Histamine H4 receptor

Histamine H4 receptor

protein
Name=histamine receptor H4
caption=


width=
HGNCid=17383
Symbol=HRH4
AltSymbols=
EntrezGene=59340
OMIM=606792
RefSeq=NM_021624
UniProt=Q9H3N8
PDB=
ECnumber=
Chromosome=18
Arm=q
Band=11.2
LocusSupplementaryData=The histamine H4 receptor is, like the other three histamine receptors, a member of the G protein-coupled receptor superfamily.cite journal | author = Oda T, Morikawa N, Saito Y, Masuho Y, Matsumoto S | title = Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes | journal = J. Biol. Chem. | volume = 275 | issue = 47 | pages = 36781–6 | year = 2000 | pmid = 10973974 | doi = 10.1074/jbc.M006480200 | issn = ] cite journal | author = Nakamura T, Itadani H, Hidaka Y, Ohta M, Tanaka K | title = Molecular cloning and characterization of a new human histamine receptor, HH4R | journal = Biochem. Biophys. Res. Commun. | volume = 279 | issue = 2 | pages = 615–20 | year = 2000 | pmid = 11118334 | doi = 10.1006/bbrc.2000.4008 | issn = ] cite journal | author = Nguyen T, Shapiro DA, George SR, Setola V, Lee DK, Cheng R, Rauser L, Lee SP, Lynch KR, Roth BL, O'Dowd BF | title = Discovery of a novel member of the histamine receptor family | journal = Mol. Pharmacol. | volume = 59 | issue = 3 | pages = 427–33 | year = 2001 | pmid = 11179435 | doi = | issn = | url = http://molpharm.aspetjournals.org/cgi/content/abstract/59/3/427 | format = abstract ]

Tissue distribution

H4 is highly expressed in bone marrow and white blood cells and regulates zymosan-induced neutrophil release from bone marrow and subsequent infiltration in the pleurisy model along with L-selectin.cite journal | author = Takeshita K, Bacon KB, Gantner F | title = Critical role of L-selectin and histamine H4 receptor in zymosan-induced neutrophil recruitment from the bone marrow: comparison with carrageenan | journal = J. Pharmacol. Exp. Ther. | volume = 310 | issue = 1 | pages = 272–80 | year = 2004 | pmid = 14996947 | doi = 10.1124/jpet.103.063776 | issn = ] It is also expressed in the colon, liver, lung, small intestine, spleen, testes, thymus, tonsils, and trachea. [http://www.bioreagents.com/index.cfm/fuseaction/products.detail/CatNbr/OPA1-15360 Bioreagents.com: Histamine H4 Receptor] ]

Function

They have been shown to mediate mast cell chemotaxis.cite journal | author = Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP | title = Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells | journal = J. Pharmacol. Exp. Ther. | volume = 305 | issue = 3 | pages = 1212–21 | year = 2003 | pmid = 12626656 | doi = 10.1124/jpet.102.046581 | issn = ] It seems to do this by the mechanism of Gi-coupled decrease in cAMP. [http://www.ebi.ac.uk/interpro/IEntry?ac=IPR008102 InterPro: IPR008102 Histamine H4 receptor] ]

Ligands

Agonists

* 4-Methylhistamine
* VUF-8430 (2- [(Aminoiminomethyl)amino] ethyl carbamimidothioic acid ester)

Antagonists

* JNJ 7777120
* VUF-6002 (1- [(5-Chloro-1H-benzimidazol-2-yl)carbonyl] -4-methylpiperazine)

Therapeutic potential

By inhibiting the H4 receptor, asthma and allergy may be treated.

The highly selective histamine H4 antagonist VUF-6002 is orally active and inhibits the activity of both mast cells and eosinophils "in vivo", [Varga C, Horvath K, Berko A, Thurmond RL, Dunford PJ, Whittle BJ. Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat. "European Journal of Pharmacology". 2005 Oct 17;522(1-3):130-8. PMID 16213481] and has antiinflammatory and antihyperalgesic effects. [Coruzzi G, Adami M, Guaita E, de Esch IJ, Leurs R. 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". 2007 Jun 1;563(1-3):240-4. PMID 17382315]

References

External links

* [http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2967 IUPHAR GPCR Database - H4 Histamine Receptor]
*MeshName|HRH4+protein,+human


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