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]. 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[1]. 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[2][3]. 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][4]. 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[1].
References:
- [1]. Alonso N, et al. Physiological implications of biased signaling at histamine H2 receptors. Front Pharmacol. 2015 Mar 10;6:45. [Content Brief]
- [2]. Li D, et al. Cardiac mast cells regulate myocyte ANP release via histamine H2 receptor in beating rabbit atria. Regul Pept. 2009 Jun 5;155(1-3):33-8. [Content Brief]
- [3]. Saheera S, et al. Histamine 2 receptors in cardiovascular biology: A friend for the heart. Drug Discov Today. 2022 Jan;27(1):234-245. [Content Brief]
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H2 Receptor Related Products (64)
Related Products (64)
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Asenapine citrate
0 ImagesCat. No.: HY-10121BCAS No.: 1411867-74-7Synonyms: Org 5222 citrateAsenapine 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.
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DA 4626
0 ImagesCat. No.: HY-122148CAS No.: 83184-14-9DA 4626 is a competitive H2-histamine receptor antagonist. DA 4626 inhibits adenylate cyclase activity with a KB value of 40 nM.
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H3R antagonist 5
0 ImagesCat. No.: HY-14517CAS No.: 879368-27-1H3R 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.
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Carcinine
0 ImagesCat. No.: HY-107567CAS No.: 56897-53-1Synonyms: β-AlanylhistamineCarcinine (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.
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UR-AK49
0 ImagesCat. No.: HY-167897CAS No.: 902154-32-9UR-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.
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Emedastine difumarate
0 ImagesCat. No.: HY-B2178CAS No.: 87233-62-3Emedastine 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.
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CP-66948
0 ImagesCat. No.: HY-19048CAS No.: 101189-47-3CP-66948 is a histamine H2-receptor antagonist with gastric antisecretory activity and mucosal protective properties.
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Roxatidine acetate
0 ImagesCat. No.: HY-B0305CAS No.: 78628-28-1Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity.
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Lavoltidine
0 ImagesCat. No.: HY-121450CAS No.: 76956-02-0Synonyms: Loxtidine; AH-234844Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
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Platelet aggregation-IN-3
0 ImagesCat. No.: HY-176060CAS No.: 1029802-21-8Platelet aggregation-IN-3 (Compound 5) is a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. Platelet aggregation-IN-3 can inhibit platelet aggregation induced by ADP and collagen and can also modulate tumour cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is promising for research of antiplatelet therapy in cardiovascular diseases and the prevention of cancer-related thrombosis and tumour metastasis.
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AY 29315
0 ImagesCat. No.: HY-167141CAS No.: 114394-28-4AY 29315 is a selective and orally active histamine H2-receptor antagonist. AY 29315 can inhibit astric acid secretion and shows antiulcer activity. AY 29315 can be used for the research of gastric ulcer.
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Famotidine-13C,d3
0 ImagesCat. No.: HY-B0377SCAS No.: 2744683-81-4Synonyms: MK-208-13C,d3Famotidine-13C,d3 (MK-208-13C,d3) is the deuterated, 13C-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.
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NO-794
0 ImagesCat. No.: HY-182643CAS No.: 105150-87-6NO-794 is a histamine H2 receptor antagonist. NO-794 inhibits gastric acid secretion in pylorus-ligated rats. NO-794 can be used for the research of peptic ulcers.
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BMY-25271
0 ImagesCat. No.: HY-100191CAS No.: 78441-82-4BMY-25271 is a histamine H2 receptor antagonist.
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Zolantidine
0 ImagesCat. No.: HY-101373CAS No.: 104076-38-2Synonyms: SK&F 95282Zolantidine (SKF 95282) is a potent, selective and cross the blood-brain barrier histamine H2 antagonist. Zolantidine induces antinociception.
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Arpromidine
0 ImagesCat. No.: HY-164430CAS No.: 106669-71-0Synonyms: BU-E-50Arpromidine (BU-E-50) is the agonist for histamine H2 receptor and the antagonist for histamine H1 receptor. Arpromidine exhibits positive inotropic effect with less risks in causing arrhythmias. Arpromidine can be used in research of congestive heart failure.
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Famotidine hydrochloride
0 ImagesCat. No.: HY-B0377ACAS No.: 125193-62-6Synonyms: MK-208 hydrochlorideFamotidine hydrochloride (MK-208 hydrochloride) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine hydrochloride inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine hydrochloride scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine hydrochloride crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine hydrochloride reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine hydrochloride can be used in studies related to COVID-19, liver injury and acute gastric ulcer.
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Ranitidine-d6 hydrochloride
0 ImagesCat. No.: HY-B0281ASCAS No.: 1185238-09-8Ranitidine-d6 hydrochloride is the deuterium labeled Ranitidine hydrochloride (HY-B0281A). Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride 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 hydrochloride inhibits breast tumor development and spread in mice.
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Famotidine-13C
0 ImagesCat. No.: HY-B0377S1Synonyms: MK-208-13CFamotidine-13C (MK-208-13C) is the 13C-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.
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Osutidine
0 ImagesCat. No.: HY-105101CAS No.: 140695-21-2Osutidine is a selective histamine H2 receptor antagonist, can effectively inhibit histamine-stimulated gastric acid secretion. Osutidine does not affect [14C]aminopyrine accumulation stimulated by carbachol or dibutyryl-cAMP. Osutidine is insurmountable and includes non-competitive inhibition. Osutidine can be used for the study of gastric mucosal injury.
