Abstract
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, [(11)C]3-BrPA, were investigated in rat biodistribution and nonhuman primate PET studies. Despite high in vitro affinity for the human NET, the uptake of [(11)C]3-BrPA in the brain and the heart was not displaceable with pharmacological doses of NET antagonists.
Publication types
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Comparative Study
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Brain / diagnostic imaging*
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Brain / metabolism*
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Dopamine / metabolism
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Humans
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Indans / chemical synthesis*
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Ligands*
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Macaca mulatta
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Male
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Metabolic Clearance Rate
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Norepinephrine / metabolism
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Protein Binding
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Radiopharmaceuticals / pharmacology
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Rats
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Rats, Sprague-Dawley
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Serotonin / metabolism
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Serotonin Plasma Membrane Transport Proteins / metabolism*
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Species Specificity
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Tomography, Emission-Computed / methods
Substances
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Indans
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Ligands
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Radiopharmaceuticals
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SLC6A4 protein, human
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Serotonin Plasma Membrane Transport Proteins
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Serotonin
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Dopamine
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Norepinephrine