组胺
反激动剂
组胺H1受体
美吡拉明
敌手
基因表达
内分泌学
受体
内科学
药理学
化学
基因
生物
医学
生物化学
作者
Hiroyuki Mizuguchi,Shohei Ono,Masashi Hattori,Hiroyuki Fukui
摘要
Histamine H1 receptor (H1R) expression influences the severity of allergy symptoms. We examined the effect of inverse agonists on H1R gene expression. Two inverse agonists (carebastine and mepyramine), but not the neutral antagonist oxatomide, decreased inositol phosphate accumulation. The inverse agonists also decreased H1R gene expression and down-regulated H1R mRNA below basal expression, while basal H1R mRNA expression was maintained after oxatomide treatment. These results suggest that inverse agonists more potently alleviate allergy symptoms by not only inhibiting stimulus-induced up-regulation of H1R gene expression but also by suppressing basal histamine signaling through their inverse agonistic activity.
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