Abstract
Novel 4-phenyl tetrahydroisoquinolines that inhibit both dopamine and norepinephrine transporters were designed and prepared. In this Letter, we describe the synthesis, in vitro activity and associated structure-activity relationships of this series. We also report the ex vivo NET occupancy of a representative compound, 41.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Dopamine Plasma Membrane Transport Proteins / antagonists & inhibitors
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Dopamine Plasma Membrane Transport Proteins / metabolism
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Dopamine Uptake Inhibitors / chemical synthesis
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Dopamine Uptake Inhibitors / chemistry*
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Dopamine Uptake Inhibitors / metabolism
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Kinetics
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Norepinephrine Plasma Membrane Transport Proteins / antagonists & inhibitors
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Norepinephrine Plasma Membrane Transport Proteins / metabolism
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Protein Binding
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Selective Serotonin Reuptake Inhibitors / chemical synthesis
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Selective Serotonin Reuptake Inhibitors / chemistry
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Selective Serotonin Reuptake Inhibitors / metabolism
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Serotonin Plasma Membrane Transport Proteins / chemistry
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Serotonin Plasma Membrane Transport Proteins / metabolism
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Structure-Activity Relationship
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Tetrahydroisoquinolines / chemical synthesis
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Tetrahydroisoquinolines / chemistry*
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Tetrahydroisoquinolines / metabolism
Substances
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Dopamine Plasma Membrane Transport Proteins
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Dopamine Uptake Inhibitors
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Norepinephrine Plasma Membrane Transport Proteins
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Serotonin Plasma Membrane Transport Proteins
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Serotonin Uptake Inhibitors
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Tetrahydroisoquinolines