TY - JOUR
T1 - Histamine H1-receptor-mediated keratan sulfate production in rabbit chondrocytes
T2 - Involvement of protein kinase C
AU - Fukuda, K.
AU - Yamasaki, H.
AU - Nagata, Y.
AU - Motoyoshi, H.
AU - Matsumura, F.
AU - Kuno, T.
AU - Tanaka, S.
N1 - Copyright:
Copyright 2020 Elsevier B.V., All rights reserved.
PY - 1991
Y1 - 1991
N2 - 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.
AB - 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.
KW - Phorbol 12,13-dibutyrate
KW - Phorbol ester
KW - Pyrilamine
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U2 - 10.1152/ajpcell.1991.261.3.c413
DO - 10.1152/ajpcell.1991.261.3.c413
M3 - Article
C2 - 1887868
AN - SCOPUS:0025990853
VL - 261
SP - C413-C416
JO - American Journal of Physiology
JF - American Journal of Physiology
SN - 0363-6143
IS - 3 30-3
ER -