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The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and, through a separate G protein-dependent mechanism, the phosphoinositide/protein kinase (PKC) signaling pathway.
基因功能參考文獻(xiàn):
Pharmacological or genetic modulations of H2 and H4 HRs (H2R and H4R) not only suppressed gefitinib-induced cytostasis and differentiation of AML cells but also blocked EGFR and ERK1/2 inhibition in MDA-MB-231 cells PMID: 27180173
High constitutive Akt2 activity in U937 promonocytes: effective reduction of Akt2 phosphorylation by the histamine H2-receptor and the beta2-adrenergic receptor PMID: 26475619
Lack of Association between rs2067474 Polymorphism in Histamine Receptor H2 Gene and Breast Cancer in Chinese Han Population PMID: 25922853
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. PMID: 25192644
upregulated on T regs following seasonal pollen exposure; allergen immunotherapy had no impact on the expression PMID: 24980224
The inhibitory effects of histamine on reactive oxygen species production in whole blood phagocytes are caused by H2R rather than H4R histamine receptors. PMID: 24530738
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 PMID: 23465664
rs2607474 GG homozygote confers a significantly increased risk for age- and inflammation-related DAPK and CDH1 methylation in gastric epithelium. PMID: 23280118
HR2 receptor is involved in histamine-induced GDF-15 expression. PMID: 22975449
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. PMID: 22720301
1018 GG homozygosity of HRH2 may be associated with the severity of gastric mucosal atrophy PMID: 22615049
Excitation of dentate nucleus neurons by histamine suggests that initiation and planning of movement is modulated by histaminergic projections. PMID: 21683759
GRK2 induces desensitization of H2R through a phosphorylation-independent and RGS-dependent mechanism PMID: 21705320
Results describe the interactions between human H2 receptor and its agonists. PMID: 21212009
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 PMID: 20012462
histamine up-regulates LOX-1 expression via the H2 receptor in THP-1 monocytes PMID: 11728449
Stimulation of phosphodiesterase IV is mediated by the H2 receptor and related to intracellular levels of cAMP. PMID: 12824943
Data show that the rapid and prolonged modulation of cell surface histamine H2 receptor levels by histamine was regulated solely via internalization. PMID: 14523557
significant differences in H2 receptor expression in different vascular cell types might play a critical role in histamine induced cellular responses PMID: 15167968
human mast cells constitutively express primarily H2 and H4 receptors and that H2 receptors are functionally linked to cellular processes. PMID: 15191551
Involvement of histamine H2 receptors in the histamine induced ets-1 expression in melanoma cells PMID: 15848191
The equilibrium between receptor endocytosis and recycling is altered before H2R upregulation, probably via suppressing H2R degradation. PMID: 15961859
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 PMID: 16203768
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. PMID: 17347323
HRH2 trafficking was analyzed by examination of the roles of arrestin, dynamin, and clathrin on HRH2 internalization. PMID: 18617631
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. PMID: 18691388
role in allergy, autoimmunity, graft rejection, malignancy PMID: 18802338
H2r exposure to an agonist caused desensitization controlled by H2r phosphorylation via GRK2 and GRK3. PMID: 11641433
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. PMID: 11466390