Abstract
Potent 5-HT1A/SSRIs at low nanomolar and subnanomolar concentrations were identified in a series of 1-(1H-indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols. Incorporation of an alpha-Me group in the piperidine ring with its specific stereochemistry enhanced binding affinity at the 5-HT reuptake site and in vitro 5-HT(1A) antagonist functional activity.
MeSH terms
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Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
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Indicators and Reagents
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Paroxetine / pharmacology
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Piperidines / chemical synthesis*
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Piperidines / pharmacology*
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Propanols / chemical synthesis*
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Propanols / pharmacology*
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Receptor, Serotonin, 5-HT1A / drug effects*
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Selective Serotonin Reuptake Inhibitors / chemical synthesis*
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Selective Serotonin Reuptake Inhibitors / pharmacology*
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Serotonin Antagonists / chemical synthesis*
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Serotonin Antagonists / pharmacology*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Indicators and Reagents
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Piperidines
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Propanols
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Serotonin Antagonists
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Serotonin Uptake Inhibitors
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Receptor, Serotonin, 5-HT1A
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Guanosine 5'-O-(3-Thiotriphosphate)
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Paroxetine