Synthesis and biological evaluation of trans-3-phenyl-1-indanamines as potential norepinephrine transporter imaging agents

The development of radioligands suitable for studying the central nervous system (CNS) norepinephrine transporter (NET) in vivo will provide important new tools for examining the pathophysiology and pharmacotherapy of a variety of neuropsychiatric disorders including major depression. Towards this e...

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Bibliographic Details
Published in:Nuclear medicine and biology 2005-08, Vol.32 (6), p.593-605
Main Authors: McConathy, Jonathan, Owens, Michael J., Kilts, Clinton D., Malveaux, Eugene J., Votaw, John R., Nemeroff, Charles B., Goodman, Mark M.
Format: Article
Language:English
Subjects:
Animals
Brain - diagnostic imaging
Brain - metabolism
Carbon-11
Dopamine - metabolism
Humans
Indans - chemical synthesis
Ligands
Macaca mulatta
Male
Metabolic Clearance Rate
Monoamine transporter ligands
Norepinephrine - metabolism
Norepinephrine transporter
Phenylindanamine
Positron emission tomography
Protein Binding
Radiopharmaceuticals - pharmacology
Rats
Rats, Sprague-Dawley
Serotonin - metabolism
Serotonin Plasma Membrane Transport Proteins - metabolism
Species Specificity
Tomography, Emission-Computed - methods
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Summary:The development of radioligands suitable for studying the central nervous system (CNS) norepinephrine transporter (NET) in vivo will provide important new tools for examining the pathophysiology and pharmacotherapy of a variety of neuropsychiatric disorders including major depression. Towards this end, a series of trans-3-phenyl-1-indanamine derivatives were prepared and evaluated in vitro. The biological properties of the most promising compound, [ 11C]3-BrPA, were investigated in rat biodistribution and nonhuman primate PET studies. Despite high in vitro affinity for the human NET, the uptake of [ 11C]3-BrPA in the brain and the heart was not displaceable with pharmacological doses of NET antagonists.
ISSN:0969-8051
1872-9614
DOI:10.1016/j.nucmedbio.2005.04.012