Abstract
A series of (1S,3S,6R,10S)-(Z)-9-(thienylmethylene- or substituted thienylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes was prepared and evaluated for the ability to block dopamine, serotonin, and norepinephrine reuptake by their respective transporters. Compound 5b is a NET-selective inhibitor, 5c is a mixed NET- and SERT-selective inhibitor, while 11 is a SERT-selective inhibitor.
Publication types
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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 / drug effects
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Brain / metabolism
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Carrier Proteins / metabolism
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Dopamine Plasma Membrane Transport Proteins
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Ligands
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Membrane Glycoproteins / metabolism
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Membrane Transport Proteins / metabolism
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Molecular Conformation
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Nerve Tissue Proteins*
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Neurotransmitter Uptake Inhibitors / chemical synthesis
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Neurotransmitter Uptake Inhibitors / pharmacology*
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Norepinephrine / physiology*
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Norepinephrine Plasma Membrane Transport Proteins
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Rats
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Selective Serotonin Reuptake Inhibitors / chemical synthesis
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Selective Serotonin Reuptake Inhibitors / pharmacology*
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Serotonin / physiology
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Serotonin Plasma Membrane Transport Proteins
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Stereoisomerism
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Structure-Activity Relationship
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Symporters / metabolism
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Thiophenes / chemical synthesis
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Thiophenes / pharmacology*
Substances
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Carrier Proteins
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Dopamine Plasma Membrane Transport Proteins
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Ligands
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Membrane Glycoproteins
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Membrane Transport Proteins
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Nerve Tissue Proteins
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Neurotransmitter 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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Slc6a2 protein, rat
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Slc6a4 protein, rat
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Symporters
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Thiophenes
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Serotonin
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Norepinephrine