Histamine H1-receptor-mediated keratan sulfate production in rabbit chondrocytes: Involvement of protein kinase C

K. Fukuda, H. Yamasaki, Y. Nagata, H. Motoyoshi, F. Matsumura, T. Kuno, S. Tanaka

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25 Citations (Scopus)


We investigated the characteristics of the histamine H1-receptor in cultured rabbit chondrocytes. Scatchard analysis of [3H]pyrilamine, an H1-antagonist, binding to the chondrocytes revealed a single class of binding sites with K(D) and B(max) values of 90 ± 12 nM and 56 ± 11 fmol/104 cells, respectively. H1-agonists stimulated the production of keratan sulfate in a dose-dependent manner. Stimulation of keratan sulfate production was inhibited by pyrilamine. Protein kinase C inhibitors (sphingosine and H-7) also had inhibitory effects. Phorbol 12,13-dibutyrate, a direct activator of protein kinase C, activated the production. When protein kinase C in the chondrocytes was downregulated by preincubation with phorbol ester, the effect of the H1-agonist on keratan sulfate production was abolished. These results indicate that the histamine H1-receptor on chondrocytes mediates the accumulation of keratan sulfate production and that protein kinase C is involved in these events.

Original languageEnglish
Pages (from-to)C413-C416
JournalAmerican Journal of Physiology - Cell Physiology
Issue number3 30-3
Publication statusPublished - 1991


  • Phorbol 12,13-dibutyrate
  • Phorbol ester
  • Pyrilamine

ASJC Scopus subject areas

  • Physiology
  • Cell Biology


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