Role of therapeutics for allergic diseases in targeting histamine H 1 receptor gene expression

Abstract

Histamine H1 receptors are down-regulated as one step in receptor desensitization. Five phosphorylation sites of the H1 receptor seem to play a key role in receptor down-regulation. In contrast, an increase in the H1 receptor expression level following its mRNA elevation was found in the nasal mucosa in hypersensitivity model rats. Up-regulation of the H1 receptor was induced by the direct stimulation of the H1 receptor. H1 receptor up-regulation was suppressed by pretreatment with antiallergic agents. © 2007 The Pharmaceutical Society of Japan.