GABA rho1 receptor: inhibition by protein kinase C activators.
The effects of protein kinase C (PKC) activators on gamma-aminoburyric acid (GABA) rho 1 receptor function were studied in rho 1 -expressing Xenopus 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 rho 1 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 rho 1 receptor function can be regulated by PKC-mediated phosphorylation events.
Kusama
T
T
Department of Physiology and Anatomy, Nihon University College of Pharmacy, Chiba, Japan.
Sakurai
M
M
Kizawa
Y
Y
Uhl
G R
GR
Murakami
H
H
D000470:Alkaloids / Q000494:pharmacology; D000818:Animals; D000242:Cyclic AMP / Q000031:analogs & derivatives / Q000494:pharmacology; D004224:Diterpenes; D004594:Electrophysiology; D004789:Enzyme Activation; D018756:GABA Antagonists / Q000494:pharmacology*; D011493:Protein Kinase C / Q000819:agonists*; D018079:Receptors, GABA / Q000502:physiology*; D019311:Staurosporine; D013729:Terpenes / Q000494:pharmacology; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology*; D013873:Thionucleotides / Q000494:pharmacology; D014162:Transfection; D014982:Xenopus laevis
D000470:Alkaloids; D004224:Diterpenes; D018756:GABA Antagonists; D018079:Receptors, GABA; D013729:Terpenes; D013873:Thionucleotides; C011309:mezerein; C015929:8-((4-chlorophenyl)thio)cyclic-3',5'-AMP; D000242:Cyclic AMP; D011493:Protein Kinase C; D019311:Staurosporine; D013755:Tetradecanoylphorbol Acetate