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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 Edit

Histamine receptors
Receptor Location Mechanism of action Function Antagonists Uses of antagonists
H1 Throughout the body, especially in:[3]
Gq
H2 Gs
cAMP2+
H3 Gi
H4 Gi As of July 2021, no clinical uses exist.
Potential uses include:[6]

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 Edit

  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.
  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.

External links Edit

  • "Histamine Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
  • The Histamine Receptor
  • Histamine+Receptor at the U.S. National Library of Medicine Medical Subject Headings (MeSH)

histamine, receptor, histamine, receptors, class, protein, coupled, receptors, which, bind, histamine, their, primary, endogenous, ligand, there, four, known, histamine, receptors, receptor, receptor, receptor, receptorcomparison, edits, receptor, location, me. 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 H1 receptor H2 receptor H3 receptor H4 receptorComparison EditHistamine receptors Receptor Location Mechanism of action Function Antagonists Uses of antagonistsH1 Throughout the body especially in 3 Smooth musclesvascular endothelial cells cells of walls of blood vessels adrenal medullaheartbrainspinal cord Gq 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 Allergiesnauseasleep disordersH2 Gastric parietal cellssmooth musclesmast cellsneutrophilsheartuterus Gs 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 diseaseStress ulcersGastroesophageal reflux diseaseDyspepsiaAspiration pneumoniaH3 Thalamuscaudate nucleuscerebral cortexsmall intestinetestesprostate Gi Decrease Acetylcholine Serotonin and Norepinephrine Neurotransmitter release in CNS Presynaptic autoreceptors H3 receptor antagonists ABT 239 Ciproxifan Clobenpropit Thioperamide NarcolepsyAlzheimer s diseaseAttention deficit hyperactivity disorder ADHD SchizophreniaH4 Immune system lymphocytes leukocytes Lymphoid organs thymus spleen liver 4 gastrointestinal tract GIT pancreas bile ducts Gi mediate mast cell chemotaxis 5 H4 receptor antagonists Thioperamide JNJ 7777120 As of July 2021 update no clinical uses exist Potential uses include 6 rheumatoid arthritis 7 asthmaallergic rhinitisatopic dermatitispruritusThere 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 Edit 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 H 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 Edit 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 Retrieved from https en wikipedia org w index php title Histamine receptor amp oldid 1178514122, wikipedia, wiki, book, books, library,

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