Histamine Receptor Family

The histamine receptors are a type of G protein-coupled receptors which bind histamine as their primary endogenous ligand. Histamine is a monoamine signaling molecule that functions through four G-protein-coupled histamine receptors: H1, H2, H3, and H4. Histamine mediates many of the biological activities stimulated by various immunological and non-immunological stimuli by differential expression of H1 to H4 on effector cells, including mast cells and basophils, etc. Histamine receptors are activated by the endogenous ligand histamine. There are significant species differences between histamine receptor orthologues. The H3 receptor genes in human and rat are significantly spliced variance. The potency order of histamine at histamine receptor subtypes is H3 = H4 > H2 > H1. Some agonists of the human H3 receptor show significant ligand preference.

(A) Schematic overview of the canonical heterotrimeric G-protein–mediated signaling pathways activated by the four histamine receptor subtypes. (B) Overview of the different FRET biosensors used in this study to analyze the signaling profiles of the four histamine receptor subtypes. All biosensors are based on a CFP/YFP FRET pair. AC, adenylyl cyclase; DAG, diacylglycerol; mDia, mammalian diaphanous-related formin 1; PKA, protein kinase A; PKC, protein kinase C; RhoGEF, Rho guanine exchange factor; ROCK, Rho-associated coiled-coil-containing protein kinase. Fig.1 Histamine receptor signaling. (Scammell, 2011)

Here show four of the histamine receptors, HRH1 to HRH4, which are four variants encoded by different genes. There are various splice variants of H3 in different species. Although all the receptors are 7-transmembrane G protein-coupled receptors, H1 and H2 are very different from H3 and H4 in their activities. H1 causes an increase in PIP2 hydrolysis. H2 stimulates gastric acid secretion. H3 mediates feedback inhibition of histamine.

Histamine Receptor Members

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  1. Scammell T E and Winrow C J. (2011). Orexin receptors: pharmacology and therapeutic opportunities. Annu Rev Pharmacol Toxicol. 51: 243-66.

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