Histamine Receptor H1 (HRH1)

H1-R; hisH1

SPN	Q765
HGNC	5182
MGI	107619
PubMed	7935475
RGD	2830
UniProt	P35367
Wiki	HRH1

The receptor is a histamine receptor belonging to the family of G-protein-coupled receptors. This receptor which is activated by the biogenic amine histamine is expressed throughout the body, specifically in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. The H₁ receptor is linked to an intracellular G-protein (G_q) that activates phospholipase C and the phosphatidylinositol (PIP2) signaling pathway. Based on the number of drugs available on market it is the most clinically important molecular drug target.The production of prostaglandin E2 synthase induces the release of histamine from neurons, causing systemic vasodilation, along with increased cell permeability due to its action on H1 receptors.

Reference

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"Two threonine residues and two serine residues in the second and third intracellular loops are both involved in histamine H1 receptor downregulation."
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"Structure of the human histamine H1 receptor complex with doxepin."
Nature 475:65-70(2011) [PubMed] [Europe PMC] [Abstract]

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Science 314:268-274(2006) [PubMed] [Europe PMC] [Abstract]