1-(2-pyrimidinyl)piperazine antagonizes GABA-activated currents in cultured spinal neurones of the rat

Stephen M. Smith, David Hughes

Research output: Contribution to journalArticle

Abstract

Buspirone is an anxiolytic drug with an unknown mechanism of action. We have addressed the proposal that its therapeutic effect is due to a metabolite, 1-(2-pyrimidinyl)-piperazine (1-PP), increasing the open probability of γ-aminobutyric acid (GABA)-activated channels. By making whole-cell recordings from cultured spinal neurones we demonstrated that 1-PP, in contrast to flurazepam, actually antagonizes GABA- and glycine-activated currents. These observations are inconsistent with this proposed mechanism of action for buspirone.

Original languageEnglish (US)
Pages (from-to)366-367
Number of pages2
JournalBrain research
Volume493
Issue number2
DOIs
StatePublished - Jul 31 1989

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Keywords

  • 1-(2-Pyrimidinyl)piperazine
  • Benzodiazepine
  • Buspirone
  • Chloride channel
  • Glycine
  • Neuron
  • Spinal cord
  • γ-Aminobutyric acid

ASJC Scopus subject areas

  • Neuroscience(all)
  • Molecular Biology
  • Clinical Neurology
  • Developmental Biology

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