Histamine receptor

The histamine receptors are a class of G protein–coupled receptors which bind histamine as their primary endogenous ligand.^[1]

There are four known histamine receptors:

H₁ receptor
H₂ receptor
H₃ receptor
H₄ receptor

Comparison[]

Histamine receptors
Receptor	Mechanism	Function	Antagonists
H₁	G_q	ileum contraction modulate circadian cycle itching systemic vasodilatation bronchoconstriction (allergy-induced asthma)	H₁-receptor antagonists Diphenhydramine Loratadine Cetirizine Fexofenadine Clemastine Rupatadine
H₂	G_s ↑ cAMP²⁺	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 Famotidine Nizatidine
H₃	G_i	Decrease Acetylcholine, Serotonin and Norepinephrine Neurotransmitter release in CNS Presynaptic autoreceptors	H₃-receptor antagonists ABT-239 Ciproxifan Clobenpropit Thioperamide
H₄	G_i	mediate mast cell chemotaxis.^[2]	H₄-receptor antagonists Thioperamide JNJ 7777120

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 PIP₂ hydrolysis, H2 stimulates gastric acid secretion, and H3 mediates feedback inhibition of histamine.

References[]

^ Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacol. Rev. 49 (3): 253–78. PMID 9311023.
^ Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP (2003). "Histamine H₄ receptor mediates chemotaxis and calcium mobilization of mast cells". J. Pharmacol. Exp. Ther. 305 (3): 1212–21. doi:10.1124/jpet.102.046581. PMID 12626656.

External links[]

"Histamine Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Holger Stark: Histamine Receptors, BIOTREND Reviews No. 01, November 2007
The Histamine Receptor
Histamine+Receptor at the US National Library of Medicine Medical Subject Headings (MeSH)

[pmid9311023-1] Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacol. Rev. 49 (3): 253–78. PMID 9311023.

[pmid12626656-2] Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP (2003). "Histamine H₄ receptor mediates chemotaxis and calcium mobilization of mast cells". J. Pharmacol. Exp. Ther. 305 (3): 1212–21. doi:10.1124/jpet.102.046581. PMID 12626656.

[1]

[2]