Histamine Receptor
Histamine receptors are G protein-coupled receptors through which histamine regulates proliferation, apoptosis, differentiation, immune signaling, and tissue-specific cellular responses[1]. Mechanistically, H1R and H2R stimulate cholangiocyte proliferation through Ca2+- and cAMP-dependent pathways, whereas H3R and H4R inhibit biliary growth during cholangiocyte hyperplasia or cholangiocarcinoma models[1]. In inflammation-associated colorectal cancer, H1R shows protumorigenic activity, while H2R shows antitumorigenic activity by suppressing MAPK phosphorylation and chemokine gene expression[2]. Compared with related isoforms, H4R is preferentially expressed in bone marrow progenitor populations and mediates growth factor-induced cell-cycle arrest through a cAMP/PKA-dependent pathway rather than apoptosis[3]. For experimental applications, H1R antagonism and H2R activation can be combined to suppress lipopolysaccharide-induced MAPK signaling, while H3R or H4R agonists provide tools to reduce biliary proliferation or cholangiocarcinoma growth[1][2].
References:
- [1]. Francis H, et al. Histamine regulation of biliary proliferation. J Hepatol. 2012 May;56(5):1204-1206. [Content Brief]
- [2]. Shi Z, et al. Distinct roles of histamine H1- and H2-receptor signaling pathways in inflammation-associated colonic tumorigenesis. Am J Physiol Gastrointest Liver Physiol. 2019 Jan 1;316(1):G205-G216. [Content Brief]
- [3]. Petit-Bertron AF, et al. H4 histamine receptors mediate cell cycle arrest in growth factor-induced murine and human hematopoietic progenitor cells. PLoS One. 2009 Aug 7;4(8):e6504. [Content Brief]
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Histamine Receptor Antagonists
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Histamine Receptor Related Products (517)
Related Products (517)
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Loratadine (Standard)
0 ImagesSynonyms: Loratidine (Standard); SCH 29851 (Standard)Loratadine (Standard) is the analytical standard of Loratadine. This product is intended for research and analytical applications. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
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Notrilobolide
0 ImagesCat. No.: HY-N12210CAS No.: 2363714-40-1Notrilobolide is a sesquiterpene lactone. Notrilobolide induces a potent histamine release from peritoneal rat mast cells.
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Fexofenadine-d6
0 ImagesSynonyms: MDL-16455-d6; Terfenadine carboxylate-d6Fexofenadine-d6 (MDL-16455-d6) is deuterium labeled Fexofenadine, which is an antihistamine pharmaceutical agent.
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Peptide 401
0 ImagesCat. No.: HY-12537CAS No.: 32908-73-9Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT).
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Tiaramide hydrochloride
0 ImagesSynonyms: RHC 2592-ATiaramide (RHC 2592-A) hydrochloride is an analgesic agent with antiallergic activity, and is also a non-steroidal, anti-inflammatory compound. Tiaramide hydrochloride inhibits histamine release.
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Immethridine dihydrobromide
0 ImagesImmethridine (dihydrobromide) is a potent and highly selective histamine H3 receptor agonist with pKi and pEC50 value of 9.07 and 9.74, respectively. Immethridine can be used for the research of myocardial ischemia, inflammatory, and gastric acid related diseases research.
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H4R antagonist 2
0 ImagesH4R antagonist 2 (page 68), a Furo[3,2-d]pyrimidine derivative, is a potent H4R antagonist. H4R antagonist 2 can be used in research of rheumatoid arthritis.
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Propiomazine
0 ImagesPropiomazine is an orally active antihistamine agent. Propiomazine is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.
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Diphenhydramine hydrochloride (Standard)
0 ImagesDiphenhydramine (hydrochloride) (Standard) is the analytical standard of Diphenhydramine (hydrochloride). This product is intended for research and analytical applications. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB).
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(Rac)-Bepotastine besilate
0 Images(Rac)-Bepotastine (besilate) is the isomer of Bepotastine (besilate) (HY-A0015), and can be used as an experimental control. Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.
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Tesmilifene fumarate
0 ImagesSynonyms: DPPE fumarateTesmilifene fumarate (DPPE fumarate), an H1C receptor antagonist, potentiates a wide range of cytotoxics and even to offer some protection of normal cells.
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Nesosteine
0 ImagesCat. No.: HY-158337CAS No.: 84210-62-8Synonyms: CO-1177Nesosteine (CO-1177) is a bronchitis inhibitor that improves the rheology and production of airway bronchial mucus in rabbits. Nesosteine significantly reduced the viscosity of airway bronchial mucus in animals with sulfuric acid nebulized bronchitis and increased mucus production in healthy animals. Nesosteine is more active than mucus-regulating drugs such as Sobrerol, N-acetylcysteine, bromhexine, ambroxol, S-carboxymethylcysteine, and mercaptoalanine. Nesosteine also reduced the content of total proteins in airway bronchial mucus, such as albumin, α1, α2, β, and γ mucins.
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BMY-25368 hydrochloride
0 ImagesCat. No.: HY-19010ACAS No.: 86134-36-3Synonyms: SKF 94482 hydrochlorideBMY-25368 hydrochloride is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 hydrochloride competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food.
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Bufrolin
0 ImagesCat. No.: HY-106481CAS No.: 54867-56-0Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide.
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Setastine
0 ImagesSynonyms: EGIS-2062 free acid; EGYT-2062 free acidSetastine (EGIS-2062 (free acid); EGYT-2062 (free acid) is an orally effective, non-sedative and long acting anti-allergic agent. Setastine possesses potent histamine Hi-receptor blocking properties and can be used for allergies and rhinitis research[1]<.
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Chlorcyclizine hydrochloride
0 ImagesChlorcyclizine hydrochloride is a histamine H1 antagonist.
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Chlorphenoxamine
0 ImagesChlorphenoxamine, an antihistamine and anticholinergic agent is a GPCR antagonist. Chlorphenoxamine inhibits multiple lethal viral diseases, such as SARS-CoV, MERS-CoV, EBOV and malaria. Chlorphenoxamine shows anti-filovirus activity against both EBOV and Marburg virus (MARV) with IC50s of 1.1 μM and 6.2 μM, respectively. Chlorphenoxamine is used for allergic conditions, urticaria, viral diseases and Parkinson’s disease.
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(S)-Setastine
0 ImagesCat. No.: HY-119832BSynonyms: (S)-EGIS-2062 free acid; (S)-EGYT-2062 free acid(S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent antagonist of H1 receptor-mediated responses. (S)-Setastine has a long-lasting antihistamine effect and good oral efficacy. (S)-Setastine can be used in the research of allergic diseases.
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Cetirizine methyl ester
0 ImagesCat. No.: HY-12966CAS No.: 83881-46-3Cetirizine methyl ester is an impurity of Cetirizine (HY-17042). Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist.
