of compounds in the 4-fluoroalkyl-3-halophenyl nortropanes family are described as diagnostic and therapeutic agents for diseases associated with serotonin transporter dysfunction. These compounds bind to serotonin transporter protein with high affinity and selectivity. The invention provides methods of synthesis which incorporate radioisotopic halogens at a last step which permit high radiochemical yield and maximum usable product life. The radiolabeled compounds of the invention are useful as imaging agents for visualizing the location and density of serotonin transporter by PET and SPECT imaging.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {2002},
month = {1}
}

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Works referenced in this record:

Synthesis of radiolabeled inhibitors of presynaptic monoamine uptake systems; [18F]GBR 13119 (DA),[11C]nisoxetine (NE), and [11C]fluoxetine (5-HT)
journal, January 1989


Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships
journal, August 1987


3β-(4-Ethyl-3-iodophenyl)nortropane-2β- carboxylic Acid Methyl Ester as a High-Affinity Selective Ligand for the Serotonin Transporter
journal, November 1997


Synthesis of a radiotracer for studying serotonin uptake sites with positron emission tomography: [11C]McN-5652-Z
journal, October 1992


Radiosynthesis and evaluation of N-(3-[18F]fluoropropyl)paroxetine as a radiotracer for in vivo labeling of serotonin uptake sites by PET
journal, January 1991

  • Suehiro, Makiko; Wilson, Alan A.; Scheffel, Ursula
  • International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology, Vol. 18, Issue 7
  • https://doi.org/10.1016/0883-2897(91)90019-H

Citalopram: Labelling with carbon-11 and evaluation in rat as a potential radioligand for in vivo PET studies of 5-HT re-uptake sites
journal, January 1991