PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 32572668-11 2020 At the histamine-binding site in hH1R, the distinct interactions established between the phenyl and chlorophenyl moieties of the two enantiomers with the amino acids lining up the pocket and between their free carboxylates and Lys179 in the second extracellular loop account for the improved pharmacological profile of (R)-cetirizine. Histamine 7-16 histamine receptor H1 Homo sapiens 33-37 33918180-0 2021 Analysis of Missense Variants in the Human Histamine Receptor Family Reveals Increased Constitutive Activity of E4106.30x30K Variant in the Histamine H1 Receptor. Histamine 43-52 histamine receptor H1 Homo sapiens 140-161 33918180-6 2021 The E4106.30x30K missense variant displays a higher affinity for the endogenous agonist histamine than wild-type H1R, whereas antagonist affinity was not affected. Histamine 88-97 histamine receptor H1 Homo sapiens 113-116 33443845-13 2021 Iba-1 fluorescence, cell area and phagocytosis were enhanced by histamine through H1R. Histamine 64-73 histamine receptor H1 Homo sapiens 82-85 32536619-7 2020 Crotamiton strongly inhibited histamine-induced calcium influx in HEK293T cells, expressing both histamine receptor 1 (H1R) and transient receptor potential vanilloid 1 (TRPV1), as a model of histamine-induced itching. Histamine 30-39 histamine receptor H1 Homo sapiens 119-122 33080103-2 2020 In this study, we analysed the role and expression of histamine receptor 1 (HRH1) in haematological malignancies. Histamine 54-63 histamine receptor H1 Homo sapiens 76-80 22436-4 1977 Inhibition of histamine-induced skin whealing appears to be a quantitative index of the time course of histamine H1-receptor antagonist action. Histamine 14-23 histamine receptor H1 Homo sapiens 103-124 33497977-7 2021 Results showed that the local anesthetics can directly occupy histamine binding sites on H1R, and the KD values obtained from different CMC methods exhibited positive correlations with each other (p < 0.01). Histamine 62-71 histamine receptor H1 Homo sapiens 89-92 33497977-9 2021 This was not only in line with the Ca2+ responses in activating H1R, but also consistent with the same amino acid residues shared with histamine in the H1R active site. Histamine 135-144 histamine receptor H1 Homo sapiens 152-155 32521742-1 2020 H1-antihistamines antagonize histamine and prevent it from binding to the histamine H1 receptor (H1R). Histamine 7-16 histamine receptor H1 Homo sapiens 74-95 32764823-8 2020 Histamine increased the expression of H1R, H2R and H4R as well as of interleukin-6, cyclooxygenase-2, and prostaglandin-E2 secretion even without pressure application and induced receptor activator of NF-kB ligand (RANKL) protein expression with unchanged osteoprotegerin secretion. Histamine 0-9 histamine receptor H1 Homo sapiens 38-41 32521742-1 2020 H1-antihistamines antagonize histamine and prevent it from binding to the histamine H1 receptor (H1R). Histamine 7-16 histamine receptor H1 Homo sapiens 97-100 32395857-4 2021 Histamine and its G-protein coupled receptors (H1R-H4R) play vital roles in multiple cancer-associated processes in TME, where histamine is mainly produced by mast cells. Histamine 0-9 histamine receptor H1 Homo sapiens 47-50 32395857-4 2021 Histamine and its G-protein coupled receptors (H1R-H4R) play vital roles in multiple cancer-associated processes in TME, where histamine is mainly produced by mast cells. Histamine 127-136 histamine receptor H1 Homo sapiens 47-50 32061592-3 2020 It has been reported that LA is a potential exogenous ligand for histamine receptor 1 (H1R). Histamine 65-74 histamine receptor H1 Homo sapiens 87-90 32127042-15 2020 Histamine significantly promoted myocardial differentiation from human induced pluripotent stem cells (hiPSCs) with better structure and function via a H1R-dependent signal. Histamine 0-9 histamine receptor H1 Homo sapiens 152-155 31949043-10 2020 These results indicate that histamine controls HA metabolism by up-regulating HYBID and down-regulating HAS2 via distinct signaling pathways downstream of histamine receptor H1. Histamine 28-37 histamine receptor H1 Homo sapiens 155-176 33148907-1 2020 The purpose of this study is to examine the effect of intranasal corticosteroid (INCS) administration on histamine H1 receptor (H1R) gene expression in the nasal mucosa of healthy participants and the effects of dexamethasone on basal and histamine-induced H1R mRNA expression, and histamine-induced phosphorylation of extracellular signal-regulated kinase (ERK) in HeLa cells. Histamine 105-114 histamine receptor H1 Homo sapiens 128-131 33148907-6 2020 Dexamethasone suppressed basal levels of H1R mRNA, and histamine-induced up-regulation of H1R mRNA and ERK phosphorylation in HeLa cells. Histamine 55-64 histamine receptor H1 Homo sapiens 90-93 33148907-7 2020 These data suggested that corticosteroid inhibited both basal transcription and histamine-induced transcriptional activation of H1R through its suppression of ERK phosphorylation in the signaling pathway involved in H1R gene transcription. Histamine 80-89 histamine receptor H1 Homo sapiens 128-131 33148907-7 2020 These data suggested that corticosteroid inhibited both basal transcription and histamine-induced transcriptional activation of H1R through its suppression of ERK phosphorylation in the signaling pathway involved in H1R gene transcription. Histamine 80-89 histamine receptor H1 Homo sapiens 216-219 30742585-3 2019 The pleiotropic effects of histamine are mediated by four types of receptors that belong to the G-protein-coupled receptor family: histamine H1 receptor (HRH-1), histamine H2 receptor, histamine H3 receptor, and histamine H4 receptor. Histamine 27-36 histamine receptor H1 Homo sapiens 131-152 31718622-8 2019 RESULTS: The expression of four histamine receptors was significantly elevated in BPS/IC (H1R, P < 0.001; H2R, P = 0.031; H3R, P = 0.008; H4R, P = 0.048). Histamine 32-41 histamine receptor H1 Homo sapiens 90-93 31338198-1 2019 Some histamine H1 receptor (H1R) antagonists induce adverse sedative reactions caused by blockade of histamine transmission in the brain. Histamine 5-14 histamine receptor H1 Homo sapiens 28-31 30629470-8 2019 In HS, pretreatment with histamine significantly increased the Ca2+ responses to cinnamaldehyde and GSK1016790A, an effect prevented by H1R antagonism. Histamine 25-34 histamine receptor H1 Homo sapiens 136-139 30629470-11 2019 We demonstrate that the mucosal microenvironment in IBS contains mediators, such as histamine, which sensitize TRPV4 and TRPA1 via H1R activation, most likely contributing to increased visceral pain perception in IBS. Histamine 84-93 histamine receptor H1 Homo sapiens 131-134 31083709-5 2019 Using a serial addition of increasing concentrations of a GPCR agonist while continuously monitoring the sample"s impedance, we were able to establish a full concentration-response curve for the endogenous agonist histamine on a single layer of U-373 MG cells endogenously expressing the histamine 1 receptor (H1R). Histamine 214-223 histamine receptor H1 Homo sapiens 288-308 31083709-5 2019 Using a serial addition of increasing concentrations of a GPCR agonist while continuously monitoring the sample"s impedance, we were able to establish a full concentration-response curve for the endogenous agonist histamine on a single layer of U-373 MG cells endogenously expressing the histamine 1 receptor (H1R). Histamine 214-223 histamine receptor H1 Homo sapiens 310-313 30462522-8 2019 The bimodal functions of histamine include protumorigenic effects through H1R and antitumorigenic effects via H2R, and these results were supported by gene expression profiling studies on tumor specimens of patients with colorectal cancer. Histamine 25-34 histamine receptor H1 Homo sapiens 74-77 30742585-3 2019 The pleiotropic effects of histamine are mediated by four types of receptors that belong to the G-protein-coupled receptor family: histamine H1 receptor (HRH-1), histamine H2 receptor, histamine H3 receptor, and histamine H4 receptor. Histamine 27-36 histamine receptor H1 Homo sapiens 154-159 30742585-8 2019 In both groups HRH-1 mRNA gene expression was observed as statistically significant increased after histamine stimulation compared to cells not treated, while in HRH-4 only in allergy group we observed statistical increase. Histamine 100-109 histamine receptor H1 Homo sapiens 15-20 30742585-9 2019 FXF successively blocked histamine affinity in HRH-1 mRNA gene expression but not in HRH-4, where we not observed any reaction. Histamine 25-34 histamine receptor H1 Homo sapiens 47-52 31212298-7 2019 CONCLUSION: The TRPV4 agonist RN-1747, and possibly also the structurally similar TRPV4 antagonist RN-1734, should be used with caution because of yet unidentified interference with histamine signaling via H1R. Histamine 182-191 histamine receptor H1 Homo sapiens 206-209 31212298-2 2019 Histamine acting via histamine 1 receptor (H1R) to open TRP cation channels might also be involved. Histamine 0-9 histamine receptor H1 Homo sapiens 21-41 29615980-3 2018 We observed concentration-dependent increases in cytosolic Ca2+ concentrations after treatment with histamine (1-100 microM) and complete suppression of histamine-induced Ca2+ mobilizations by H1 histamine receptor (H1R) antagonist d-chlorpheniramine (d-CPA) in hRPE-YC cells. Histamine 100-109 histamine receptor H1 Homo sapiens 193-219 31212298-2 2019 Histamine acting via histamine 1 receptor (H1R) to open TRP cation channels might also be involved. Histamine 0-9 histamine receptor H1 Homo sapiens 43-46 31212298-3 2019 METHOD: The enterochromaffin cell line P-STS, responsive to histamine via H1R, was used as model to study possible synergism between histamine and TRP vanilloid 4 (TRPV4) pathways. Histamine 60-69 histamine receptor H1 Homo sapiens 74-77 30498974-1 2018 Binding of histamine to the G-protein coupled histamine H1 receptor plays an important role in the context of allergic reactions; however, no crystal structure of the resulting complex is available yet. Histamine 11-20 histamine receptor H1 Homo sapiens 46-67 29615980-3 2018 We observed concentration-dependent increases in cytosolic Ca2+ concentrations after treatment with histamine (1-100 microM) and complete suppression of histamine-induced Ca2+ mobilizations by H1 histamine receptor (H1R) antagonist d-chlorpheniramine (d-CPA) in hRPE-YC cells. Histamine 153-162 histamine receptor H1 Homo sapiens 193-219 30012475-13 2018 SIGNIFICANCE: Histamine suppresses apo A-I gene expression in hepatocytes via the histamine H1 receptor by elevating NF-kappaB expression and binding to the apo A-I promoter. Histamine 14-23 histamine receptor H1 Homo sapiens 82-103 30150993-7 2018 Both H1R and H4R have important roles in the progression and modulation of histamine-mediated allergic diseases. Histamine 75-84 histamine receptor H1 Homo sapiens 5-16 30150993-10 2018 In the present review, we examine the accumulating evidence suggesting novel therapeutic approaches that explore both H1R and H4R as therapeutic targets for histamine-mediated allergic diseases. Histamine 157-166 histamine receptor H1 Homo sapiens 118-121 29027719-9 2018 EGC expressed H1R and the effects of supernatant upon Ca2+ response to ATP in EGC were blocked by pyrilamine and reproduced by histamine via H1R. Histamine 127-136 histamine receptor H1 Homo sapiens 14-17 29027719-9 2018 EGC expressed H1R and the effects of supernatant upon Ca2+ response to ATP in EGC were blocked by pyrilamine and reproduced by histamine via H1R. Histamine 127-136 histamine receptor H1 Homo sapiens 141-144 29027719-13 2018 Histamine, via activation of H1R-dependent pathways, partly mediates altered Ca2+ response to ATP in EGC. Histamine 0-9 histamine receptor H1 Homo sapiens 29-32 29615980-7 2018 Treatment of hRPE-YC cells with d-CPA or with more specific H1R antagonist, ketotifen, blocked the histamine-induced phase shifts. Histamine 99-108 histamine receptor H1 Homo sapiens 60-63 29433511-7 2018 RESULTS: Astrocytes could constitutively express three histamine receptors (H1R, H2R, and H3R), and these three histamine receptors could be selectively upregulated to varying degrees upon histamine treatment. Histamine 55-64 histamine receptor H1 Homo sapiens 76-79 29433511-9 2018 The effects of histamine were completely abolished by either an H1R or H3R antagonist, while an H2R antagonist attenuated the effects partly. Histamine 15-24 histamine receptor H1 Homo sapiens 64-67 27843000-0 2017 Changes in gene expression induced by histamine, fexofenadine and osthole: Expression of histamine H1 receptor, COX-2, NF-kappaB, CCR1, chemokine CCL5/RANTES and interleukin-1beta in PBMC allergic and non-allergic patients. Histamine 38-47 histamine receptor H1 Homo sapiens 89-110 30032131-4 2018 The presence of histamine or agonists targeting the H1R, H2R and, in particular, the H4R during in vitro differentiation from monocytes to macrophages modified the M2 phenotype by regulating the macrophage differentiation marker CD68 and CD163 expressions. Histamine 16-25 histamine receptor H1 Homo sapiens 52-60 29033838-6 2017 Using a calcium-sensitive fluorescent dye and a label free, dynamic mass redistribution based assay, functional recovery of the H1R responsiveness was measured by stimulating the cells with histamine over time, and the recovery was quantified as the receptor recovery time. Histamine 190-199 histamine receptor H1 Homo sapiens 128-131 27843000-2 2017 This paper compares results of histamine, FXF and osthole impact on HRH-1, COX-2, NF-kappaB-p50, CCR1 mRNA expression. Histamine 31-40 histamine receptor H1 Homo sapiens 68-73 28332048-5 2017 Histamine released from mast cells and basophils exerts its biological activities by activating four G protein-coupled receptors, namely H1R, H2R, H3R (expressed mainly in the brain), and the recently identified H4R. Histamine 0-9 histamine receptor H1 Homo sapiens 137-140 27751876-5 2016 The calcium and the impedimetric assay depended on Gq coupling of the H1R, as demonstrated by complete inhibition of the histamine-induced signals in the presence of the Gq inhibitor FR900359 (UBO-QIC). Histamine 121-130 histamine receptor H1 Homo sapiens 70-73 27468652-5 2016 Antihistamines displayed similar kinetic signatures on antagonizing histamine-induced beta-arrestin2 recruitment as compared to displacing radioligand binding from the H1R. Histamine 4-13 histamine receptor H1 Homo sapiens 168-171 27358232-3 2016 The four histamine receptor subtypes (H1R, H2R, H3R, and H4R) respond to the ligand histamine by activating three canonical heterotrimeric G-protein-mediated signaling pathways with a reported high degree of specificity. Histamine 9-18 histamine receptor H1 Homo sapiens 38-41 27170049-10 2016 Orbital fibroblasts expressed HRH1 and loratadine and SC-514 both blocked histamine-induced IL-6, IL-8 and CCL2 production by orbital fibroblasts. Histamine 74-83 histamine receptor H1 Homo sapiens 30-34 25909280-5 2015 Genotyping was performed to detect known SNPs (n = 10) among genes (HDC, HNMT, ABP1, HRH1, and HRH4) within the histamine pathway. Histamine 112-121 histamine receptor H1 Homo sapiens 85-89 25682263-4 2016 Histamine, a major aminergic brain neurotransmitter, stimulates the production of MMP-9 in keratinocytes through the histamine H1 receptor (H1R). Histamine 0-9 histamine receptor H1 Homo sapiens 117-138 25682263-4 2016 Histamine, a major aminergic brain neurotransmitter, stimulates the production of MMP-9 in keratinocytes through the histamine H1 receptor (H1R). Histamine 0-9 histamine receptor H1 Homo sapiens 140-143 26752109-12 2016 Moreover, TRPV1 responses of submucosal neurons from healthy volunteers could be potentiated by their pre-incubation with histamine; this effect was blocked by the HRH1 antagonist pyrilamine. Histamine 122-131 histamine receptor H1 Homo sapiens 164-168 26440050-8 2016 We further demonstrate that several intracellular signaling pathways are involved in histamine-induced TR3 transcript variants, including histamine receptor H1-mediated phospholipase C (PLC)/calcium /calcineurin/protein kinase C (PKC)/protein kinase D (PKD) pathway and ERK pathway, as well as histamine receptor H3-mediated PKC-ERK pathway. Histamine 85-94 histamine receptor H1 Homo sapiens 138-159 26619301-4 2016 Here, we report the mechanism of MBCA on phorbol 12-myristate-13-acetate (PMA)- or histamine-induced upregulation of H1R gene expression in HeLa cells, and in vivo effects of MBCA were also determined in toluene-2,4-diisocyanate (TDI)-sensitized rats. Histamine 83-92 histamine receptor H1 Homo sapiens 117-120 27872516-12 2016 Histamine had a proliferative effect on both HPFs and HCFs, the effective concentration (10 mumol/L) on HPFs was lower than on HCFs (100 mumol/L), and the effect could be blocked by H1R antagonist. Histamine 0-9 histamine receptor H1 Homo sapiens 182-185 27872516-15 2016 Histamine may play an important role in the proliferation of HPFs and act through H1R. Histamine 0-9 histamine receptor H1 Homo sapiens 82-85 26398212-7 2015 Calcium increase patterns of HeLa cells were conserved at any histamine concentrations tested, whereas the overexpression of histamine H1 receptor, which robustly increased histamine-induced inositol phospholipid hydrolysis, converted calcium oscillations to sustained calcium increases only at high histamine concentrations. Histamine 62-71 histamine receptor H1 Homo sapiens 125-146 25712856-7 2015 Combined stimulation with histamine and Pam3CSK4 or LPS led to a significant amplification in expression of CCL20 and IL-8 when compared with treatment with each stimulant alone (p < 0.05), and this effect was mediated via pathways involving the H1R (p < 0.05). Histamine 26-35 histamine receptor H1 Homo sapiens 249-252 26598006-6 2015 These findings suggest that antihistamines suppressed histamine-induced transcriptional activation of H1R gene in the nasal mucosa, in addition to their blocking effect against histamine on H1R, resulting in a decrease of nasal symptoms. Histamine 32-41 histamine receptor H1 Homo sapiens 102-105 26598006-6 2015 These findings suggest that antihistamines suppressed histamine-induced transcriptional activation of H1R gene in the nasal mucosa, in addition to their blocking effect against histamine on H1R, resulting in a decrease of nasal symptoms. Histamine 32-41 histamine receptor H1 Homo sapiens 190-193 26598006-6 2015 These findings suggest that antihistamines suppressed histamine-induced transcriptional activation of H1R gene in the nasal mucosa, in addition to their blocking effect against histamine on H1R, resulting in a decrease of nasal symptoms. Histamine 54-63 histamine receptor H1 Homo sapiens 102-105 26598006-7 2015 These findings further suggest that by their inverse agonistic activity, antihistamines suppress the basal transcription of nasal H1R in the absence of histamine in responders. Histamine 77-86 histamine receptor H1 Homo sapiens 130-133 26057691-4 2015 It turned out that histamine-induced intracellular calcium increase was significantly blocked by caffeic acid in HEK293T cells that express H1R and TRPV1, molecules required for transmission of histamine-induced itch in sensory neurons. Histamine 19-28 histamine receptor H1 Homo sapiens 140-143 26057691-4 2015 It turned out that histamine-induced intracellular calcium increase was significantly blocked by caffeic acid in HEK293T cells that express H1R and TRPV1, molecules required for transmission of histamine-induced itch in sensory neurons. Histamine 194-203 histamine receptor H1 Homo sapiens 140-143 26036574-5 2015 Interestingly, an H1R antagonist, but not H2R or H4R antagonists, antagonized the histamine-mediated suppression of alphaSMA expression by TGF-beta1. Histamine 82-91 histamine receptor H1 Homo sapiens 18-21 25872410-10 2015 RESULTS: The MUC5AC expression levels were increased by histamine treatment in either nasal tissues of Der f challenged guinea pigs or NCI-H292 cells, whereas the MUC5AC protein over-production induced by histamine administration was significantly inhibited by H1R antagonist chlorpheniramine. Histamine 56-65 histamine receptor H1 Homo sapiens 261-264 25872410-10 2015 RESULTS: The MUC5AC expression levels were increased by histamine treatment in either nasal tissues of Der f challenged guinea pigs or NCI-H292 cells, whereas the MUC5AC protein over-production induced by histamine administration was significantly inhibited by H1R antagonist chlorpheniramine. Histamine 205-214 histamine receptor H1 Homo sapiens 261-264 25137637-3 2014 Many of the allergic and inflammatory actions of histamine are mediated by the histamine H1 receptor. Histamine 49-58 histamine receptor H1 Homo sapiens 79-100 25723478-13 2015 Histamine directly activates esophageal epithelial cytokine secretion in vitro in an H1R dependent fashion. Histamine 0-9 histamine receptor H1 Homo sapiens 85-88 25374757-0 2014 Histamine Promotes the Release of Interleukin-6 via the H1R/p38 and NF-kappaB Pathways in Nasal Fibroblasts. Histamine 0-9 histamine receptor H1 Homo sapiens 56-59 25374757-8 2014 Among the histamine-receptor specific antagonists, only the H1R antagonist significantly decreased IL-6 production in histamine-stimulated nasal fibroblasts. Histamine 10-19 histamine receptor H1 Homo sapiens 60-63 25374757-10 2014 The H1R antagonist actively suppressed pp38 and NF-kappaB expression in histamine-induced nasal fibroblasts, but not pERK and pJNK. Histamine 72-81 histamine receptor H1 Homo sapiens 4-7 24809793-0 2014 Histamine induces human lung fibroblast-mediated collagen gel contraction via histamine H1 receptor. Histamine 0-9 histamine receptor H1 Homo sapiens 78-99 24631173-1 2014 The present study was undertaken to characterize the presence of histamine H1R using molecular biology tools and unravel the influx and release mechanism(s) involved in calcium signalling cascades in histamine-induced myometrial contraction in buffaloes. Histamine 65-74 histamine receptor H1 Homo sapiens 75-78 24752587-3 2014 In the present study, we found that microglia can constitutively express all four histamine receptors (H1R, H2R, H3R, and H4R), and the expression of H1R and H4R can be selectively upregulated in primary cultured microglia in a dose-dependent manner by histamine. Histamine 82-91 histamine receptor H1 Homo sapiens 150-161 24752587-5 2014 The antagonists of H1R and H4R but not H2R and H3R reduced histamine-induced TNF-alpha and IL-6 production, MAPK and PI3K/AKT pathway activation, and mitochondrial membrane potential loss in microglia, suggesting that the actions of histamine are via H1R and H4R. Histamine 59-68 histamine receptor H1 Homo sapiens 19-30 24752587-5 2014 The antagonists of H1R and H4R but not H2R and H3R reduced histamine-induced TNF-alpha and IL-6 production, MAPK and PI3K/AKT pathway activation, and mitochondrial membrane potential loss in microglia, suggesting that the actions of histamine are via H1R and H4R. Histamine 59-68 histamine receptor H1 Homo sapiens 251-262 24752587-5 2014 The antagonists of H1R and H4R but not H2R and H3R reduced histamine-induced TNF-alpha and IL-6 production, MAPK and PI3K/AKT pathway activation, and mitochondrial membrane potential loss in microglia, suggesting that the actions of histamine are via H1R and H4R. Histamine 233-242 histamine receptor H1 Homo sapiens 19-30 24752587-9 2014 We also demonstrate that histamine induced TNF-alpha and IL-6 release from activated microglia via H1R and H4R-MAPK and PI3K/AKT-NF-kappa B signaling pathway, which will deepen the understanding of microglia-mediated neuroinflammatory symptoms of chronic neurodegenerative disease. Histamine 25-34 histamine receptor H1 Homo sapiens 99-110 24535227-4 2014 We identified 88 SNPs including 4 available alleles disrupting an existing exonic splicing enhancer and 84 SNPs causing missense mutation, which may impact the effect of histamine on the HRH1 protein. Histamine 170-179 histamine receptor H1 Homo sapiens 187-191 23962049-0 2014 Histamine stimulates hydrogen peroxide production by bronchial epithelial cells via histamine H1 receptor and dual oxidase. Histamine 0-9 histamine receptor H1 Homo sapiens 84-105 24450605-11 2014 While enhancement of histamine-mediated wound healing is mediated predominantly via the HRH1 receptor, other keratinocyte-expressed receptors are also involved. Histamine 21-30 histamine receptor H1 Homo sapiens 88-92 23962049-10 2014 Using HEK-293 cells expressing Duox1 or Duox2 and endogenous H1R, histamine triggers an immediate intracellular calcium signal and H2O2 release. Histamine 66-75 histamine receptor H1 Homo sapiens 61-64 23962049-8 2014 Out of the four histamine receptors (H1R-H4R), H1R has the highest expression in BECs and mediates the H2O2-producing effects of histamine. Histamine 16-25 histamine receptor H1 Homo sapiens 37-40 23962049-8 2014 Out of the four histamine receptors (H1R-H4R), H1R has the highest expression in BECs and mediates the H2O2-producing effects of histamine. Histamine 16-25 histamine receptor H1 Homo sapiens 47-50 23414213-8 2013 RESULTS: We demonstrated that FcepsilonRI stimulation promotes the generation of H1R-expressing macrophage-like cells with enhanced histamine biosynthesis and H1R-mediated proinflammatory properties. Histamine 132-141 histamine receptor H1 Homo sapiens 81-84 24312564-9 2013 Histamine induced large whole cell currents in HEK293 cells co-expressing TRPV1 and the histamine H1 receptor, and the TRPV1 antagonist capsazepine abolished these currents. Histamine 0-9 histamine receptor H1 Homo sapiens 88-109 23709238-9 2013 CONCLUSION: Ductal epithelial cells are non-professional histamine-producing cells able to release histamine via OCTs at the resting state up to ~100 nM, enough to excite H3R/H4R(+) epithelial cells, but not H1R, which requires burst release from mast cells. Histamine 99-108 histamine receptor H1 Homo sapiens 208-211 23677734-4 2013 The Histamine mediates its functions via its 4 G-protein-coupled Histamine H1 receptor (H1R) to histamine H1 receptor (H4R). Histamine 4-13 histamine receptor H1 Homo sapiens 65-86 23677734-4 2013 The Histamine mediates its functions via its 4 G-protein-coupled Histamine H1 receptor (H1R) to histamine H1 receptor (H4R). Histamine 4-13 histamine receptor H1 Homo sapiens 88-91 23677734-4 2013 The Histamine mediates its functions via its 4 G-protein-coupled Histamine H1 receptor (H1R) to histamine H1 receptor (H4R). Histamine 4-13 histamine receptor H1 Homo sapiens 96-117 23414213-10 2013 CONCLUSION: 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. Histamine 46-55 histamine receptor H1 Homo sapiens 167-170 23333628-3 2013 Recently, we demonstrated that histamine or phorbol-12-myristate-13-acetate (PMA) stimulation induced the up-regulation of H1R gene expression through the protein kinase Cdelta (PKCdelta)/extracellular signal-regulated kinase/poly(ADP-ribose) polymerase-1 signaling pathway in HeLa cells expressing H1R endogenously. Histamine 31-40 histamine receptor H1 Homo sapiens 123-126 23453703-1 2013 Antihistamines are thought to antagonize histamine and prevent it from binding to the histamine H1 receptor (H1R). Histamine 4-13 histamine receptor H1 Homo sapiens 86-107 23453703-1 2013 Antihistamines are thought to antagonize histamine and prevent it from binding to the histamine H1 receptor (H1R). Histamine 4-13 histamine receptor H1 Homo sapiens 109-112 23453703-8 2013 Both inverse agonists and neutral antagonists suppressed histamine-induced H1R mRNA elevation. Histamine 57-66 histamine receptor H1 Homo sapiens 75-78 23333628-6 2013 In the present study, we examined the effect of quercetin on histamine- and PMA-induced up-regulation of H1R gene expression in HeLa cells. Histamine 61-70 histamine receptor H1 Homo sapiens 105-108 23333628-8 2013 Quercetin suppressed histamine- and PMA-induced up-regulation of H1R gene expression. Histamine 21-30 histamine receptor H1 Homo sapiens 65-68 22582780-1 2012 CONCLUSION: The data suggest that histamine up-regulates MUC2 gene regulation and mucin production in airway epithelial cells through histamine 1 receptor (H1R). Histamine 34-43 histamine receptor H1 Homo sapiens 134-154 23220277-9 2013 Finally, we dock agonist histamine into H1R and H4R, and then perform 20ns MD simulations for the complexes. Histamine 25-34 histamine receptor H1 Homo sapiens 40-43 23220277-10 2013 H1R or H4R bound with histamine show strong conformational changes from TM5, TM6 and TM7, outward movement of intracellular part of TM6, and conformational change of Tyr(7.53), which is consistent with the recent crystal structures of active GPCRs. Histamine 22-31 histamine receptor H1 Homo sapiens 0-3 22582780-1 2012 CONCLUSION: The data suggest that histamine up-regulates MUC2 gene regulation and mucin production in airway epithelial cells through histamine 1 receptor (H1R). Histamine 34-43 histamine receptor H1 Homo sapiens 156-159 22582780-2 2012 Histamine appears to play an important role in the early phase of mucin regulation, which might be effectively blocked by an H1R antagonist. Histamine 0-9 histamine receptor H1 Homo sapiens 125-128 22582780-12 2012 Histamine-induced MUC2 mRNA expression and mucin secretion were significantly suppressed by pretreatment with H1R antagonist. Histamine 0-9 histamine receptor H1 Homo sapiens 110-113 22304689-5 2012 The histamine H1 receptor (H1R) agonist 2-pyridylethylamine and H2R agonist dimaprit down-regulated the expression of NKG2D ligands, and activation of H1R and H2R signalling by A23187 and forskolin, respectively, had the same effect, indicating that the histamine-induced down-regulation of NKG2D ligands is mediated by H1R and H2R. Histamine 4-13 histamine receptor H1 Homo sapiens 27-30 22304689-5 2012 The histamine H1 receptor (H1R) agonist 2-pyridylethylamine and H2R agonist dimaprit down-regulated the expression of NKG2D ligands, and activation of H1R and H2R signalling by A23187 and forskolin, respectively, had the same effect, indicating that the histamine-induced down-regulation of NKG2D ligands is mediated by H1R and H2R. Histamine 4-13 histamine receptor H1 Homo sapiens 151-154 22304689-5 2012 The histamine H1 receptor (H1R) agonist 2-pyridylethylamine and H2R agonist dimaprit down-regulated the expression of NKG2D ligands, and activation of H1R and H2R signalling by A23187 and forskolin, respectively, had the same effect, indicating that the histamine-induced down-regulation of NKG2D ligands is mediated by H1R and H2R. Histamine 4-13 histamine receptor H1 Homo sapiens 151-154 22304689-10 2012 These results suggest that histamine down-regulates NKG2D ligands through the activation of an H1R- and H2R-mediated ubiquitin-proteasome pathway and consequently reduces susceptibility to NK cells. Histamine 27-36 histamine receptor H1 Homo sapiens 95-98 22232416-10 2012 In contrast, H1R and H4R with opposing subset-related expression may have a regulatory or fine-tuning role in histamine-induced functional activities. Histamine 110-119 histamine receptor H1 Homo sapiens 13-16 22100544-7 2012 Activated Galpha(q) physically interacts with the relevant portions of LARG in COS-7 cells and histamine causes activation of LARG in native HeLa cells endogenously expressing HRH1, G(q), and LARG. Histamine 95-104 histamine receptor H1 Homo sapiens 176-180 22186623-5 2012 These results suggest that inverse agonists more potently alleviate allergy symptoms by not only inhibiting stimulus-induced up-regulation of H1R gene expression but also by suppressing basal histamine signaling through their inverse agonistic activity. Histamine 192-201 histamine receptor H1 Homo sapiens 142-145 22286689-1 2012 BACKGROUND: Urticaria is mainly caused by mast cell-derived histamine through the histamine H(1) receptor. Histamine 60-69 histamine receptor H1 Homo sapiens 82-105 21956435-8 2012 IF double-labelling experiments showed a strong correlation of increased histamine expression with expression of H1R and H2R on intestinal enterocytes (histamine/H1R, rho = 0.841, p < 0.0001 and histamine/H2R, rho = 0.806, p < 0.0001). Histamine 73-82 histamine receptor H1 Homo sapiens 113-116 21956435-8 2012 IF double-labelling experiments showed a strong correlation of increased histamine expression with expression of H1R and H2R on intestinal enterocytes (histamine/H1R, rho = 0.841, p < 0.0001 and histamine/H2R, rho = 0.806, p < 0.0001). Histamine 73-82 histamine receptor H1 Homo sapiens 162-165 21956435-8 2012 IF double-labelling experiments showed a strong correlation of increased histamine expression with expression of H1R and H2R on intestinal enterocytes (histamine/H1R, rho = 0.841, p < 0.0001 and histamine/H2R, rho = 0.806, p < 0.0001). Histamine 152-161 histamine receptor H1 Homo sapiens 113-116 21255012-2 2011 We have shown that histamine, acting via H1 receptors (H1R), synergizes lipopolysaccharide (LPS)-induced production of prostaglandin I(2) (PGI(2)), PGE(2) and interleukin-6 (IL-6) by endothelial cells. Histamine 19-28 histamine receptor H1 Homo sapiens 41-53 21930594-6 2011 Collectively, these results demonstrate that Ahr negatively regulates IL-6 production via H1R signaling through the suppression of histamine production in macrophages following LPS stimulation. Histamine 131-140 histamine receptor H1 Homo sapiens 90-93 21730054-0 2011 Involvement of protein kinase Cdelta/extracellular signal-regulated kinase/poly(ADP-ribose) polymerase-1 (PARP-1) signaling pathway in histamine-induced up-regulation of histamine H1 receptor gene expression in HeLa cells. Histamine 135-144 histamine receptor H1 Homo sapiens 170-191 21730054-5 2011 Here we studied the molecular mechanism of H1R up-regulation in HeLa cells that express H1R endogenously in response to histamine and phorbol 12-myristate 13-acetate (PMA). Histamine 120-129 histamine receptor H1 Homo sapiens 43-46 21730054-5 2011 Here we studied the molecular mechanism of H1R up-regulation in HeLa cells that express H1R endogenously in response to histamine and phorbol 12-myristate 13-acetate (PMA). Histamine 120-129 histamine receptor H1 Homo sapiens 88-91 21730054-6 2011 In HeLa cells, histamine stimulation caused up-regulation of H1R gene expression. Histamine 15-24 histamine receptor H1 Homo sapiens 61-64 20607332-1 2011 Histamine is an important biogenic amine, which acts with a group of four G-protein coupled receptors (GPCRs), namely H(1) to H(4) (H(1)R - H(4)R) receptors. Histamine 0-9 histamine receptor H1 Homo sapiens 132-137 21255012-4 2011 In this study, we examined whether LPS stimulates the H1R expression in human coronary artery endothelial cells (HCAEC) with resultant enhancement of histamine responsiveness. Histamine 150-159 histamine receptor H1 Homo sapiens 54-57 21255012-12 2011 Histamine-induced enhancement of the synthesis of PGI(2), PGE(2) and IL-6 by LPS-primed HCAEC was completely blocked by an H1R antagonist. Histamine 0-9 histamine receptor H1 Homo sapiens 123-126 32092833-5 2012 These results suggest that inverse agonists more potently alleviate allergy symptoms by not only inhibiting stimulus-induced up-regulation of H1R gene expression but also by suppressing basal histamine signaling through their inverse agonistic activity. Histamine 192-201 histamine receptor H1 Homo sapiens 142-145 21782040-1 2011 Histamine plays major roles in allergic diseases and its action is mediated mainly by histamine H(1) receptor (H1R). Histamine 0-9 histamine receptor H1 Homo sapiens 111-114 21782040-2 2011 We have demonstrated that histamine signaling-related H1R and histidine decarboxylase (HDC) genes are allergic diseases sensitive genes and their expression level affects severity of the allergic symptoms. Histamine 26-35 histamine receptor H1 Homo sapiens 54-57 21782040-8 2011 In HeLa cells, AL extract suppressed phorbol-12-myristate-13-acetate- or histamine-induced up-regulation of H1R mRNA. Histamine 73-82 histamine receptor H1 Homo sapiens 108-111 21730054-16 2011 These results suggest the involvement of the PKCdelta/ERK/poly(ADP-ribose) polymerase-1 signaling pathway in histamine- or PMA-induced up-regulation of H1R gene expression in HeLa cells. Histamine 109-118 histamine receptor H1 Homo sapiens 152-155 21364192-2 2011 In search of new intracellular mechanisms modulating endothelial effector functions, we identified nicotinic acid adenine dinucleotide phosphate (NAADP) as a crucial second messenger in histamine-induced Ca(2+) release via H1 receptors (H1R). Histamine 186-195 histamine receptor H1 Homo sapiens 223-241 21324712-0 2011 Histamine differentially regulates the production of Th1 and Th2 chemokines by keratinocytes through histamine H1 receptor. Histamine 0-9 histamine receptor H1 Homo sapiens 101-122 21255012-2 2011 We have shown that histamine, acting via H1 receptors (H1R), synergizes lipopolysaccharide (LPS)-induced production of prostaglandin I(2) (PGI(2)), PGE(2) and interleukin-6 (IL-6) by endothelial cells. Histamine 19-28 histamine receptor H1 Homo sapiens 55-58 20112007-1 2010 Histamine plays an important role in allergy mainly through histamine H1 receptor (H1R). Histamine 0-9 histamine receptor H1 Homo sapiens 60-81 21297357-4 2011 H1R mediates allergy histamine signals. Histamine 21-30 histamine receptor H1 Homo sapiens 0-3 20112007-1 2010 Histamine plays an important role in allergy mainly through histamine H1 receptor (H1R). Histamine 0-9 histamine receptor H1 Homo sapiens 83-86 20112007-9 2010 Stimulation with histamine also up-regulated H1R mRNA, and co-stimulation with histamine and IL-4 elevated H1R mRNA level significantly higher than the stimulation with histamine or IL-4 alone did. Histamine 17-26 histamine receptor H1 Homo sapiens 45-48 20112007-9 2010 Stimulation with histamine also up-regulated H1R mRNA, and co-stimulation with histamine and IL-4 elevated H1R mRNA level significantly higher than the stimulation with histamine or IL-4 alone did. Histamine 79-88 histamine receptor H1 Homo sapiens 107-110 20112007-9 2010 Stimulation with histamine also up-regulated H1R mRNA, and co-stimulation with histamine and IL-4 elevated H1R mRNA level significantly higher than the stimulation with histamine or IL-4 alone did. Histamine 79-88 histamine receptor H1 Homo sapiens 107-110 20112007-11 2010 The effects of histamine and IL-4 were additive, suggesting that these allergic mediators will work together to up-regulate H1R level, and thus make the allergic symptom worse by intensifying H1R-mediated allergic processes. Histamine 15-24 histamine receptor H1 Homo sapiens 124-127 20112007-11 2010 The effects of histamine and IL-4 were additive, suggesting that these allergic mediators will work together to up-regulate H1R level, and thus make the allergic symptom worse by intensifying H1R-mediated allergic processes. Histamine 15-24 histamine receptor H1 Homo sapiens 192-195 20040740-6 2010 The synergistic effect of histamine is mediated by histamine receptor-1 (H1R). Histamine 26-35 histamine receptor H1 Homo sapiens 73-76 19568768-2 2009 The expression of genes and proteins involved in the biosynthesis (histidine decarboxylase, HDC), action (histamine receptors: HRH1-HRH4), and metabolism of histamine is largely unknown both in the normal human adrenal cortex and in adrenocortical tumors. Histamine 106-115 histamine receptor H1 Homo sapiens 127-131 19907186-7 2010 CONCLUSION: Histamine appears to induce IL-6 production through H1R in human amnion cells. Histamine 12-21 histamine receptor H1 Homo sapiens 64-67 19907186-6 2010 In addition, the H1R antagonist olopatadine significantly blocked histamine-induced production of IL-6, whereas the H2R antagonist ranitidine did not. Histamine 66-75 histamine receptor H1 Homo sapiens 17-20 19825989-1 2009 Histamine regulates functions via four receptors (HRH1, HRH2, HRH3, and HRH4). Histamine 0-9 histamine receptor H1 Homo sapiens 50-54 18695846-3 2009 During the early response in AR, histamine has been found to be the most abundant mediator and it is associated with many symptoms of this disease mediated through the histamine H1 receptor. Histamine 33-42 histamine receptor H1 Homo sapiens 168-189 19443731-6 2009 The histamine-induced cytosolic free Ca(2+) concentration ([Ca(2+)](i)) increase was inhibited by histamine H1 receptor-specific antagonists, and the expression of the functional histamine H1 receptor was confirmed by reverse transcription-polymerase chain reaction. Histamine 4-13 histamine receptor H1 Homo sapiens 98-119 19443731-6 2009 The histamine-induced cytosolic free Ca(2+) concentration ([Ca(2+)](i)) increase was inhibited by histamine H1 receptor-specific antagonists, and the expression of the functional histamine H1 receptor was confirmed by reverse transcription-polymerase chain reaction. Histamine 4-13 histamine receptor H1 Homo sapiens 179-200 18577700-11 2008 In conclusion, the differences in N terminus and E2-loop between hH(1)R and gpH(1)R exert an influence on affinity and/or potency for histamine and phenoprodifens 5, 6R, and 6S. Histamine 134-143 histamine receptor H1 Homo sapiens 65-71 18548114-0 2008 Histamine upregulates keratinocyte MMP-9 production via the histamine H1 receptor. Histamine 0-9 histamine receptor H1 Homo sapiens 60-81 19047480-5 2009 We identified bulky phenylhistamines with higher potency and affinity at hH(1)R compared with gpH(1)R. Molecular dynamics simulations of ligand-H(1)R interactions revealed four potential binding modes for phenylhistamines possessing an additional histamine moiety; the terminal histamine moiety showed a high flexibility in the binding pocket. Histamine 26-35 histamine receptor H1 Homo sapiens 73-79 19047480-5 2009 We identified bulky phenylhistamines with higher potency and affinity at hH(1)R compared with gpH(1)R. Molecular dynamics simulations of ligand-H(1)R interactions revealed four potential binding modes for phenylhistamines possessing an additional histamine moiety; the terminal histamine moiety showed a high flexibility in the binding pocket. Histamine 26-35 histamine receptor H1 Homo sapiens 74-79 19047480-5 2009 We identified bulky phenylhistamines with higher potency and affinity at hH(1)R compared with gpH(1)R. Molecular dynamics simulations of ligand-H(1)R interactions revealed four potential binding modes for phenylhistamines possessing an additional histamine moiety; the terminal histamine moiety showed a high flexibility in the binding pocket. Histamine 211-220 histamine receptor H1 Homo sapiens 73-79 19047480-5 2009 We identified bulky phenylhistamines with higher potency and affinity at hH(1)R compared with gpH(1)R. Molecular dynamics simulations of ligand-H(1)R interactions revealed four potential binding modes for phenylhistamines possessing an additional histamine moiety; the terminal histamine moiety showed a high flexibility in the binding pocket. Histamine 211-220 histamine receptor H1 Homo sapiens 74-79 18577700-6 2008 In the series hH(1)R > h(gpE2)H(1)R > h(gpNgpE2)H(1)R, we observed a significant decrease in potency of histamine 1 in the GTPase assay. Histamine 110-119 histamine receptor H1 Homo sapiens 14-20 18498711-2 2008 Several stimulants, including histamine, muscarinic agonists and platelet-activating factor, have now been shown to regulate H1R levels and may have roles in regulating the H1R level in physiological and pathological conditions. Histamine 30-39 histamine receptor H1 Homo sapiens 125-128 18577700-6 2008 In the series hH(1)R > h(gpE2)H(1)R > h(gpNgpE2)H(1)R, we observed a significant decrease in potency of histamine 1 in the GTPase assay. Histamine 110-119 histamine receptor H1 Homo sapiens 15-20 18577700-6 2008 In the series hH(1)R > h(gpE2)H(1)R > h(gpNgpE2)H(1)R, we observed a significant decrease in potency of histamine 1 in the GTPase assay. Histamine 110-119 histamine receptor H1 Homo sapiens 33-38 18498711-2 2008 Several stimulants, including histamine, muscarinic agonists and platelet-activating factor, have now been shown to regulate H1R levels and may have roles in regulating the H1R level in physiological and pathological conditions. Histamine 30-39 histamine receptor H1 Homo sapiens 173-176 18296861-5 2008 Histamine added to the in vitro assay of scratch wound healing either increased or inhibited SW756 migration rate by acting either on H1R or H4R, respectively. Histamine 0-9 histamine receptor H1 Homo sapiens 134-137 18339040-1 2008 Histamine is the primary mediator involved the pathophysiology of allergic rhinitis and chronic urticaria, and this explains the prominent role that histamine H(1)-receptor antagonists have in the treatment of these disorders. Histamine 0-9 histamine receptor H1 Homo sapiens 149-172 18377770-3 2008 This new receptor, the histamine H4 receptor (H4R), has a higher affinity for histamine compared with the histamine H1 receptor and appears to be more selectively expressed, found mainly on hematopoietic cells. Histamine 23-32 histamine receptor H1 Homo sapiens 106-127 17478759-0 2007 Histamine upregulates the expression of inducible nitric oxide synthase in human intimal smooth muscle cells via histamine H1 receptor and NF-kappaB signaling pathway. Histamine 0-9 histamine receptor H1 Homo sapiens 113-134 18172439-2 2008 The inflammatory responses resulting from the liberation of histamine have long been thought to be mediated by the histamine H1 receptor, and H1-receptor antagonists--commonly known as antihistamines--have been used to treat allergies for many years. Histamine 60-69 histamine receptor H1 Homo sapiens 115-136 17222324-2 2007 Dysregulated histamine neurotransmission is associated with an altered circadian rhythmicity that is partially restored following central histamine H1 receptor blockade in cirrhotic animals. Histamine 13-22 histamine receptor H1 Homo sapiens 138-159 17336292-3 2007 YM-344484 was found to potently inhibit both the CCL11-induced Ca2+ influx in human CCR3-expressing cells (Kb=1.8 nM) and histamine-induced Ca2+ influx in histamine H1 receptor-expressing PC3 cells (Kb=47 nM). Histamine 122-131 histamine receptor H1 Homo sapiens 155-176 16890992-8 2007 This review summarizes our works on the functions of histamine neurons using human PET studies, including the development of radiolabeled tracers for histamine H1 receptors (H1R: (11)C-doxepin and (11)C-pyrilamine), PET measurements of H1R in depression, schizophrenia, and Alzheimer"s disease (AD), and studies on the sedative effects of antihistamines using H(2)(15)O and H1R occupancy in the human brain. Histamine 53-62 histamine receptor H1 Homo sapiens 236-239 17409634-1 2007 Histamine is a major mediator in allergy acting mainly through the histamine H(1) receptor (H1R). Histamine 0-9 histamine receptor H1 Homo sapiens 67-90 17409634-1 2007 Histamine is a major mediator in allergy acting mainly through the histamine H(1) receptor (H1R). Histamine 0-9 histamine receptor H1 Homo sapiens 92-95 17409634-4 2007 Histamine stimulation significantly increased both H1R promoter activity and mRNA level without alteration in mRNA stability. Histamine 0-9 histamine receptor H1 Homo sapiens 51-54 17409634-5 2007 H1R protein was also up-regulated by histamine. Histamine 37-46 histamine receptor H1 Homo sapiens 0-3 16890992-8 2007 This review summarizes our works on the functions of histamine neurons using human PET studies, including the development of radiolabeled tracers for histamine H1 receptors (H1R: (11)C-doxepin and (11)C-pyrilamine), PET measurements of H1R in depression, schizophrenia, and Alzheimer"s disease (AD), and studies on the sedative effects of antihistamines using H(2)(15)O and H1R occupancy in the human brain. Histamine 53-62 histamine receptor H1 Homo sapiens 236-239 15564772-0 2004 Desloratadine inhibits constitutive and histamine-stimulated nuclear factor-kappaB activity consistent with inverse agonism at the histamine H1 Receptor. Histamine 40-49 histamine receptor H1 Homo sapiens 131-152 16329713-4 2005 Quantitatively, histamine is the most abundant mediator present during an allergic episode - thus, antihistamines (historically called histamine H(1) receptor antagonists, now called H(1) receptor inverse agonists) are a first-line defense against allergic rhinitis and chronic idiopathic urticaria. Histamine 16-25 histamine receptor H1 Homo sapiens 135-158 16884695-3 2006 The main signalling pathway, involved in the stimulation of NGF production by histamine, includes activation of histamine H(1)-receptor, stimulation of Ca(2+)-dependent protein kinase C and mitogen-activated protein kinase. Histamine 78-87 histamine receptor H1 Homo sapiens 112-135 16884695-6 2006 Thus, activation of histamine H(1)-receptor-protein kinase C-mitogen-activated protein kinase signalling pathway plays a crucial role not only in the direct stimulation of NGF secretion by histamine, but also in the indirect stimulation via different types of interactions between histamine, interleukin-1beta, and interleukin-6, which may have important therapeutic implications in modulation of NGF production. Histamine 189-198 histamine receptor H1 Homo sapiens 20-43 16250893-10 2006 The effect of histamine is mediated by the H1R (histamine 1 receptor) and involves activation of the calcineurin/NFAT pathway. Histamine 14-23 histamine receptor H1 Homo sapiens 43-68 15843518-2 2005 Recent reports showed effects of histamine on human monocyte-derived dendritic cells (MoDC) mediated primarily via histamine H1 receptors (H1R) and H2R. Histamine 33-42 histamine receptor H1 Homo sapiens 111-142 15652235-0 2005 Histamine H1 receptor antagonist blocks histamine-induced proinflammatory cytokine production through inhibition of Ca2+-dependent protein kinase C, Raf/MEK/ERK and IKK/I kappa B/NF-kappa B signal cascades. Histamine 40-49 histamine receptor H1 Homo sapiens 0-21 15107581-7 2004 However, down-regulation of the mutant H1R was completely impaired, whereas that of wild-type H1R occurred by approximately 60% by the treatment with 100 microM histamine for 24 h. These results suggest that these residues are responsible for receptor down-regulation but not for receptor internalization. Histamine 161-170 histamine receptor H1 Homo sapiens 39-42 15599091-2 2004 Increase in histamine-induced homologous phosphorylation of H1R was induced in a dose- and time-dependent manner. Histamine 12-21 histamine receptor H1 Homo sapiens 60-63 15599091-5 2004 Histamine-induced phosphorylation of H1R was partially inhibited by three protein kinase inhibitors including Ro-31-8220 for protein kinase C (PKC), KN-93 for calcium/calmodulin-dependent kinase II (CaMKII), and KT5823 for protein kinase G (PKG), while, M3-receptor-mediated phosphorylation of H1R was completely inhibited by Ro 31-8220. Histamine 0-9 histamine receptor H1 Homo sapiens 37-40 15599091-5 2004 Histamine-induced phosphorylation of H1R was partially inhibited by three protein kinase inhibitors including Ro-31-8220 for protein kinase C (PKC), KN-93 for calcium/calmodulin-dependent kinase II (CaMKII), and KT5823 for protein kinase G (PKG), while, M3-receptor-mediated phosphorylation of H1R was completely inhibited by Ro 31-8220. Histamine 0-9 histamine receptor H1 Homo sapiens 294-297 15599091-7 2004 Increased phosphorylation of H1R, by 5-fold over the basal level, induced with a combination of PMA, 8-Br-cGMP, and 8-Br-cAMP was still lower than that with histamine. Histamine 157-166 histamine receptor H1 Homo sapiens 29-32 15107581-7 2004 However, down-regulation of the mutant H1R was completely impaired, whereas that of wild-type H1R occurred by approximately 60% by the treatment with 100 microM histamine for 24 h. These results suggest that these residues are responsible for receptor down-regulation but not for receptor internalization. Histamine 161-170 histamine receptor H1 Homo sapiens 94-97 24764588-3 2004 Olopatadine hydrochloride ophthalmic solution 0.1% is a topical antiallergic agent that is both an antihistamine with high affinity and selectivity for the histamine H1 receptor and a mast cell stabilizer that inhibits the release of histamine and other proinflammatory mediators from human conjunctival mast cells. Histamine 103-112 histamine receptor H1 Homo sapiens 156-177 11916128-5 2002 The enhancing effects of histamine were completely inhibited by a potent H1 receptor (H1R) antagonist, emedastine difumarate. Histamine 25-34 histamine receptor H1 Homo sapiens 73-90 14975703-4 2004 Histamine, which alone showed no effect, enhanced the sphingosine 1-phosphate-induced expressions via histamine H(1) receptor. Histamine 0-9 histamine receptor H1 Homo sapiens 102-125 14520517-0 2003 Analysis of histamine and modeling of ligand-receptor interactions in the histamine H(1) receptor for Magic Angle Spinning NMR studies. Histamine 12-21 histamine receptor H1 Homo sapiens 74-97 12662472-1 2003 Histamine and antihistamines are so deeply woven into the fabric of allergic diseases that it is sometimes difficult to see how this field could advance beyond our current, potent histamine H1-receptor drugs. Histamine 0-9 histamine receptor H1 Homo sapiens 180-201 14978232-8 2004 Investigation of the residues involved in histamine and lisuride binding, using H1R mutants and molecular modeling, have revealed that although these ligands are structurally different, the lisuride-binding pocket in the H1R closely corresponds to the histamine-binding pocket. Histamine 42-51 histamine receptor H1 Homo sapiens 80-83 14978232-8 2004 Investigation of the residues involved in histamine and lisuride binding, using H1R mutants and molecular modeling, have revealed that although these ligands are structurally different, the lisuride-binding pocket in the H1R closely corresponds to the histamine-binding pocket. Histamine 42-51 histamine receptor H1 Homo sapiens 221-224 14978232-8 2004 Investigation of the residues involved in histamine and lisuride binding, using H1R mutants and molecular modeling, have revealed that although these ligands are structurally different, the lisuride-binding pocket in the H1R closely corresponds to the histamine-binding pocket. Histamine 252-261 histamine receptor H1 Homo sapiens 221-224 8732234-1 1996 BACKGROUND: Histamine plays an important role in producing nasal symptoms via histamine H1 receptor (H1R) in allergic rhinitis. Histamine 12-21 histamine receptor H1 Homo sapiens 78-99 11282781-2 2001 We have investigated the effect of IL-1beta on histamine H(1)-receptor (H(1)R)-mediated inositol phosphate (IP) accumulation in human airway smooth muscle cells (HASMC) and on histamine-induced contraction of human bronchial rings. Histamine 47-56 histamine receptor H1 Homo sapiens 72-77 10899954-4 2000 Similar processes of desensitization/resensitization occurred even under hypertonic conditions, where histamine-mediated internalization of the histamine H(1) receptor is inhibited. Histamine 102-111 histamine receptor H1 Homo sapiens 144-167 10051702-5 1999 OBJECTIVE: We examined the effects of DEP extract on the expression of histamine H1 receptor (H1R) mRNA in human nasal epithelial cells (HNECs) and human mucosal microvascular endothelial cells (HMMECs), and on the production of IL-8 and GM-CSF induced by histamine. Histamine 71-80 histamine receptor H1 Homo sapiens 94-97 9007531-6 1996 The effects of histamine on [3H]GABA release, [3H]inositol phosphate accumulation and Ca2+ mobilisation were blocked by the selective histamine H1 receptor antagonist mepyramine. Histamine 15-24 histamine receptor H1 Homo sapiens 134-155 8806799-5 1996 The histamine-enhanced expression of E-selectin and ICAM-1 was inhibited by the histamine H1 receptor antagonists, mepyramine and diphenhydramine. Histamine 4-13 histamine receptor H1 Homo sapiens 80-101 11498525-6 2001 Responses to histamine were inhibited by the histamine H(1) receptor antagonist mepyramine (K(D) 3.5 nM) and following pre-treatment with pertussis toxin (PTX; 57% inhibition). Histamine 13-22 histamine receptor H1 Homo sapiens 45-68 11023712-2 2000 We found that platelet aggregation mediated by subthreshold concentrations of histamine (1-4 microm) plus adrenaline (0.5-2 microm) is inhibited by both an alpha(2)-adrenoceptor blocker (yohimbine) and a histamine (H1) receptor antagonist (diphenhydramine). Histamine 78-87 histamine receptor H1 Homo sapiens 204-227 9531164-9 1998 CONCLUSION: The increase of the expressions of H1R mRNA may explain, in part, the nasal hyperreactivity to histamine observed in patients with nasal allergy. Histamine 107-116 histamine receptor H1 Homo sapiens 47-50 8778348-1 1996 The binding cavity of histamine and histamine antagonists is explored using site directed mutagenesis of the human histamine H1 receptor and the amino acids involved in ligand binding are identified. Histamine 22-31 histamine receptor H1 Homo sapiens 115-136 8778348-1 1996 The binding cavity of histamine and histamine antagonists is explored using site directed mutagenesis of the human histamine H1 receptor and the amino acids involved in ligand binding are identified. Histamine 36-45 histamine receptor H1 Homo sapiens 115-136 8732234-1 1996 BACKGROUND: Histamine plays an important role in producing nasal symptoms via histamine H1 receptor (H1R) in allergic rhinitis. Histamine 12-21 histamine receptor H1 Homo sapiens 101-104 8523041-1 1995 A modelling study has been carried out, investigating the binding of histamine (Hist), 2-methylhistamine (2-MeHist) and 2-phenylhistamine (2-PhHist) at two postulated agonistic binding sites on transmembrane domain 5 (TM5) of the histamine H1-receptor. Histamine 69-78 histamine receptor H1 Homo sapiens 230-251 7556402-5 1995 Responses to histamine were significantly reduced by the histamine H1 receptor antagonist mepyramine (1-10 microM) but not altered by the histamine H2 receptor antagonist cimetidine (100 microM) or by the histamine H3 receptor antagonist thioperamide (1 microM). Histamine 13-22 histamine receptor H1 Homo sapiens 57-78 7614779-1 1995 Histamine H1-receptor antagonists are reversible, competitive inhibitors of the actions of histamine, a critical mediator in the pathophysiology of the allergic response. Histamine 91-100 histamine receptor H1 Homo sapiens 0-21 7717464-2 1995 As the effect of histamine at a given site will be mediated by its specific receptors, we investigated by in situ hybridization and Northern blot analysis the expression and localization of human histamine H1 receptor mRNA in the arterial wall and in cultured human aortic intimal smooth muscle cells (SMC) and immortalized SMC (ISS10) and endothelial cells (SE1). Histamine 17-26 histamine receptor H1 Homo sapiens 196-217 8397092-3 1993 The response to histamine was inhibited by mepyramine (KA 4.3 x 10(9) M-1), indicating the involvement of the histamine H1 receptor in this response. Histamine 16-25 histamine receptor H1 Homo sapiens 110-131 8093027-1 1994 Based on structural comparison with other biogenic amine receptors and the histamine H2 receptor, it has been suggested that in the human histamine H1 receptor, Asp107, Thr194, and Asn198 are the residues involved in binding of histamine. Histamine 75-84 histamine receptor H1 Homo sapiens 138-159 8358540-21 1993 We show here that the acute histamine pretreatment of HeLa cells results in the desensitization of histamine H1 receptor-mediated IPn production. Histamine 28-37 histamine receptor H1 Homo sapiens 99-120 1607549-7 1992 These results extend and support our previous finding that histamine directly causes vascular permeability through H1R and stimulates nasal glandular secretion indirectly through reflexes. Histamine 59-68 histamine receptor H1 Homo sapiens 115-118 1426009-7 1992 The changes evoked by histamine were dose-dependent, related to the duration of incubation of the cells with histamine, and blocked by mepyramine, a histamine H1 receptor antagonist. Histamine 22-31 histamine receptor H1 Homo sapiens 149-170 1426009-8 1992 The results suggest that the endothelial cells respond to histamine through the histamine H1 receptor. Histamine 58-67 histamine receptor H1 Homo sapiens 80-101 1358393-8 1992 The contractile response to histamine was antagonized by the histamine H1-receptor antagonist, clemizole (0.1 microM) but was potentiated by the histamine H2-receptor antagonist, ranitidine (10 microM). Histamine 28-37 histamine receptor H1 Homo sapiens 61-82 34893496-0 2022 High Expression of Histamine Receptor, HRH1, Reduces Immunotherapy Response. Histamine 19-28 histamine receptor H1 Homo sapiens 39-43 1685127-4 1991 These results indicate that trifluoperazine specifically inhibits histamine-induced phosphoinositide hydrolysis as a histamine H1-receptor antagonist in human astrocytoma cells. Histamine 66-75 histamine receptor H1 Homo sapiens 117-138 34822775-0 2022 The allergy mediator histamine confers resistanceto immunotherapy in cancer patients via activationof the macrophage histamine receptor H1. Histamine 21-30 histamine receptor H1 Homo sapiens 117-138 1684671-7 1991 The effects of histidine, as well as histamine, were blocked by mepyramine, a histamine H1-receptor antagonist, and by ranitidine, an H2-antagonist. Histamine 37-46 histamine receptor H1 Homo sapiens 78-99 1711684-1 1990 Histamine release from isolated human basophils test was used to evaluate an activity of: histamine receptors H1 and H2 blockers, agonists of beta-receptors, calcium channel blocking agents, hydrocortisone, and disodium cromoglycate (Intal). Histamine 0-9 histamine receptor H1 Homo sapiens 90-119 34595742-1 2021 Histamine-activated histamine H1 receptor (H1R) signaling regulates many gene expressions, mainly through the protein kinase C (PKC)/extracellular signal-regulated kinases (ERK) signaling. Histamine 0-9 histamine receptor H1 Homo sapiens 20-41 34622396-1 2021 H1 receptor antagonists, known as H1-antihistamines (AHs), inactivate the histamine H1-receptor thereby preventing histamine causing the primary symptoms of allergic diseases, such as atopic dermatitis, pollinosis, food allergies, and urticaria. Histamine 115-124 histamine receptor H1 Homo sapiens 74-95 34595742-1 2021 Histamine-activated histamine H1 receptor (H1R) signaling regulates many gene expressions, mainly through the protein kinase C (PKC)/extracellular signal-regulated kinases (ERK) signaling. Histamine 0-9 histamine receptor H1 Homo sapiens 43-46 34595742-4 2021 H1R gene itself is also up-regulated by the activation of H1R signaling with histamine. Histamine 77-86 histamine receptor H1 Homo sapiens 0-3 34595742-4 2021 H1R gene itself is also up-regulated by the activation of H1R signaling with histamine. Histamine 77-86 histamine receptor H1 Homo sapiens 58-61 34595742-6 2021 Stimulation with histamine up-regulates H1R gene expression through the activation of H1R in HeLa cells. Histamine 17-26 histamine receptor H1 Homo sapiens 40-43 34595742-6 2021 Stimulation with histamine up-regulates H1R gene expression through the activation of H1R in HeLa cells. Histamine 17-26 histamine receptor H1 Homo sapiens 86-89 34595742-10 2021 H1R-activated H1R gene up-regulation in response to histamine was also observed in U373 astroglioma cells. Histamine 52-61 histamine receptor H1 Homo sapiens 0-3 34595742-10 2021 H1R-activated H1R gene up-regulation in response to histamine was also observed in U373 astroglioma cells. Histamine 52-61 histamine receptor H1 Homo sapiens 14-17 34595742-12 2021 In addition, the promoter region responsible for histamine-induced H1R gene transcription in U373 cells was different from that of HeLa cells. Histamine 49-58 histamine receptor H1 Homo sapiens 67-70 34698097-0 2021 Signaling Pathway of Histamine H1 Receptor-Mediated Histamine H1 Receptor Gene Upregulation Induced by Histamine in U-373 MG Cells. Histamine 103-112 histamine receptor H1 Homo sapiens 21-42 34698097-0 2021 Signaling Pathway of Histamine H1 Receptor-Mediated Histamine H1 Receptor Gene Upregulation Induced by Histamine in U-373 MG Cells. Histamine 103-112 histamine receptor H1 Homo sapiens 52-73 34698097-1 2021 Histamine H1 receptor (H1R) is one of the targets of histamine in the nervous system and the peripheral tissues. Histamine 53-62 histamine receptor H1 Homo sapiens 0-21 34698097-1 2021 Histamine H1 receptor (H1R) is one of the targets of histamine in the nervous system and the peripheral tissues. Histamine 53-62 histamine receptor H1 Homo sapiens 23-26 34698097-2 2021 Protein kinase Cdelta (PKCdelta) signaling is involved in histamine-induced upregulation of H1R gene expression in HeLa cells. Histamine 58-67 histamine receptor H1 Homo sapiens 92-95 34698097-3 2021 Histamine also upregulates H1R gene expression in U-373 MG cells. Histamine 0-9 histamine receptor H1 Homo sapiens 27-30 34698097-5 2021 Here, we investigated the molecular mechanism of histamine-induced H1R gene upregulation in U-373 MG cells. Histamine 49-58 histamine receptor H1 Homo sapiens 67-70 34698097-6 2021 Histamine-induced H1R gene upregulation was inhibited by H1R antagonist d-chlorpheniramine, but not by ranitidine, ciproxifan, or JNJ77777120, and H2R, H3R, or H4R antagonists, respectively. Histamine 0-9 histamine receptor H1 Homo sapiens 18-21 34698097-6 2021 Histamine-induced H1R gene upregulation was inhibited by H1R antagonist d-chlorpheniramine, but not by ranitidine, ciproxifan, or JNJ77777120, and H2R, H3R, or H4R antagonists, respectively. Histamine 0-9 histamine receptor H1 Homo sapiens 57-60 35378699-0 2022 Histamine and histamine receptor H1 (HRH1) axis: new target for enhancing immunotherapy response. Histamine 0-9 histamine receptor H1 Homo sapiens 37-41 2625517-5 1989 The response to histamine was inhibited at all ages in both rabbit and human bowel by specific histamine H1 receptor blockade with diphenhydramine, and not by H2 or cholinergic receptor blockers. Histamine 16-25 histamine receptor H1 Homo sapiens 95-116 35328605-1 2022 The histamine H1 receptor (H1R) is a G protein-coupled receptor (GPCR) and plays a key role in allergic reactions upon activation by histamine which is locally released from mast cells and basophils. Histamine 133-142 histamine receptor H1 Homo sapiens 4-25 35328605-1 2022 The histamine H1 receptor (H1R) is a G protein-coupled receptor (GPCR) and plays a key role in allergic reactions upon activation by histamine which is locally released from mast cells and basophils. Histamine 133-142 histamine receptor H1 Homo sapiens 27-30 35328605-5 2022 To evaluate this so-called biased agonism for H1R, bioluminescence resonance energy transfer (BRET)-based biosensors were applied to measure H1R signaling through heterotrimeric Gq proteins, second messengers (inositol 1,4,5-triphosphate and Ca2+), and receptor-protein interactions (GRKs and beta-arrestins) in response to histamine, 2-phenylhistamines, and histaprodifens in a similar cellular background. Histamine 324-333 histamine receptor H1 Homo sapiens 141-144 3461852-1 1986 Serotonin and histamine H1, H2 receptor agonists or antagonists inhibited [3H]histamine uptake by HL-60 cells, according to the following order of potency: impromidine greater than 4-MH greater than histamine greater than AET greater than PEA and: cimetidine, histamine greater than diphenhydramine, serotonin. Histamine 78-87 histamine receptor H1 Homo sapiens 14-39 3461852-1 1986 Serotonin and histamine H1, H2 receptor agonists or antagonists inhibited [3H]histamine uptake by HL-60 cells, according to the following order of potency: impromidine greater than 4-MH greater than histamine greater than AET greater than PEA and: cimetidine, histamine greater than diphenhydramine, serotonin. Histamine 78-87 histamine receptor H1 Homo sapiens 14-39 2872089-6 1986 Histamine H1 receptor antagonist (10(-6)M) inhibited histamine-induced beta-END-LI release from the cells. Histamine 53-62 histamine receptor H1 Homo sapiens 0-21