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Title: 4-fluoroalkyl-3-halophenyl nortropanes

Patent ·
OSTI ID:874483
 [1];  [2]
  1. Atlanta, GA
  2. Indianapolis, IN
+ Show Author Affiliations

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.

Research Organization:
Oak Ridge National Laboratory (ORNL), Oak Ridge, TN (United States)
DOE Contract Number:
FG02-97ER62367
Assignee:
Emory University (Atlanta, GA)
Patent Number(s):
US 6399042
Application Number:
10/558916
OSTI ID:
874483
Country of Publication:
United States
Language:
English

References (7)

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
Synthesis and Transporter Binding Properties of 3β-(4‘-Alkyl-, 4‘-alkenyl-, and 4‘-alkynylphenyl)nortropane-2β-carboxylic Acid Methyl Esters:  Serotonin Transporter Selective Analogs journal January 1996
Radiosynthesis and evaluation of N-(3-[18F]fluoropropyl)paroxetine as a radiotracer for in vivo labeling of serotonin uptake sites by PET
  • 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
journal January 1991
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

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Related Subjects

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/