Abstract
A series of indolylcyclohexylamines possessing potent and selective serotonin reuptake inhibition is reported. The most interesting compounds proved to have subnanomolar 5-HT transporter activity, and exhibited moderate 5-HT(1A) affinity.
MeSH terms
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Animals
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Antidepressive Agents / chemical synthesis
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Antidepressive Agents / pharmacology*
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CHO Cells
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Carrier Proteins / drug effects*
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Carrier Proteins / metabolism
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Cricetinae
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Cyclohexylamines / chemical synthesis
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Cyclohexylamines / pharmacology*
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Humans
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Indoles / chemistry
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Inhibitory Concentration 50
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Membrane Glycoproteins / drug effects*
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Membrane Glycoproteins / metabolism
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Membrane Transport Proteins*
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Nerve Tissue Proteins*
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Rats
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Receptors, Adrenergic, alpha / drug effects*
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Receptors, Adrenergic, alpha / metabolism
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Receptors, Serotonin / drug effects*
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Receptors, Serotonin / metabolism
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Receptors, Serotonin, 5-HT1
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Selective Serotonin Reuptake Inhibitors / metabolism
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Selective Serotonin Reuptake Inhibitors / pharmacology*
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Serotonin Plasma Membrane Transport Proteins
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Structure-Activity Relationship
Substances
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Antidepressive Agents
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Carrier Proteins
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Cyclohexylamines
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Indoles
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Membrane Glycoproteins
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Membrane Transport Proteins
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Nerve Tissue Proteins
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Receptors, Adrenergic, alpha
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Receptors, Serotonin
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Receptors, Serotonin, 5-HT1
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SLC6A4 protein, human
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Serotonin Plasma Membrane Transport Proteins
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Serotonin Uptake Inhibitors
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Slc6a4 protein, rat