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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Gizzerosine
0 ImagesCat. No.: HY-121399CAS No.: 89238-78-8Gizzerosine is an H2 receptor agonist. It can stimulate the gastric acid secretion of broiler chickens, thus causing gizzard erosion in them. Gizzerosine has significant research value in the fields of agricultural farming and feed science.
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Ebrotidine (Standard)
0 ImagesSynonyms: FI3542 (Standard)Ebrotidine (Standard) (FI3542 (Standard)) is the analytical standard of Ebrotidine (HY-15538). This product is intended for research and analytical applications. Ebrotidine (FI3542) is a competitive histamine H2 receptor (histamine H2 receptor) antagonist with gastric acid secretion inhibitory and gastric mucosal protective effects. Ebrotidine alleviates gastric mucosal injury and epithelial cell apoptosis induced by Indomethacin (HY-14397) and Helicobacter pylori LPS (HY-D1056), and accelerates chronic gastric ulcer healing by promoting rapid recovery of IL-4 and inhibiting TNF-α, endothelin-1 (ET-1) and NOS-2. Ebrotidine can be used in studies on gastric ulcer healing, NSAID-induced gastric mucosal injury, Helicobacter pylori-associated gastritis, and H2 receptor-mediated gastric mucosal protection mechanisms.
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Histamine H2 receptor antagonist-1
0 ImagesCat. No.: HY-116596CAS No.: 127966-78-3Antiulcer Agent 3 is a orally active histamine H2-receptor competitive antagonist (pA2 = 6.7). Antiulcer Agent 3 reduces gastric acid secretion. Antiulcer Agent 3 reduces gastric lesions in water-immersion stress-induced ulcer rat models. Antiulcer Agent 3 protects against HCl-ethanol-induced gastric lesions in rats. Antiulcer Agent 3 can be used for the research of peptic ulcer disease.
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Impromidine
0 ImagesCat. No.: HY-116777CAS No.: 55273-05-7Synonyms: SKF 92676Impromidine (SKF 92676) is a potent agonist for histamine H2 receptor. Impromidine induces gastric mucosal blood flow and acid secretion.
