Histamine receptor

The histamine receptors are a class of G protein–coupled receptors which bind histamine as their primary endogenous ligand.[1][2]

There are four known histamine receptors:

Comparison

Histamine receptors
Receptor	Location	Mechanism of action	Function	Antagonists	Uses of antagonists
H₁	Throughout the body, especially in:[3] Smooth muscles vascular endothelial cells (cells of walls of blood vessels) adrenal medulla heart brain spinal cord	G_q	ileum contraction modulate circadian cycle itching systemic vasodilatation (indirect effect throughout the increased production of NO) bronchoconstriction (allergy-induced asthma)	H₁-receptor antagonists Azelastine Diphenhydramine Loratadine Cetirizine Fexofenadine Clemastine Rupatadine	Allergies nausea sleep disorders
H₂	Gastric parietal cells smooth muscles mast cells neutrophils heart uterus	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	Peptic ulcer disease Stress ulcers Gastroesophageal reflux disease Dyspepsia Aspiration pneumonia
H₃	Thalamus caudate nucleus cerebral cortex small intestine testes prostate	G_i	Decrease Acetylcholine, Serotonin and Norepinephrine Neurotransmitter release in CNS Presynaptic autoreceptors	H₃-receptor antagonists ABT-239 Ciproxifan Clobenpropit Thioperamide	Narcolepsy Alzheimer's disease Attention deficit hyperactivity disorder (ADHD) Schizophrenia
H₄	Immune system lymphocytes leukocytes Lymphoid organs thymus spleen liver[4] gastrointestinal tract (GIT) pancreas bile ducts	G_i	mediate mast cell chemotaxis.[5]	H₄-receptor antagonists Thioperamide JNJ 7777120	As of July 2021, no clinical uses exist. Potential uses include:[6] rheumatoid arthritis[7] asthma allergic rhinitis atopic dermatitis pruritus

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, et al. (September 1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacological Reviews. 49 (3): 253–278. PMID 9311023.
Ravhe IS, Krishnan A, Manoj N (January 2021). "Evolutionary history of histamine receptors: Early vertebrate origin and expansion of the H₃-H₄ subtypes". Molecular Phylogenetics and Evolution. 154: 106989. doi:10.1016/j.ympev.2020.106989. PMID 33059072. S2CID 222842322.
"Histamine H1 Receptor - an overview | ScienceDirect Topics". www.sciencedirect.com. Retrieved 2023-10-03.
Deiteren A, De Man JG, Pelckmans PA, De Winter BY (March 2015). "Histamine H₄ receptors in the gastrointestinal tract". British Journal of Pharmacology. 172 (5): 1165–1178. doi:10.1111/bph.12989. PMC 4337694. PMID 25363289.
Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP (June 2003). "Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells". The Journal of Pharmacology and Experimental Therapeutics. 305 (3): 1212–1221. doi:10.1124/jpet.102.046581. PMID 12626656. S2CID 14932773.
"Histamine H4 Receptor Antagonist - an overview | ScienceDirect Topics". www.sciencedirect.com. Retrieved 2023-10-03.
Kim KW, Kim BM, Lee KA, Lee SH, Firestein GS, Kim HR (April 2017). "Histamine and Histamine H4 Receptor Promotes Osteoclastogenesis in Rheumatoid Arthritis". Scientific Reports. 7 (1): 1197. Bibcode:2017NatSR...7.1197K. doi:10.1038/s41598-017-01101-y. PMC 5430934. PMID 28446753.

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 U.S. National Library of Medicine Medical Subject Headings (MeSH)

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[pmid9311023-1] Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, et al. (September 1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacological Reviews. 49 (3): 253–278. PMID 9311023.

[2] Ravhe IS, Krishnan A, Manoj N (January 2021). "Evolutionary history of histamine receptors: Early vertebrate origin and expansion of the H₃-H₄ subtypes". Molecular Phylogenetics and Evolution. 154: 106989. doi:10.1016/j.ympev.2020.106989. PMID 33059072. S2CID 222842322.

[3] "Histamine H1 Receptor - an overview | ScienceDirect Topics". www.sciencedirect.com. Retrieved 2023-10-03.

[4] Deiteren A, De Man JG, Pelckmans PA, De Winter BY (March 2015). "Histamine H₄ receptors in the gastrointestinal tract". British Journal of Pharmacology. 172 (5): 1165–1178. doi:10.1111/bph.12989. PMC 4337694. PMID 25363289.

[pmid12626656-5] Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP (June 2003). "Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells". The Journal of Pharmacology and Experimental Therapeutics. 305 (3): 1212–1221. doi:10.1124/jpet.102.046581. PMID 12626656. S2CID 14932773.

[6] "Histamine H4 Receptor Antagonist - an overview | ScienceDirect Topics". www.sciencedirect.com. Retrieved 2023-10-03.

[7] Kim KW, Kim BM, Lee KA, Lee SH, Firestein GS, Kim HR (April 2017). "Histamine and Histamine H4 Receptor Promotes Osteoclastogenesis in Rheumatoid Arthritis". Scientific Reports. 7 (1): 1197. Bibcode:2017NatSR...7.1197K. doi:10.1038/s41598-017-01101-y. PMC 5430934. PMID 28446753.