Inhibition of a gamma aminobutyric acid A receptor by caffeine

Julianna Kardos, Tamás Blandl

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16 Citations (Scopus)

Abstract

The effect of caffeine was studied on the progress of gamma aminobutyric acid A receptor channel (GABAAR) mediated transmembrane36Cl flux and [3H]GABA release in native membrane vesicles from rat cerebral cortex using rapid kinetic techniques. GABA response on the second time-scale mediated by the slower desensitizing GABAAR was inactivated by 5 mM caffeine whereas subsecond GABA response retained activity. An inhibitor of caffeine-evoked GABA release, dantrolene (0.025 mM), inhibited the effect of caffeine on GABA-mediated transmembrane36Cl ion flux. The caffeine-evoked GABA release indicated a rise of [Ca2+]i near to completion within 0.2 s. It can be assumed that elevated [Ca2+]i during depolarization and inhibition of GABAAR with longer mean lifetime function together resulting in a disinhibition of neurotransmission.

Original languageEnglish
Pages (from-to)1249-1252
Number of pages4
JournalNeuroreport
Volume5
Issue number10
DOIs
Publication statusPublished - Jun 1994

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Keywords

  • Caffeine
  • Cl flux
  • GABA
  • Native membrane vesicles
  • Rat cerebral cortex

ASJC Scopus subject areas

  • Neuroscience(all)

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