Preliminary evaluation of anticonvulsant activity and neurotoxicity of some 1,4-substituted piperazine derivatives

Acta Pol Pharm. 2009 Sep-Oct;66(5):571-8.

Abstract

A series of 1,4-piperazine derivatives was synthesized and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (ScMet) assays and for neurotoxicity (TOX). The compounds were only moderately effective. The anticonvulsant activity was accompanied by neurotoxicity. 1-[(4-Chlor-3-methylphenoxy)-acetyl]-4-(2-methoxyphenyl)-piperazine was also evaluated in six hertz seizure test (6-Hz) and showed good activity. At the dose of 100 mg/kg b. w. the compound produced 100% protection after 0.5 h without neurotoxic effect.

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis
  • Anticonvulsants / pharmacology*
  • Anticonvulsants / toxicity
  • Disease Models, Animal
  • Electroshock
  • Male
  • Mice
  • Neurotoxicity Syndromes / etiology*
  • Pentylenetetrazole
  • Piperazines / chemical synthesis
  • Piperazines / pharmacology*
  • Piperazines / toxicity
  • Seizures / drug therapy*
  • Structure-Activity Relationship

Substances

  • Anticonvulsants
  • Piperazines
  • Pentylenetetrazole