Histamine receptor Totally Explained

Everything about The Histamine Receptor totally explained

The histamine receptors are a class of G-protein coupled receptors with histamine as their endogenous ligand. There are four known histamine receptors:

Comparison

Receptor	Mechanism	Function	Antagonists
H₁	G_q	ileum contraction modulate circadian cycle systemic vasodilatation bronchoconstriction (asthma)	H₁-receptor antagonists Diphenhydramine Loratadine Cetirizine
H₂	G_s ↑ Ca²⁺	speed up sinus rhythm Stimulation of gastric acid secretion Smooth muscle relaxation Inhibit antibody synthesis, T-cell proliferation and cytokine production	H₂-receptor antagonists Ranitidine Cimetidine
H₃	G_i	Neurotransmitter in CNS Presynaptic autoreceptors	H₃-receptor antagonists Thioperamide Ciproxifan Cipralisant
H₄	G_i	mediate mast cell chemotaxis.	H₄-receptor antagonists Thioperamide

There are several splice variants of H₃ present in various species. Though all of the receptors are 7-transmembrane g protein coupled receptors, H₁ and H₂ are quite different from H₃ and H₄ in their activities. H₁ causes an increase in phosphoinositol hydrolysis, H2 stimulates gastric acid secretion, and H3 mediates feedback inhibition of histamine.

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