Synthesis of new 1-phenyl-2-(4-substituted-piperazin-1-yl)-propanol derivatives and evaluation of their antidepressant-like effects

Arch Pharm Res. 2013 Jul;36(7):802-11. doi: 10.1007/s12272-013-0119-1.

Abstract

In this study, we synthesized eight novel 1-phenyl-2-(4-substituted-piperazin-1-yl)-propanol derivatives and evaluated their antidepressant-like activities. The chemical structures of the synthesised compounds were elucidated by spectroscopy and elemental analyses. Potential antidepressant-like effects of the test compounds (20 mg kg(-1)) were investigated using the tail-suspension test and modified forced swimming test (MFST) in mice. Additionally, the spontaneous locomotor activity of the mice was assessed using the activity cage apparatus. Both the reference drug fluoxetine (20 mg kg(-1)) and the test compounds 3a-3e and 3g significantly shortened the immobility time of the mice in both the behavioural tests. These test compounds also increased the swimming time in MFST without any change in the climbing duration. Compounds 3c-3e and 3g were significantly more potent in inducing these effects than 3a and 3b. None of the compounds changed the locomotor activities of the animals, thus antidepressant-like effects of test compounds were specific. The findings support those of previous studies that reported antidepressant-like activities of aryl alkanol piperazine derivatives.

MeSH terms

  • Animals
  • Antidepressive Agents / chemical synthesis*
  • Antidepressive Agents / therapeutic use
  • Depression / drug therapy*
  • Depression / psychology
  • Drug Evaluation, Preclinical / methods
  • Hindlimb Suspension / psychology
  • Mice
  • Mice, Inbred BALB C
  • Motor Activity / drug effects
  • Motor Activity / physiology
  • Piperazine
  • Piperazines / chemical synthesis*
  • Piperazines / pharmacology
  • Piperazines / therapeutic use
  • Propranolol / chemical synthesis*
  • Propranolol / pharmacology
  • Propranolol / therapeutic use
  • Random Allocation
  • Swimming / psychology
  • Treatment Outcome

Substances

  • Antidepressive Agents
  • Piperazines
  • Piperazine
  • Propranolol