Abstract
A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT1A 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 affinities at the 5-HT1A receptor and serotonin reuptake site in vitro. In vivo evaluation of this series of compounds demonstrated elevated extracellular serotonin levels from the basal and quick recovery of neuron firing that was presumably suppressed by the initial acute activation of 5-HT1A somatodendritic autoreceptors.
MeSH terms
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Animals
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Antidepressive Agents / administration & dosage
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Antidepressive Agents / chemistry
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Antidepressive Agents / pharmacology*
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Brain / drug effects
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Drug Evaluation, Preclinical
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In Vitro Techniques
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Male
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Molecular Conformation
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Piperidines / administration & dosage
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Piperidines / chemistry
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Piperidines / pharmacology*
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Propanols / administration & dosage
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Propanols / chemistry
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Propanols / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Selective Serotonin Reuptake Inhibitors / administration & dosage
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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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Stereoisomerism
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Structure-Activity Relationship
Substances
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Antidepressive Agents
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Piperidines
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Propanols
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Serotonin 5-HT1 Receptor Antagonists
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Serotonin Uptake Inhibitors