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 Inhibitors
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Histamine Receptor Antagonists
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Histamine Receptor Related Products (517)
Related Products (517)
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BMY-25368
0 ImagesCat. No.: HY-19010CAS No.: 86134-80-7Synonyms: SKF 94482BMY-25368 (SKF 94482) is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 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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Roxatidine (Standard)
0 ImagesCat. No.: HY-137941RCAS No.: 78273-80-0Roxatidine (Standard) is the analytical standard of Roxatidine. This product is intended for research and analytical applications. Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is a 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.
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Carbinoxamine maleate salt (Standard)
0 ImagesCarbinoxamine maleate salt (Standard) is the analytical standard of Carbinoxamine maleate salt (HY-B1589A). This product is intended for research and analytical applications. Carbinoxamine maleate salt is a blood-brain barrier-permeable histamine H1 receptor antagonist. Carbinoxamine maleate salt blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. Carbinoxamine maleate salt inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. Carbinoxamine maleate salt can be used in research on allergic rhinitis, influenza, etc.
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Cinitapride-d5
0 ImagesCat. No.: HY-B2089SCAS No.: 2714421-62-0Cinitapride-d5 is the deuterium labeled Cinitapride.
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Clemizole penicillin
0 ImagesCat. No.: HY-W754356CAS No.: 6011-39-8Clemizole penicillin is a composite preparation containing two active components, Clemizole (HY-30234) and penicillin, with antihistamine, anti-inflammatory, and bactericidal activities. The Clemizole component of Clemizole penicillin targets the H1 receptor, CrtN, and TRPC5 calcium channel, while penicillin exerts antibacterial effects. The clemizole contained in Clemizole penicillin acts as a reversible competitive inhibitor of the TRPC5 calcium channel; it also competitively targets the CrtN enzyme of Staphylococcus aureus to block staphyloxanthin biosynthesis. Clemizole penicillin can be used in research on lobar pneumonia and syphilis.
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Lodoxamide (Standard)
0 ImagesCat. No.: HY-14270RCAS No.: 53882-12-5Synonyms: U-42585E free acid (Standard)Lodoxamide (Standard) is the analytical standard of Lodoxamide. This product is intended for research and analytical applications. Lodoxamide (U-42585E free acid) is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.
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Carcinine dihydrochloride (Standard)
0 ImagesSynonyms: β-Alanylhistamine dihydrochloride (Standard)Carcinine dihydrochloride (Standard) is the analytical standard of Carcinine (dihydrochloride) (HY-107567B). This product is intended for research and analytical applications. 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.
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(S)-(+)-Dimethindene maleate (Standard)
0 ImagesCat. No.: HY-107647RCAS No.: 136152-65-3(S)-(+)-Dimethindene maleate (Standard) is the analytical standard of (S)-(+)-Dimethindene (maleate) (HY-107647). This product is intended for research and analytical applications. (S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48).
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Psoralenoside (Standard)
0 ImagesCat. No.: HY-N7503RCAS No.: 905954-17-8Psoralenoside is a benzofuran glycoside from Psoralea corylifolia. Psoralenoside exhibits high binding affinities against histaminergic H1, calmodulin, and voltage-gated L-type calcium channels (E-value≥-6.5 Kcal/mol). Psoralenoside shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.
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Levodropropizine-d5
0 ImagesCat. No.: HY-B1895S1Synonyms: (S)-(-)-Dropropizine-d5; DF-526-d5Levodropropizine-d5 ((S)-(-)-Dropropizine-d5) is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.
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Pitolisant-d6
0 ImagesCat. No.: HY-12199S1CAS No.: 2416991-77-8Synonyms: Tiprolisant-d6Pitolisant-d6 (Tiprolisant-d6) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
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Azelastine hydrochloride (Standard)
0 ImagesCat. No.: HY-B0462RCAS No.: 79307-93-0Azelastine (hydrochloride) (Standard) is the analytical standard of Azelastine (hydrochloride). This product is intended for research and analytical applications. Azelastine hydrochloridem, an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine hydrochloride can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2.
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Thiethylperazine-d3
0 ImagesCat. No.: HY-B1794SThiethylperazine-d3 is the deuterium labeled Thiethylperazinee (HY-B1794). Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects.
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Chlorphenoxamine (Standard)
0 ImagesChlorphenoxamine (Standard) is the analytical standard of Chlorphenoxamine (HY-B1607). This product is intended for research and analytical applications. Chlorphenoxamine, 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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Olopatadine-d3 (hydrochloride)
0 ImagesCat. No.: HY-B0426ASCAS No.: 1331635-21-2Olopatadine-d3 hydrochloride (ALO4943A-d3) is the deuterium labeled Olopatadine hydrochloride. Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4+ and CD8+ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis.
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VUF10460 (Standard)
0 ImagesCat. No.: HY-101420RCAS No.: 1028327-66-3
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GSK189254A hydrochloride
0 ImagesCat. No.: HY-12200CAS No.: 945493-87-8Synonyms: GSK189254GSK189254A hydrochloride is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
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Pitolisant hydrochloride (Standard)
0 ImagesSynonyms: Ciproxidine (Standard); BF 2649 (Standard)Pitolisant (hydrochloride) (Standard) is the analytical standard of Pitolisant (hydrochloride). This product is intended for research and analytical applications. Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
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Bepotastine besilate (Standard)
0 ImagesBepotastine (besilate) (Standard) is the analytical standard of Bepotastine (besilate). This product is intended for research and analytical applications. 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.
