An Overview of Histamine Receptor
Histamine is an organic nitrogen compound, which participates in local immune response and regulates the physiological function of intestinal tract as neurotransmitter. Molecular biological methods show that all histamine receptors belong to the large family of G protein-coupled receptors (GPCRs). And histamine exerts its effects through at least four different receptor subtypes.
Major types of Histamine Receptor
Classification criteria of four specific histamine receptors (H1, H2, H3 and H4) were first determined according to their clinical pharmacological characteristics, and subsequently characterized by their DNA sequences. And the four histamine receptors are members of G protein coupled receptor. It takes histamine as its main endogenous ligand. A comparison of the four types of receptors is outlined, which shows that the four receptors are different in the best characterized function, the G protein coupling, the pathway of the signal transduction, and so on. In addition, these different biological effects are mediated by activating specific histamine receptors, and their tissue expression patterns and functions are different.
Inhibition of Histamine Receptor
The major inhibitors of the four histamine receptors are as follows. The H1 antihistamines include: , , , S 38093, and . Meanwhile it has important physiological functions in controlling gastric mucosa, allergic diseases, and regulating sleep revival cycle and so on. Histamine has also been shown to be involved in cell proliferation, embryo development and tumor growth. In terms of the activities of those four histamine receptors, H1 and H2 are quite different from H3 and H4. H1 causes PIP2 hydrolysis to increase and cure allergy primarily acting on these receptors. H2 stimulates gastric acid secretion, and H3 mediates histamine feedback inhibition. Moreover, H4 mainly acts on the receptors of asthma and chronic pruritus.
1. Parsons, ME. (2006) ‘Histamine and its receptors’, BRITISH JOURNAL OF PHARMACOLOGY, 147, S127-S135.
Blaya,Bruno.(2010)‘Histamineandhistaminereceptorantagonistsincancerbiology’, Inflammation & Allergy Drug Targets, 9(3), 146-157.
Idzko M. (2002) ‘Expression and function of histamine receptors in human monocyte-derived dendritic cells’, The Journal of Allergy and Clinical Immunology, 109(5), 839-846.
Esbenshade TA. (2003) ‘Differential activation of dual signaling responses by human H1 and H2 histamine receptors’, Journal of Receptor and Signal Transduction Research,23(1): 17 –31.
Lippert U. (2004) ‘Human skin mast cells express H2 and H4, but not H3 receptors’, The Journal of Investigative Dermatology,123(1): 116–23.
Coruzzi, G. (2007) ‘Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation’, European Journal of Pharmacology,563(1-3): 240–4.
Thurmond RL, (2008) ‘The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines’ Nat Rev Drug Discov, 7(1), 41-53.
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