Abstract
A series of 3-aryl-3-azolylpropan-1-amines was prepared and screened for its capability of inhibiting monoamine reuptake. Analogs with nanomolar potency, good human in vitro microsomal stability, and low drug-drug interaction potential were described. In vivo models were used to evaluate the compound 19r for antidepressive, anxiolytic, and analgesic activity.
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Analgesics / chemistry
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Analgesics / pharmacokinetics
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Analgesics / pharmacology
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Analgesics / therapeutic use
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Animals
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Anti-Anxiety Agents / chemistry
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Anti-Anxiety Agents / pharmacokinetics
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Anti-Anxiety Agents / pharmacology
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Anti-Anxiety Agents / therapeutic use
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Antidepressive Agents / chemistry
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Antidepressive Agents / pharmacokinetics
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Antidepressive Agents / pharmacology
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Antidepressive Agents / therapeutic use*
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CHO Cells
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Cell Line
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Cricetinae
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Cricetulus
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Dopamine / metabolism*
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Humans
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Mice
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Neurotransmitter Uptake Inhibitors / chemistry
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Neurotransmitter Uptake Inhibitors / pharmacokinetics
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Neurotransmitter Uptake Inhibitors / pharmacology
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Neurotransmitter Uptake Inhibitors / therapeutic use*
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Norepinephrine / metabolism*
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Propylamines / chemistry
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Propylamines / pharmacokinetics
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Propylamines / pharmacology
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Propylamines / therapeutic use*
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Rats
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Serotonin / metabolism*
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Tetrazoles / chemistry
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Tetrazoles / pharmacokinetics
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Tetrazoles / pharmacology
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Tetrazoles / therapeutic use*
Substances
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Analgesics
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Anti-Anxiety Agents
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Antidepressive Agents
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Neurotransmitter Uptake Inhibitors
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Propylamines
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Tetrazoles
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Serotonin
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Dopamine
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Norepinephrine