Abstract
The synthesis and structure-activity relationship of a new class of indole derivatives with low-nanomolar affinity for the SERT and high selectivity versus the 5-HT1A receptor were recently reported. Based on their chemical structure, four new indolylpropylamine derivatives which contain atoms to afford future labeling with PET isotopes, were synthesized and evaluated as SERT ligands. The chemistry of these novel derivatives, their biological evaluation, the general method of preparing the precursor indole for labeling, and the C-11 labeling of the most promising indole derivative, are described herein.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Carbon Radioisotopes / chemistry
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Cell Line
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Humans
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Indoles / chemical synthesis
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Indoles / chemistry*
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Isoquinolines / chemical synthesis
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Isoquinolines / chemistry*
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Isotope Labeling
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Ligands
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Positron-Emission Tomography*
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Propylamines / chemical synthesis
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Propylamines / chemistry*
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Rats
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Rats, Inbred Strains
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Serotonin Plasma Membrane Transport Proteins / analysis*
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Serotonin Plasma Membrane Transport Proteins / blood
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Serotonin Plasma Membrane Transport Proteins / chemistry
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Structure-Activity Relationship
Substances
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2-(3-(5-fluoro-1H-indol-3-yl)-propyl)-6-methoxy-1,2,3,4-tetrahydro-isoquinoline
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Carbon Radioisotopes
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Indoles
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Isoquinolines
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Ligands
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Propylamines
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Serotonin Plasma Membrane Transport Proteins