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Title: 4-haloethenylphenyl tropane:serotonin transporter imaging agents

Patent ·
OSTI ID:1175203
;

A series of compounds in the 4-fluoroalkyl-3-halophenyl nortropanes and 4-haloethenylphenyl tropane families 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:
Emory Univ., Atlanta, GA (United States)
Sponsoring Organization:
USDOE
DOE Contract Number:
FG02-97ER62367
Assignee:
Emory University (Atlanta, GA)
Patent Number(s):
6,843,979
Application Number:
09/974,729
OSTI ID:
1175203
Country of Publication:
United States
Language:
English

References (8)

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
Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: potential positron emission tomography (PET) imaging agents for the dopamine transporter journal December 2001
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

37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY