2. Vías de señalización
  3. GPCR/G Protein
    Immunology/Inflammation
    Neuronal Signaling
  4. Histamine Receptor
  5. H2 Receptor Isoform

H2 Receptor

Histamine H2 receptor (H2R, HRH2) is a class A G protein-coupled receptor that mediates key histamine-dependent physiological responses and is best known for regulating gastric acid secretion through Gs-dependent activation of adenylyl cyclase, elevation of intracellular cAMP, and subsequent protein kinase A (PKA) signaling[1][2]. Mechanistically, H2R signaling extends beyond gastric physiology and influences cellular survival, receptor desensitization, internalization, and ERK1/2 pathway activation, highlighting its broader role in signal transduction and tissue homeostasis[2][3]. In cardiovascular systems, H2R participates in histamine-mediated regulation of atrial natriuretic peptide (ANP) release and cardiac function, and altered H2R signaling has been investigated in heart failure and related experimental models[4][5]. Compared with related histamine receptor isoforms, H2R is distinguished by its predominant coupling to Gs/cAMP signaling, whereas H1 receptors primarily activate phospholipase C pathways, H3 receptors function mainly as inhibitory presynaptic receptors, and H4 receptors are associated with immune cell regulation[1][6]. For experimental applications, selective agonists and antagonists have been widely used to dissect H2R-dependent signaling networks; notably, ligands such as famotidine can exhibit pathway-selective or biased signaling properties, differentially affecting cAMP and ERK signaling outputs and thereby providing useful pharmacological tools for mechanistic studies[3].

Productos relacionados con H2 Receptor (54):

Cat. No. Nombre del producto Efecto Pureza
  • HY-101373A
    Zolantidine dimaleate
    		Antagonist 99.19%
    Zolantidine dimaleate (SKF 95282 dimaleate) is a potent, selective and cross the blood-brain barrier histamine H2 antagonist. Zolantidine dimaleate induces antinociception.
  • HY-101167
    Aminopotentidine
    		Antagonist 98.54%
    Aminopotentidine is a histamine H2 receptor antagonist with KB values of 220 nM and 280 nM for human and guinea pig H2 receptors, respectively. It can also serve as a precursor for the synthesis of [125I] iodo derivatives.
  • HY-137941
    Roxatidine
    		Antagonist 98.25%
    Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is an orally active histamine H2-receptor antagonist. Roxatidine, an anti-ulcer agent, suppresses histamine release (thus inhibiting proton secretion) and inhibits the production of VEGF-1, an important marker of inflammation and angiogenesis. Anti-allergic inflammatory effect. Roxatidine is promising for research of gastric and duodenal ulcers.
  • HY-B1557A
    Betazole dihydrochloride
    		Agonist
    Betazole (Ametazole) dihydrochloride, a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole dihydrochloride induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole dihydrochloride has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity.
  • HY-15541
    Zaltidine
    		Antagonist 99.49%
    Zaltidine dihydrochloride (CP-5736 dihydrochloride) is a highly specific H2 receptor antagonist with antisecretion activity. Zaltidine dihydrochloride reduces the stimulant effect of histamine on gastric acid secretion by binding to histamine H2 receptors on gastric parietal cells, thus reducing gastric acid production. Zaltidine dihydrochloride can be used in the study of gastric acid-related diseases such as duodenal ulcers.
  • HY-14289A
    Cimetidine hydrochloride
    		Antagonist
    Cimetidine (SKF-92334) hydrochloride is an orally active, inverse and BBB-permeable histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity.
  • HY-14289S
    Cimetidine-d3
    		Modulator
    Cimetidine-d3 is the deuterium labeled Cimetidine. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity.
  • HY-B0310S
    Nizatidine-d3
    		Antagonist 98.80%
    Nizatidine-d3 is the deuterium labeled Nizatidine. Nizatidine is a potent and orally active histamine H2 receptor antagonist, can be used for the research of stomach?and?intestines ulcers. Nizatidine works by decreasing the secretion of gastric?acid the stomach makes and prevent ulcers from coming back after they have healed in animal models.
  • HY-107563A
    ROS 234 dioxalate
    		Antagonist
    ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access.
  • HY-107567B
    Carcinine dihydrochloride
    		Antagonist 99.39%
    Carcinine (β-Alanylhistamine) dihydrochloride is the dihydrochloride salt of Carcinine (HY-107567). Carcinine is a selective and orally active histamine H3 receptor antagonist with a Ki of 0.2939 μM. Carcinine can reduce histamine content. Carcinine exhibits anti-oxidant activity and neuroprotective effects. Carcinine shows positive inotropic effect and can reduce blood sugar and blood lipid levels. Carcinine can be used for the researches of inflammation, neurological, cardiovascular and metabolic disease, such as retinal damage, seizure and diabetes.
  • HY-101234
    ICI 162846
    		Antagonist
    ICI 162846 is an orally active antagonist of H2 receptor. ICI 162846 inhibits acid production accompanied by an increase in the secretion of histamine in chronic duodenal ulcer (CDU) models. ICI 162846 is effective in preventing CDU.
  • HY-B0693A
    Ranitidine bismuth citrate
    		Antagonist
    Ranitidine bismuth citrate is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine bismuth citrate antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine bismuth citrate has selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate also has anti-Helicobacter pylori infection. Ranitidine bismuth citrate inhibits breast tumor development and spread in mice.
  • HY-105535
    Etintidine hydrochloride
    		Antagonist
    Etintidine (BL-5641) hydrochloride is a potent orally active histamine H2-receptor antagonist. Etintidine hydrochloride can be used for gastrointestinal ulcer diseases research.
  • HY-106078
    Oxmetidine
    		Antagonist
    Oxmetidine (SKF 92994) is an orally active H2-receptor antagonist, and is an anti-ulcer agent.
  • HY-10121B
    Asenapine citrate
    		Antagonist
    Asenapine citrate, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine citrate can be used in the research of schizophrenia and bipolar disorder.
  • HY-122148
    DA 4626
    		Antagonist
    DA 4626 is a competitive H2-histamine receptor antagonist. DA 4626 inhibits adenylate cyclase activity with a KB value of 40 nM.
  • HY-14517
    H3R antagonist 5
    		Agonist
    H3R antagonist 5 (Compound 1b) is a selective histamine H3 receptor inverse agonist with a IC50 of 0.54 nM and the ability to cross the blood-brain barrier. H3R antagonist 5 can be used in central nervous system-related research.
  • HY-107567
    Carcinine
    		Antagonist
    Carcinine (β-Alanylhistamine) is a selective and orally active histamine H3 receptor antagonist with a Ki of 0.2939 μM. Carcinine can reduce histamine content. Carcinine exhibits anti-oxidant activity and neuroprotective effects. Carcinine shows positive inotropic effect and can reduce blood sugar and blood lipid levels. Carcinine can be used for the researches of inflammation, neurological, cardiovascular and metabolic disease, such as retinal damage, seizure and diabetes.
  • HY-167897
    UR-AK49
    		Agonist
    UR-AK49 (compound 11) is a human histamine H1 and H2 receptor agonist. UR-AK49 has an EC50 of 23 nM in a GTPase assay with hH2R-Gsalpha fusion protein expressed in Sf9 insect cells. UR-AK49 can be used in neuro-related research.
  • HY-B2178
    Emedastine difumarate
    		Agonist
    Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.