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 Related Products (517)
Related Products (517)
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Fepradinol hydrochloride
0 ImagesCat. No.: HY-118854BCAS No.: 67704-50-1Fepradinol hydrochloride is an orally active nonsteroidal anti-inflammatory agent. Fepradinol hydrochloride inhibits the increase in vascular permeability induced by histamine, 5-hydroxytryptamine, and bradykinin, reduces exudate volume, prevents leukocyte migration, and suppresses acute inflammation models. Fepradinol hydrochloride also induces thrombotic vasculopathy with epidermal necrosis, without leukocytoclastic vasculitis; triggers occlusive contact dermatitis presenting as purpuric papulonecrotic lesions, and causes strongly positive patch test reactions. Fepradinol hydrochloride can be used in research related to occlusive contact dermatitis and acute inflammation.
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Roxatidine Acetate Hydrochloride (Standard)
0 ImagesSynonyms: HOE 760 (Standard)Roxatidine (Acetate Hydrochloride) (Standard) is the analytical standard of Roxatidine (Acetate Hydrochloride). This product is intended for research and analytical applications. Roxatidine Acetate Hydrochloride is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine Acetate Hydrochloride has antisecretory potency against gastric acid secretion. Roxatidine Acetate Hydrochloride can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine Acetate Hydrochloride has antitumor activity.
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Toladryl
0 ImagesCat. No.: HY-138110CAS No.: 19804-27-4Synonyms: 4-MethyldiphenhydramineToladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guinea pigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases.
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TEI-6472
0 ImagesCat. No.: HY-105460CAS No.: 151379-49-6TEI-6472, a naphthalene derivative, can suppress IgE responses both in vitro and in vivo. TEI-6472 causes significant inhibition of FceRI-mediated histamine release.
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Metiamide (Standard)
0 ImagesCat. No.: HY-15540RCAS No.: 34839-70-8Synonyms: SK&F 92058 (Standard)Metiamide (Standard) is the analytical standard of Metiamide. This product is intended for research and analytical applications. Metiamide (SK&F 92058) is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide.
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(R)-(+)-Dimethindene maleate (Standard)
0 ImagesCat. No.: HY-107647ARCAS No.: 136152-64-2(R)-(+)-Dimethindene maleate (Standard) is the analytical standard of (R)-(+)-Dimethindene (maleate) (HY-107647A). This product is intended for research and analytical applications. (R)-(+)-Dimethindene maleate is an orally active H1-receptor blocker with antihistaminic properties in pigs.
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Cetirizine Impurity D (Standard)
0 ImagesCat. No.: HY-100661RCAS No.: 346451-15-8Cetirizine Impurity D (Standard) is the analytical standard of Cetirizine Impurity D. This product is intended for research and analytical applications. Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
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Bilastine (Standard)
0 ImagesCat. No.: HY-14447RCAS No.: 202189-78-4Bilastine (Standard) is the analytical standard of Bilastine. This product is intended for research and analytical applications. Bilastine is a histamine H1 receptor antagonist that can be used to treat allergic rhinoconjunctivitis and urticaria.
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ReN-1869 hydrochloride
0 ImagesCat. No.: HY-101724CAS No.: 170149-76-5Synonyms: NNC-05-1869 hydrochlorideReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with Ki of 0.45 μM.
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(±)-Tazifylline
0 ImagesCat. No.: HY-U00018CAS No.: 79712-55-3(±)-Tazifylline is a potent, selective and long-acting histamine H1 receptor antagonist.
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Bamirastine
0 ImagesCat. No.: HY-101601CAS No.: 215529-47-8Synonyms: TAK-427Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.
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Hydroxyzine pamoate (Standard)
0 ImagesHydroxyzine (pamoate) (Standard) is the analytical standard of Hydroxyzine (pamoate). This product is intended for research and analytical applications. Hydroxyzine pamoate is a histamine receptor H1 antagonist.
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Pitolisant-d10
0 ImagesCat. No.: HY-12199SSynonyms: Tiprolisant-d10Pitolisant-d10 (Tiprolisant-d10) 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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Loratadine-13C6
0 ImagesCat. No.: HY-17043S3Synonyms: SCH 29851-13C6Loratadine-13C6 (SCH 29851-13C6) is 13C labeled Loratadine. 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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Betazole (Standard)
0 ImagesBetazole (Standard) is the analytical standard of Betazole. This product is intended for research and analytical applications. Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active histamine H2 receptor agonist. Betazole induces gastric acid secretion and causes an immediate and significant increase in common bile duct pressure. Betazole is used as a diagnostic agent known as histalog for investigating gastric acid secretory capacity.
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Seliforant (Standard)
0 ImagesCat. No.: HY-109074RCAS No.: 1164115-89-2Synonyms: SENS-111 (Standard)Seliforant (Standard) is the analytical standard of Seliforant (HY-109074). This product is intended for research and analytical applications. Seliforant (SENS-111) is a selective and orally histamine H4 receptor antagonist.
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FR-145715
0 ImagesCat. No.: HY-167653CAS No.: 149917-31-7FR-145715 is a histamine H2 receptor antagonist, with specific anti-Helicobacter pylori activities. FR-145715 can be used for the research of gastric lesions.
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S 38093 (Standard)
0 ImagesCat. No.: HY-104003RCAS No.: 862896-30-8
