histamine H4 receptor


Gene Symbol: histamine H4 receptor
Description: histamine receptor H4
Alias: histamine H4 receptor, H4R, HH4R
Species: rat
Products:     histamine H4 receptor

Top Publications

  1. Strakhova M, Nikkel A, Manelli A, Hsieh G, Esbenshade T, Brioni J, et al. Localization of histamine H4 receptors in the central nervous system of human and rat. Brain Res. 2009;1250:41-8 pubmed publisher
    ..Our observations provide evidence of the H(4) presence in both human and rodent CNS and offer some insight into possible role of H(4) in itch and pain. ..
  2. Connelly W, Shenton F, Lethbridge N, Leurs R, Waldvogel H, Faull R, et al. The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. Br J Pharmacol. 2009;157:55-63 pubmed publisher
    The histamine H4 receptor is the most recently identified of the G protein-coupled histamine receptor family and binds several neuroactive drugs, including amitriptyline and clozapine...
  3. Ahmad S, Ansari M, Zoheir K, Bakheet S, Korashy H, Nadeem A, et al. Regulation of TNF-α and NF-κB activation through the JAK/STAT signaling pathway downstream of histamine 4 receptor in a rat model of LPS-induced joint inflammation. Immunobiology. 2015;220:889-98 pubmed publisher
    Histamine 4 receptor (H4R) is a novel target for the pharmacological modulation of histamine-mediated immune signals during inflammatory diseases...
  4. Smits R, De Esch I, Zuiderveld O, Broeker J, Sansuk K, Guaita E, et al. Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach. J Med Chem. 2008;51:7855-65 pubmed publisher
    ..Compounds from this novel series of quinazolines are antagonists at the rat H(4)R and were found to possess anti-inflammatory properties in vivo in the rat. ..
  5. Ji Y, Sakata Y, Li X, Zhang C, Yang Q, Xu M, et al. Lymphatic diamine oxidase secretion stimulated by fat absorption is linked with histamine release. Am J Physiol Gastrointest Liver Physiol. 2013;304:G732-40 pubmed publisher
    ..In addition, ip administration of the histamine H4 receptor antagonist JNJ7777120 significantly reduced the Liposyn II-induced DAO output by 65...
  6. Abiuso A, Berensztein E, Pagotto R, Pereyra E, Medina V, Martinel Lamas D, et al. H4 histamine receptors inhibit steroidogenesis and proliferation in Leydig cells. J Endocrinol. 2014;223:241-53 pubmed publisher
    The histamine H4 receptor (HRH4), discovered only 13 years ago, is considered a promising drug target for allergy, inflammation, autoimmune disorders and cancer, as reflected by a steadily growing number of scientific publications and ..
  7. Yan Z, Zhang R, Yu S, Wen W, Hong J, Zhang J, et al. [Effect of histamine H4 receptor and its antagonist on allergic rhinitis in rats]. Zhonghua Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2010;45:477-80 pubmed
    To clarify the effect of histamine H4 receptor antagonist, JNJ 7777120, and histamine H1 receptor antagonist, Loratadine, on allergic rhinitis (AR) in rats and to study the role of histamine H4 receptor antagonist and histamine H1 ..
  8. Liu C, Wilson S, Kuei C, Lovenberg T. Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. J Pharmacol Exp Ther. 2001;299:121-30 pubmed
    The recently identified histamine H4 receptor has revealed a potential new complexity for the role of histamine in the immune system...
  9. Morini G, Becchi G, Shenton F, Chazot P, Grandi D. Histamine H3 and H4 receptors are expressed on distinct endocrine cell types in the rat fundic mucosa. Inflamm Res. 2008;57 Suppl 1:S57-8 pubmed publisher

More Information


  1. Smits R, Lim H, van der Meer T, Kuhne S, Bessembinder K, Zuiderveld O, et al. Ligand based design of novel histamine H? receptor antagonists; fragment optimization and analysis of binding kinetics. Bioorg Med Chem Lett. 2012;22:461-7 pubmed publisher
    ..Analysis of its binding kinetics at the human H(4)R showed this compound to have a very different dissociative half-life in comparison with reference antagonist JNJ7777120. ..
  2. Coruzzi G, Adami M, Pozzoli C, De Esch I, Smits R, Leurs R. Selective histamine H? and H? receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach. Eur J Pharmacol. 2011;669:121-7 pubmed publisher
    ..Finally, the species-dependent variations in affinity and receptor selectivity observed for most ligands need to be carefully addressed in the pharmacological characterization of histamine H(3) and H(4) receptor functions in vivo. ..
  3. Karlstedt K, Jin C, Panula P. Expression of histamine receptor genes Hrh3 and Hrh4 in rat brain endothelial cells. Br J Pharmacol. 2013;170:58-66 pubmed publisher
    ..Both Hrh3 and Hrh4 receptors are expressed in rat brain endothelial cells, and activation of the histamine H4 receptor activates the Erk1/2 cascade...
  4. Ferreira R, Santos T, Gonçalves J, Baltazar G, Ferreira L, Agasse F, et al. Histamine modulates microglia function. J Neuroinflammation. 2012;9:90 pubmed publisher
    ..Firstly, we detected the expression of all known histamine receptor subtypes (H1R, H2R, H3R and H4R), using a murine microglial cell line and primary microglia cell cultures from rat cortex, by real-time PCR ..
  5. Rosa A, Grange C, Pini A, Katebe M, Benetti E, Collino M, et al. Overexpression of histamine H? receptors in the kidney of diabetic rat. Inflamm Res. 2013;62:357-65 pubmed publisher
  6. Desmadryl G, Gaboyard Niay S, Brugeaud A, Travo C, Broussy A, Saleur A, et al. Histamine H4 receptor antagonists as potent modulators of mammalian vestibular primary neuron excitability. Br J Pharmacol. 2012;167:905-16 pubmed publisher
    ..H(4) receptor antagonists have a pronounced inhibitory effect on vestibular neuron activity. This result highlights the potential role of H(4) receptors as pharmacological targets for the treatment of vestibular disorders. ..
  7. Pozzoli C, Adami M, Smits R, Coruzzi G. Effect of histamine H4 receptor ligands on cholinergic neurotransmission of the rat duodenum. Inflamm Res. 2009;58 Suppl 1:59-60 pubmed publisher
  8. Thurmond R, Desai P, Dunford P, Fung Leung W, Hofstra C, Jiang W, et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther. 2004;309:404-13 pubmed
    ..Here, we describe the first selective antagonist of the histamine H4 receptor, the newest member of the histamine receptor family, and provide evidence that such antagonists have anti-..