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Histamine H4 receptor: Wikis


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histamine receptor H4
Symbols HRH4; MGC133027; GPCR105; GPRv53; H4R; HH4R; H4; AXOR35; BG26
External IDs OMIM606792 MGI2429635 HomoloGene11002 IUPHAR: H4 GeneCards: HRH4 Gene
Species Human Mouse
Entrez 59340 225192
Ensembl ENSG00000134489 ENSMUSG00000037346
UniProt Q9H3N8 Q91ZY2
RefSeq (mRNA) NM_001160166 NM_153087
RefSeq (protein) NP_067637 NP_694727
Location (UCSC) Chr 18:
20.29 - 20.31 Mb
Chr 18:
13.17 - 13.18 Mb
PubMed search [1] [2]

The histamine H4 receptor is, like the other three histamine receptors, a member of the G protein-coupled receptor superfamily.[1][2][3]


Tissue distribution

H4 is highly expressed in bone marrow and white blood cells and regulates neutrophil release from bone marrow and subsequent infiltration in the zymosan-induced pleurisy mouse model.[4] It is also expressed in the colon, liver, lung, small intestine, spleen, testes, thymus, tonsils, and trachea.[5]


They have been shown to mediate mast cell chemotaxis.[6] It seems to do this by the mechanism of Gi-coupled decrease in cAMP.[7]





Therapeutic potential

By inhibiting the H4 receptor, asthma and allergy may be treated.[7]

The highly selective histamine H4 antagonist VUF-6002 is orally active and inhibits the activity of both mast cells and eosinophils in vivo,[8]and has antiinflammatory and antihyperalgesic effects.[9]


  1. ^ Oda T, Morikawa N, Saito Y, Masuho Y, Matsumoto S (2000). "Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes". J. Biol. Chem. 275 (47): 36781–6. doi:10.1074/jbc.M006480200. PMID 10973974.  
  2. ^ Nakamura T, Itadani H, Hidaka Y, Ohta M, Tanaka K (2000). "Molecular cloning and characterization of a new human histamine receptor, HH4R". Biochem. Biophys. Res. Commun. 279 (2): 615–20. doi:10.1006/bbrc.2000.4008. PMID 11118334.  
  3. ^ Nguyen T, Shapiro DA, George SR, Setola V, Lee DK, Cheng R, Rauser L, Lee SP, Lynch KR, Roth BL, O'Dowd BF (2001). "Discovery of a novel member of the histamine receptor family" (abstract). Mol. Pharmacol. 59 (3): 427–33. PMID 11179435.  
  4. ^ Takeshita K, Bacon KB, Gantner F (2004). "Critical role of L-selectin and histamine H4 receptor in zymosan-induced neutrophil recruitment from the bone marrow: comparison with carrageenan". J. Pharmacol. Exp. Ther. 310 (1): 272–80. doi:10.1124/jpet.103.063776. PMID 14996947.  
  5. ^ Histamine H4 Receptor
  6. ^ 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.  
  7. ^ a b InterPro: IPR008102 Histamine H4 receptor
  8. ^ 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
  9. ^ 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

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