Abstract
Further exploration around the recently disclosed potent triple re-uptake inhibitor 6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane led to the identification of a new series of potent triple re-uptake inhibitors endowed with good developability characteristics. The insertion of a further aryl moiety into the template allowed the 'titration' of the SERT/NET/DAT ratio leading to the identification of further tools in this important area.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Adrenergic Uptake Inhibitors / chemical synthesis
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Adrenergic Uptake Inhibitors / chemistry*
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Adrenergic Uptake Inhibitors / pharmacology
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Aza Compounds / chemistry
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Bridged Bicyclo Compounds / chemistry
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Dopamine Plasma Membrane Transport Proteins / chemistry
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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 / pharmacology
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Heptanes / chemical synthesis
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Heptanes / chemistry*
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Heptanes / pharmacology
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Humans
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Norepinephrine Plasma Membrane Transport Proteins / chemistry
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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 / pharmacology
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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
Substances
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Adrenergic Uptake Inhibitors
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Aza Compounds
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Bridged Bicyclo Compounds
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Dopamine Plasma Membrane Transport Proteins
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Dopamine Uptake Inhibitors
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Heptanes
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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