Recombinant Human Histamine H1 receptor (HRH1)

1. H1R and H4R are useful biomarkers of allergic inflammation on the ocular surface. Most notably, H4R expressed on eosinophils is useful as a biomarker of eosinophilic inflammation of the ocular surface. PMID: 28391980
2. This study demonstrated that HRH1 gene polymorphisms associated with sedation in clozapine-treated patient with schizophrenia. PMID: 28400155
3. Human H1 receptors in Chinese hamster ovary cells are apparently down-regulated by a sustained increase in intracellular Ca(2+) concentrations with no process of endocytosis and lysosomal/proteasomal degradation of receptors. PMID: 29063596
4. Antihistamines displayed similar kinetic signatures on antagonizing histamine-induced beta-arrestin2 recruitment as compared to displacing radioligand binding from the H1R. PMID: 27468652
5. Study suggests that both MAPK p44/p42 and PKC pathways appear to be involved in histamine-upregulated matrix metalloproteinase-9 release via histamine H1 receptors in astrocytes. PMID: 25682263
6. that histamine H1 receptor activation mediates MAPK activation through PLCbeta, Src, PKCdelta and MEK pathway, but does not lead to nuclear relocalization of phospho-ERK (pERK), classically associated with pro-proliferative changes. PMID: 27871651
7. Activation of the H1R by its full agonists resulted in a composite potentiating effect. Intriguingly, inactivation of the Gaq-PLC pathway by H1R inverse agonists resulted also in a potentiation of GR activity. PMID: 26635083
8. HRH1-mediated sensitization of TRPV1 is involved in IBS. Ebastine, an antagonist of HRH1, reduced visceral hypersensitivity, symptoms, and abdominal pain in patients with IBS. PMID: 26752109
9. multiple signaling pathways contribute to histamine-induced endothelial barrier dysfunction via the H1 receptor. PMID: 25582918
10. 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. PMID: 25664905
11. HRH1 transcript was significantly down-modulated in multiple sclerose compared with health control. PMID: 25293806
12. The relationship between the expression of HRH1 and prognosis was found to vary in different types of cancers, even in the same cancer from different databases. PMID: 24535227
13. But carriers of one or three copies of HRH1 (5% of individuals), HRH2 (1.1%) and HRH4 genes (0.9%) were also identified. PMID: 24236486
14. Overexpression of H1R further increases the oxidative output of Duox-expressing HEK-293 cells. PMID: 23962049
15. Histamine demonstrably inhibited ACh-induced sweating in both mice and humans via H1R-mediated signaling. PMID: 23900020
16. our study does not support the contribution of histamine H1HR gene variants to antipsychotic induced weight gain nor differences in distribution between healthy volunteers and patients with schizophrenia PMID: 23609395
17. In this review, we focus on the role of histamine and its receptors in the treatment of Alzheimer's disease. PMID: 23677734
18. Our observations point to a close histamine-/HR-mediated activation of dermal macrophages, leading to modified cell differentiation and responsiveness via H1R, which might contribute to the aggravation of allergic skin inflammation in AD. PMID: 23414213
19. Histamine was able to synergistically augment bFGF-induced angiogenesis, and this action was linked to VEGF production through H1-receptor. PMID: 23225320
20. [review] The H1, H2, and H3 receptors are all involved in recovery of neurological function when extracellular histamine is gradually increasing, after cerebral ischemia. PMID: 22860191
21. Study revealed that epithelial cells and vascular endothelial cells showed intense immunoreactivity for histamine H1 receptor inperennial allergic rhinitis. PMID: 23132961
22. The glu349asp polymorphism of histamine-1 receptor is not associated with antipsychotic induced weight gain. PMID: 21937795
23. 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. PMID: 22169095
24. Measurement of H1R occupancy is a sensitive and absolute method to characterize the non-sedating property of drugs with H1 antagonistic activity. PMID: 21433074
25. the PKCdelta/ERK/poly(ADP-ribose) polymerase-1 signaling pathway is involved in histamine- or PMA-induced up-regulation of H1R gene expression in HeLa cells PMID: 21730054
26. H1 and PAR2 receptors enhance delivery of immune-competent cells and molecules by interrupting E-cadherin adhesion in lung epithelial cells. PMID: 21686228
27. crystal structure of the H(1)R complex with doxepin, a first-generation H(1)R antagonist PMID: 21697825
28. Results demonstrate that LPS, through TLR4 activation, up-regulates the expression and function of H1R and amplifies histamine-induced inflammatory responses in HCAEC. PMID: 21255012
29. Functional coupling of the H1R to Gq-PLC leads to the activation of RhoA and Rac small GTPases and suggest distinct roles for Rho GTPases in the control of cell proliferation by histamine. PMID: 19913013
30. could be detected at the feto-maternal interface of human PMID: 11603849
31. expressed on monocyte-derived dendritic cells PMID: 11898002
32. genetic variant of this protein and body weight change during clozapine treatment in schizophrenia PMID: 12218662
33. markedly different potency for activation of multiple signaling pathways by H1- and H2-HRs PMID: 12680587
34. there are three mechanisms for h1 receptor down regulation: phosphorylation of thr-140 or ser-398 or five sites PMID: 12755404
35. No significant differences in H1R or H2R mRNA levels between seasonal allergic rhinitic and nonrhinitic subjects in-season, despite observed differences in H reactivity. PMID: 12757445
36. Thr140 and Ser398 mainly contributed to downregulation, and Thr142 or Ser396 had a slight inhibitory effect on Thr140- or Ser398-mediated process, respectively PMID: 15328002
37. rapid termination of H1HR signaling is mediated by both the kinase activity and RGS function of GRK2 PMID: 15542600
38. 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 PMID: 15820830
39. gene expression regulation of HRH1 gene by HRH1 PMID: 15928828
40. expression in chondrocytes of osteoarthritic cartilage PMID: 15928843
41. analysis of agonist binding to histamine H(1) receptor PMID: 16027157
42. characterization of important steps in the activation of the human histamine H1 receptor PMID: 16408006
43. These data suggest the use of alternative promoters directing human H1 receptor gene expression, both within and between cell types. PMID: 16484687
44. The H1R-PKC-ERK pathway may play crucial roles in eliciting cytokine production from bronchial epithelial cells stimulated by histamine, leading to airway inflammation PMID: 16491014
45. results exclude the participation of histamine receptors other than the H1 subtype in the control of human intestinal motility by oxogenous histamine PMID: 16547808
46. histamine stimulates integrin alpha-V beta-3 expression in cultured trophoblast cells; the H1 receptor is implicated PMID: 16705383
47. Ascorbate enhancement of seven-transmembrane-spanning membrane receptor activity occurs in both adrenergic and histaminergic receptors. These receptors may play a significant role in maintaining extracellular ascorbate in a reduced state. PMID: 16760260
48. These data suggest postexercise skeletal muscle hyperemia exists in endurance trained men and women. PMID: 16888049
49. Histamine stimulates IL-6 release from SW982 cells by binding to the H1 receptor and this is coupled to the PI/PKC signal transduction pathway. PMID: 17122961
50. The data suggest a global functional analogy between H1 receptor activation and the meta I/meta II charge/discharge equilibrium in rhodopsin. PMID: 17243823

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HGNC: 5182

OMIM: 600167

KEGG: hsa:3269

STRING: 9606.ENSP00000380247

UniGene: Hs.1570