GABA θ1 receptor: inhibition by protein kinase C activators

Tadashi Kusama, Manabu Sakurai, Yasuo Kizawa, George R. Uhl, Hajime Murakami

Research output: Contribution to journalArticle

Abstract

The effects of protein kinase C (PKC) activators on γ-aminobutyric acid (GABA) θ1 receptor function were studied in θ1-expressingXenopus oocytes. The PKC activator phorbol 12-myristate 13-acetate (PMA) but not the inactive analog phorbol 12-mono-myristate inhibited the GABA-gated chloride currents. Mezerein, a non-phorbol ester type PKC activator, also inhibited the θ1 responses, but 8-chlorophenylthio-cyclic AMP, a protein kinase A activator, had no effect. The effect of PMA was significantly reduced by a PKC inhibitor, staurosporine. These results suggest that GABA θ1 receptor function can be regulated by PKC-mediated phosphorylation events.

Original languageEnglish (US)
Pages (from-to)431-434
Number of pages4
JournalEuropean Journal of Pharmacology: Molecular Pharmacology
Volume291
Issue number3
DOIs
StatePublished - Nov 30 1995

Keywords

  • Down-regulation
  • GABA θ receptor
  • Phorbol ester
  • Protein kinase C
  • Staurosporine
  • Xenopus oocyte

ASJC Scopus subject areas

  • Pharmacology

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