Property Summary

NCBI Gene PubMed Count 66
PubMed Score 1579.66
PubTator Score 82.90

Knowledge Summary

Patent (10,472)

Expression

  Differential Expression (1)

Disease log2 FC p
psoriasis 3.300 7.4e-187

MLP Assay (17)

AID Type Active / Inconclusive / Inactive Description
1788 other 0 / 0 / 0 Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity
1921 other 2 / 0 / 0 Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator: Ancillary Activity
434974 screening 0 / 0 / 0 Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen
504381 other 0 / 0 / 0 Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Set 2
624355 other 0 / 0 / 0 Late stage results from the probe development efforts to identify dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and nuclear factor NF-kappa-B (NF-kB): Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs
624406 other 0 / 0 / 0 Late stage results from the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs
652083 other 0 / 0 / 0 Late-stage results from the probe development effort to identify antagonists of OPRK1: CEREP radiometric-based biochemical counterscreen panel assay
686924 other 0 / 0 / 1 ML347 Eurofin Panel Assay for BMP Inhibitor (Probe Compound)
686925 other 0 / 0 / 1 ML352 Eurofin Panel Assay for Choline Transporter Inhibitor (Probe Compound)
686926 other 0 / 0 / 1 ML354 Eurofin Panel Assay for PAR4 Antagonists Inhibitor (Probe Compound)
More...

Gene RIF (51)

PMID Text
26475619 High constitutive Akt2 activity in U937 promonocytes: effective reduction of Akt2 phosphorylation by the histamine H2-receptor and the beta2-adrenergic receptor
25922853 Lack of Association between rs2067474 Polymorphism in Histamine Receptor H2 Gene and Breast Cancer in Chinese Han Population
25664905 Thus, the results in the initial study were due to the degradation of histamine in skeletal muscle by ascorbate, because the histaminergic vasodilatation was unaffected by N-acetylcysteine.
25192644 Cimetidine reversed the exercise-induced improvement in learning and memory in rats. Central histamine H2 receptors play an important role in mediating the beneficial effects of forced exercise on learning and memory.
24980224 upregulated on T regs following seasonal pollen exposure; allergen immunotherapy had no impact on the expression
24530738 The inhibitory effects of histamine on reactive oxygen species production in whole blood phagocytes are caused by H2R rather than H4R histamine receptors.
24236486 But carriers of one or three copies of HRH1 (5% of individuals), HRH2 (1.1%) and HRH4 genes (0.9%) were also identified.
23677734 In this review, we focus on the role of histamine and its receptors in the treatment of Alzheimer's disease.
23465664 HR signaling through cyclic AMP and exchange protein directly activated by cyclic AMP was required for the histamine effect on LPS-induced monocyte-derived dendritic cells responses
23280118 rs2607474 GG homozygote confers a significantly increased risk for age- and inflammation-related DAPK and CDH1 methylation in gastric epithelium.
22975449 HR2 receptor is involved in histamine-induced GDF-15 expression.
22860191 [review] The H1, H2, and H3 receptors are all involved in recovery of neurological function when extracellular histamine is gradually increasing, after cerebral ischemia.
22720301 The results suggest that HRH2 -1018 GG homozygote is a risk factor for the severity of gastric mucosal atrophy under the influence of H. pylori infection, especially in older subjects.
22615049 1018 GG homozygosity of HRH2 may be associated with the severity of gastric mucosal atrophy
22169095 evidence supports the involvement of histaminergic and gamma-aminobutyric acidergic mechanisms in the etiology of TS and show an overlap of rare CNVs in TS and autism spectrum disorder.
21705320 GRK2 induces desensitization of H2R through a phosphorylation-independent and RGS-dependent mechanism
21683759 Excitation of dentate nucleus neurons by histamine suggests that initiation and planning of movement is modulated by histaminergic projections.
21212009 Results describe the interactions between human H2 receptor and its agonists.
20628086 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
20602615 Observational study of gene-disease association. (HuGE Navigator)
20237496 Observational study of gene-disease association. (HuGE Navigator)
20012462 expression of H(2) during nicotinamide-induced differentiation of human amniotic epithelial cells into pancreatic beta-like cells may define a time-point, indicating involvement of histamine at the earlier stages
19913121 Observational study of gene-disease association. (HuGE Navigator)
19193342 Observational study of gene-disease association, gene-gene interaction, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
19156168 Clinical trial of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
19026982 Observational study of genetic testing. (HuGE Navigator)
18802338 role in allergy, autoimmunity, graft rejection, malignancy
18691388 These results suggest that the agonist-induced H2R internalization and ERK1/2 activation are partially dynamin-dependent. Furthermore, ERK1/2 activation via H2R is likely dependent of the endocytotic process rather than dynamin itself.
18617631 HRH2 trafficking was analyzed by examination of the roles of arrestin, dynamin, and clathrin on HRH2 internalization.
18258331 a dramatic alteration in the distribution of histamine receptors in colon cancer
17627982 Histamine excites human enteric neurones and this effect involves histamine H1-4 receptors.
17347323 The point mutation Cys-17 to Tyr-17 in the human histamine H2 receptor results in the formation of an H-bond between Tyr-17 and Asp-271 , favoring the stabilization of an active receptor conformation.
16888049 These data suggest postexercise skeletal muscle hyperemia exists in endurance trained men and women.
16203768 histamine exerts both a proproliferative and a proangiogenic effect via H2/H4 receptor activation, mediated by increasing COX-2-related PGE2 production in COX-2-expressing colon cancer cells
15961859 The equilibrium between receptor endocytosis and recycling is altered before H2R upregulation, probably via suppressing H2R degradation.
15953854 Observational study of gene-disease association. (HuGE Navigator)
15928843 expression in chondrocytes of osteoarthritic cartilage
15848191 Involvement of histamine H2 receptors in the histamine induced ets-1 expression in melanoma cells
15820830 expression of the histamine (H) receptors 1 (H1) and 2 (H2) by germinal, interstitial, and peritubular cells in the testes of fertile and infertile patients
15191551 human mast cells constitutively express primarily H2 and H4 receptors and that H2 receptors are functionally linked to cellular processes.
15167968 significant differences in H2 receptor expression in different vascular cell types might play a critical role in histamine induced cellular responses
14523557 Data show that the rapid and prolonged modulation of cell surface histamine H2 receptor levels by histamine was regulated solely via internalization.
12824943 Stimulation of phosphodiesterase IV is mediated by the H2 receptor and related to intracellular levels of cAMP.
12757445 No significant differences in H1R or H2R mRNA levels between seasonal allergic rhinitic and nonrhinitic subjects in-season, despite observed differences in H reactivity.
12680587 markedly different potency for activation of multiple signaling pathways by H1- and H2-HRs
12429384 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
11898002 expressed on monocyte-derived dendritic cells
11728449 histamine up-regulates LOX-1 expression via the H2 receptor in THP-1 monocytes
11641433 H2r exposure to an agonist caused desensitization controlled by H2r phosphorylation via GRK2 and GRK3.
11603849 could be detected at the feto-maternal interface of human
11466390 Histamine H2 receptors regulate intracellular Ca2+ levels exclusively by activation of nonselective cation channels, an effect which is inhibited via specific activation of protein kinase C isoform.

AA Sequence

MAPNGTASSFCLDSTACKITITVVLAVLILITVAGNVVVCLAVGLNRRLRNLTNCFIVSLAITDLLLGLL      1 - 70
VLPFSAIYQLSCKWSFGKVFCNIYTSLDVMLCTASILNLFMISLDRYCAVMDPLRYPVLVTPVRVAISLV     71 - 140
LIWVISITLSFLSIHLGWNSRNETSKGNHTTSKCKVQVNEVYGLVDGLVTFYLPLLIMCITYYRIFKVAR    141 - 210
DQAKRINHISSWKAATIREHKATVTLAAVMGAFIICWFPYFTAFVYRGLRGDDAINEVLEAIVLWLGYAN    211 - 280
SALNPILYAALNRDFRTGYQQLFCCRLANRNSHKTSLRSNASQLSRTQSREPRQQEEKPLKLQVWSGTEV    281 - 350
TAPQGATDR                                                                 351 - 359
//

Text Mined References (69)

PMID Year Title
26475619 2016 High constitutive Akt2 activity in U937 promonocytes: effective reduction of Akt2 phosphorylation by the histamine H2-receptor and the ?2-adrenergic receptor.
25922853 2015 Lack of Association between rs2067474 Polymorphism in Histamine Receptor H2 Gene and Breast Cancer in Chinese Han Population.
25664905 2015 Effect of antioxidants on histamine receptor activation and sustained postexercise vasodilatation in humans.
25192644 2014 The role of the central histaminergic receptors in the exercise-induced improvements of the spatial learning and memory in rats.
24980224 Histamine type 2 receptor expression on peripheral blood regulatory lymphocytes in patients with allergic rhinitis treated with specific immunotherapy.
24530738 2014 Role of histamine receptors in the effects of histamine on the production of reactive oxygen species by whole blood phagocytes.
24236486 2013 Variability in histamine receptor genes HRH1, HRH2 and HRH4 in patients with hypersensitivity to NSAIDs.
23677734 2013 The neglected role of histamine in Alzheimer's disease.
23465664 2013 Histamine receptor 2 modifies dendritic cell responses to microbial ligands.
23280118 2013 Influence of HRH2 promoter polymorphism on aberrant DNA methylation of DAPK and CDH1 in the gastric epithelium.
22975449 2012 Histamine receptor 2-mediated growth-differentiation factor-15 expression is involved in histamine-induced melanogenesis.
22860191 2012 Role of histamine and its receptors in cerebral ischemia.
22720301 2012 Effects of -1018G>A polymorphism of HRH2 (rs2607474) on the severity of gastric mucosal atrophy.
22615049 2012 Association between common genetic variant of HRH2 and gastric cancer risk.
22169095 2012 Rare copy number variants in tourette syndrome disrupt genes in histaminergic pathways and overlap with autism.
21705320 2011 Roles of phosphorylation-dependent and -independent mechanisms in the regulation of histamine H2 receptor by G protein-coupled receptor kinase 2.
21683759 2011 Histamine evokes excitatory response of neurons in the cerebellar dentate nucleus via H2 receptors.
21212009 2011 Computational investigation of interactions between human H2 receptor and its agonists.
20628086 2010 Variation at the NFATC2 locus increases the risk of thiazolidinedione-induced edema in the Diabetes REduction Assessment with ramipril and rosiglitazone Medication (DREAM) study.
20602615 2010 Physiogenomic analysis of statin-treated patients: domain-specific counter effects within the ACACB gene on low-density lipoprotein cholesterol?
20237496 2010 New genetic associations detected in a host response study to hepatitis B vaccine.
20012462 2010 Decrease in expression of histamine H2 receptors by human amniotic epithelial cells during differentiation into pancreatic beta-like cells.
19913121 2009 Gene-centric association signals for lipids and apolipoproteins identified via the HumanCVD BeadChip.
19193342 2008 Multiple genetic factors in olanzapine-induced weight gain in schizophrenia patients: a cohort study.
19156168 2009 Pharmacogenetics of antipsychotic response in the CATIE trial: a candidate gene analysis.
19054851 2008 Human protein factory for converting the transcriptome into an in vitro-expressed proteome,.
19026982 2009 High-throughput chemiluminometric genotyping of single nucleotide polymorphisms of histamine, serotonin, and adrenergic receptor genes.
18802338 2008 Regulatory effects of histamine and histamine receptor expression in human allergic immune responses.
18691388 2008 Agonist-induced internalization of histamine H2 receptor and activation of extracellular signal-regulated kinases are dynamin-dependent.
18617631 2008 Histamine H2 receptor trafficking: role of arrestin, dynamin, and clathrin in histamine H2 receptor internalization.
18258331 2008 Decreased expression of histamine H1 and H4 receptors suggests disturbance of local regulation in human colorectal tumours by histamine.
18240029 2008 Reviews in molecular biology and biotechnology: transmembrane signaling by G protein-coupled receptors.
17627982 2007 Histamine excites neurones in the human submucous plexus through activation of H1, H2, H3 and H4 receptors.
17347323 2007 Mutations of Cys-17 and Ala-271 in the human histamine H2 receptor determine the species selectivity of guanidine-type agonists and increase constitutive activity.
16888049 2006 H1 and H2 receptors mediate postexercise hyperemia in sedentary and endurance exercise-trained men and women.
16203768 2005 The role of cyclooxygenase-2 in mediating the effects of histamine on cell proliferation and vascular endothelial growth factor production in colorectal cancer.
15961859 2005 Alteration of intracellular histamine H2 receptor cycling precedes antagonist-induced upregulation.
15953854 2005 Polymorphisms of high-affinity IgE receptor and histamine-related genes in patients with ASA-induced urticaria/angioedema.
15928843 2005 Demonstration of histamine H1 and H2 receptors in chondrocytes of human osteoarthritic cartilage.
15848191 2005 Histamine elevates the expression of Ets-1, a protooncogen in human melanoma cell lines through H2 receptor.
15820830 2005 Evidence for a histaminergic system in the human testis.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
15191551 2004 Human skin mast cells express H2 and H4, but not H3 receptors.
15167968 2004 Polyclonal anti-histamine H2 receptor antibodies detect differential expression of H2 receptor protein in primary vascular cell types.
15086532 2004 Identification of a novel family of G protein-coupled receptor associated sorting proteins.
15014171 2004 Human-specific amino acid changes found in 103 protein-coding genes.
14523557 2003 Nitric oxide mediates histamine induced down-regulation of H2 receptor mRNA and internalization of the receptor protein (R1).
12824943 2003 Histamine up-regulates phosphodiesterase IV activity in U-937 cells through H2 receptor stimulation and cAMP increase.
12757445 2003 Epidermal growth factor receptor - but not histamine receptor - is upregulated in seasonal allergic rhinitis.
12680587 2003 Differential activation of dual signaling responses by human H1 and H2 histamine receptors.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12429384 2002 Investigation of promoter variants of the histamine 1 and 2 receptors in schizophrenia and clozapine response.
12036966 2002 Selective inhibition of heterotrimeric Gs signaling. Targeting the receptor-G protein interface using a peptide minigene encoding the Galpha(s) carboxyl terminus.
11898002 2002 Expression and function of histamine receptors 1 and 2 on human monocyte-derived dendritic cells.
11728449 2001 Histamine increases the expression of LOX-1 via H2 receptor in human monocytic THP-1 cells.
11641433 2001 Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases.
11603849 2001 Localisation of mRNAs for diamine oxidase and histamine receptors H1 and H2, at the feto-maternal interface of human pregnancy.
11466390 2001 Inhibition of H2 histamine receptor-mediated cation channel opening by protein kinase C in human promyelocytic cells.
10837353 2000 The human histamine H(2) receptor regulates c-jun and c-fos in a differential manner.
10371214 1999 Human histamine H2 receptor gene: multiple transcription initiation and tissue-specific expression.
9725260 1998 Histamine potently suppresses human IL-12 and stimulates IL-10 production via H2 receptors.
9374694 1997 Novel insights into histamine H2 receptor biology.
9311023 1997 International Union of Pharmacology. XIII. Classification of histamine receptors.
8817552 1996 Allelic variations of the human histamine H2 receptor gene.
7794271 1995 The guinea pig histamine H2 receptor: gene cloning, tissue expression and chromosomal localization of its human counterpart.
7755641 1995 Identification of the promoter region of the human histamine H2-receptor gene.
7575521 1995 Visualization of agonist-induced internalization of histamine H2 receptors.
7511596 1994 Histamine enhances interleukin (IL)-1-induced IL-6 gene expression and protein synthesis via H2 receptors in peripheral blood mononuclear cells.
1714721 1991 Molecular cloning of the human histamine H2 receptor.