Abstract
A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT(1A) receptor antagonism and serotonin reuptake inhibition was discovered. 1-(1H-Indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols exhibited selective and high affinity at the 5-HT(1A) receptor and serotonin reuptake inhibition at nanomolar concentrations for dual activities.
MeSH terms
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Antidepressive Agents, Second-Generation / chemical synthesis
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Antidepressive Agents, Second-Generation / chemistry*
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Antidepressive Agents, Second-Generation / pharmacology*
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Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
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Indoles / chemistry
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Indoles / pharmacology
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Paroxetine / pharmacology
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Propanols / chemical synthesis
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Propanols / chemistry*
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Propanols / pharmacology*
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Receptor, Serotonin, 5-HT1A / metabolism
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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 5-HT1 Receptor Antagonists*
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Structure-Activity Relationship
Substances
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Antidepressive Agents, Second-Generation
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Indoles
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Propanols
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Serotonin 5-HT1 Receptor 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