<原著>ウサギ関節軟骨細胞におけるヒスタミン受容体機能

概要

論文の詳細を見る
Using the radioligand histamine H_1 antagonist [^3H]-pyrilamine and H_2 antagonist [^3H]-tiotidine, we characterized the histamine H_1 and H_2 receptors on rabbit articular chondrocytes. We found that single class of binding of [^3H]-pyrilamine and [^3H]-tiotidine existed on these cells, respectively. The measured K_D of binding for [^3H]-pyrilamine and [^3H]-tiotidine were 90±20 and 122±23 nM, and the maximum binding 56±17 and 2.3±0.5 fmol/10^4 cells, respectively. Histamine H_1 receptor agonists (2-methylhistamine and 2-pyridylethylamine) stimulated the release of keratan sulfate in a dose dependent manner. Histamine H_2 receptor agonists (dimaprit and 4-methylhistamine) inhibited the release of keratan sulfate in a dose dependent manner. The effect of histamine H_1 receptor agonist was inhibited by the protein kinase C inhibitor (sphingosine). When protein kinase C in the chondrocytes was down regulated by preincubation with phorbol 12,13-dibutyrate, a direct activator of protein kinase C, the effect of histamine H_1 agonist was abolished. These findings indicate that the histamine H_1 receptor is regulated by protein kinase C.
近畿大学の論文
1991-12-25