Abstract
The discovery of a series of 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles, dual acting norepinephrine reuptake inhibitors (NRIs) and 5-HT(2A) receptor antagonists, is described. The synthesis and structure-activity relationship (SAR) of this novel series of compounds is also presented.
MeSH terms
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Biological Transport / drug effects
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Cell Line
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Humans
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Indoles / chemical synthesis
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Indoles / metabolism
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Indoles / pharmacology*
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Neurotransmitter Uptake Inhibitors / chemical synthesis*
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Neurotransmitter Uptake Inhibitors / metabolism
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Neurotransmitter Uptake Inhibitors / pharmacology*
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Norepinephrine / metabolism*
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Receptor, Serotonin, 5-HT2A / metabolism
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Serotonin 5-HT2 Receptor Antagonists*
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Serotonin Antagonists / chemical synthesis*
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Serotonin Antagonists / metabolism
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Serotonin Antagonists / pharmacology*
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Structure-Activity Relationship
Substances
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Indoles
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Neurotransmitter Uptake Inhibitors
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Receptor, Serotonin, 5-HT2A
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Serotonin 5-HT2 Receptor Antagonists
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Serotonin Antagonists
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Norepinephrine