PMID: 16648669May 2, 2006Paper

Recent advances in molecular pharmacology of the histamine systems: regulation of histamine H1 receptor signaling by changing its expression level

Journal of Pharmacological Sciences
Katsuhiro MiyoshiHiroyuki Fukui

Abstract

Histamine H1 receptor (H1R) signaling is regulated by changing its expression level. Two mechanisms are involved in this regulation. One is down-regulation through receptor desensitization. Receptor phosphorylation seemed crucial because stimulation of the mutant H1R lacking five putative phosphorylation sites did not show down-regulation. The phosphorylation level of the mutant receptor was much smaller than that of the wild type ones by several protein kinases. The other is up-regulation through activation of receptor gene expression. Protein kinase C (PKC) signaling was suggested to be involved in this up-regulation. Regulation of H1R expression level was mediated not only through H1R but also autonomic nerve receptors. Stimulation of M3 muscarinic receptors (M3R) induced both down-regulation and up-regulation of H1R. Down-regulation of M3R-mediated H1R seemed not to be mediated by PKC activation, although PKC activation induced H1R phosphorylation. Elevation of H1R expression was induced by the stimulation of M3Rs. PKC was suggested to be involved in this up-regulation. Stimulation of beta2-adrenergic receptors induced H1R down-regulation through several mechanisms. One of them is enhanced receptor degradation after desensi...Continue Reading

References

Jun 1, 1993·British Journal of Pharmacology·D R Bristow, M R Zamani
Apr 6, 1999·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·K FujimotoH Fukui
Dec 20, 2003·Methods and Findings in Experimental and Clinical Pharmacology·N KawakamiH Fukui
Apr 27, 2004·Journal of Pharmacological Sciences·Shuhei HorioHiroyuki Fukui
Aug 3, 2004·Journal of Pharmacological Sciences·Katsuhiro MiyoshiHiroyuki Fukui
Dec 16, 2004·Journal of Pharmacological Sciences·Katsuhiro MiyoshiHiroyuki Fukui

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Citations

Jan 16, 2014·The Journal of Endocrinology·Romina Maria PagottoOmar Pedro Pignataro
Oct 30, 2007·The Journal of Clinical Investigation·Rajkumar NoubadeCory Teuscher
Jul 12, 2012·Clinical Oral Investigations·Martin GrimmSebastian Hoefert
Sep 15, 2016·European Archives of Oto-rhino-laryngology : Official Journal of the European Federation of Oto-Rhino-Laryngological Societies (EUFOS) : Affiliated with the German Society for Oto-Rhino-Laryngology - Head and Neck Surgery·Shao-Cheng LiuHsing-Won Wang

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