Homologous and Heterologous Phosphorylations of Human Histamine H1 Receptor in Intact Cells

DOI Web Site PubMed 被引用文献3件 参考文献26件 オープンアクセス
  • Miyoshi Katsuhiro
    Department of Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokushima
  • Kawakami Nozomi
    Department of Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokushima
  • Horio Shuhei
    Department of Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokushima
  • Fukui Hiroyuki
    Department of Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokushima

この論文をさがす

説明

Homologous and heterologous phosphorylations of histamine H1 receptor (H1R) in intact cells were investigated using Chinese hamster ovary cells stably co-expressing c-myc-tagged human histamine H1 and muscarinic M3 receptors. Increase in histamine-induced homologous phosphorylation of H1R was induced in a dose- and time-dependent manner. Maximum phosphorylation of H1R by 8-fold over the basal level was induced 1 min after the stimulation, and the increased phosphorylation level was maintained over 40 min. M3 receptor-mediated heterologous phosphorylation of H1R reached maximum by 2-fold over the basal level at 5 min after the stimulation and then rapidly returned to the basal level by 40 min after the stimulation. Histamine-induced phosphorylation of H1R was partially inhibited by three protein kinase inhibitors including Ro-31-8220 for protein kinase C (PKC), KN-93 for calcium/calmodulin-dependent kinase II (CaMKII), and KT5823 for protein kinase G (PKG), while, M3-receptor-mediated phosphorylation of H1R was completely inhibited by Ro 31-8220. Protein kinase activators including phorbol 12-myristate 13-acetate (PMA), 8-bromo-cyclic GMP (8-Br-cGMP), and 8-bromo-cyclic AMP (8-Br-cAMP) induced increases in H1R phosphorylation. Increased phosphorylation of H1R, by 5-fold over the basal level, induced with a combination of PMA, 8-Br-cGMP, and 8-Br-cAMP was still lower than that with histamine. It was suggested that H1R-mediated H1R phosphorylation involves the activation of PKC, CaMKII, PKG, and other unidentified kinases including G-protein coupled receptor kinases (GRKs) and that PKC is solely involved in M3 receptor-mediated H1R phosphorylation.<br>

収録刊行物

被引用文献 (3)*注記

もっと見る

参考文献 (26)*注記

もっと見る

キーワード

詳細情報 詳細情報について

問題の指摘

ページトップへ