2-Substituted N-aryl piperazines as novel triple reuptake inhibitors for the treatment of depression

Bioorg Med Chem Lett. 2010 Jul 1;20(13):3941-5. doi: 10.1016/j.bmcl.2010.05.008. Epub 2010 May 10.

Abstract

Recently a class of compounds known as triple reuptake inhibitors has emerged as a new strategy for the treatment of depression. These compounds work by simultaneously inhibiting the synaptic reuptake of serotonin, norepinephrine and dopamine. In this Letter we describe the optimization of a novel series of 2-substituted N-aryl piperazine based triple reuptake inhibitors.

MeSH terms

  • Animals
  • Antidepressive Agents / chemical synthesis
  • Antidepressive Agents / chemistry
  • Antidepressive Agents / pharmacology*
  • Depression / drug therapy*
  • Dopamine / metabolism
  • Dose-Response Relationship, Drug
  • Mice
  • Molecular Structure
  • Neurotransmitter Uptake Inhibitors / chemical synthesis
  • Neurotransmitter Uptake Inhibitors / chemistry
  • Neurotransmitter Uptake Inhibitors / pharmacology*
  • Norepinephrine / metabolism
  • Piperazines / chemical synthesis
  • Piperazines / chemistry
  • Piperazines / pharmacology*
  • Serotonin / metabolism
  • Stereoisomerism
  • Structure-Activity Relationship
  • Synapses / drug effects
  • Synapses / metabolism

Substances

  • Antidepressive Agents
  • Neurotransmitter Uptake Inhibitors
  • Piperazines
  • Serotonin
  • Dopamine
  • Norepinephrine