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 Ligand
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Histamine Receptor Related Products (517)
Related Products (517)
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Emedastine difumarate (Standard)
0 ImagesCat. No.: HY-B2178RCAS No.: 87233-62-3Emedastine (difumarate) (Standard) is the analytical standard of Emedastine (difumarate). This product is intended for research and analytical applications. Emedastine 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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Cetirizine dihydrochloride (Standard)
0 ImagesSynonyms: P071 (Standard)Cetirizine (dihydrochloride) (Standard) is the analytical standard of Cetirizine (dihydrochloride). This product is intended for research and analytical applications. Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
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Betahistine dihydrochloride (Standard)
0 ImagesBetahistine (dihydrochloride) (Standard) is the analytical standard of Betahistine (dihydrochloride). This product is intended for research and analytical applications. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA).
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Hydroxyzine (Standard)
0 ImagesHydroxyzine (Standard) is the analytical standard of Hydroxyzine. This product is intended for research and analytical applications. Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder.
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Ebastine (Standard)
0 ImagesSynonyms: LAS-W 090 (Standard); RP64305 (Standard)Ebastine (Standard) is the analytical standard of Ebastine. This product is intended for research and analytical applications. Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research.
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Phenindamine hydrochloride
0 ImagesPhenindamine hydrochloride (Nu 1504 hydrochloride) is the hydrochloride salt of Phenindamine (HY-A0149). Phenindamine is a histamine H1 receptor antagonist. Phenindamine hydrochloride mainly exists in the 9-9a ene configuration and as a mixture of protonated epimers. Phenindamine hydrochloride can be used in studies related to histamine H1 receptor antagonists and the salt-type structure of Phenindamine.
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Decloxizine (Standard)
0 ImagesDecloxizine (UCB-1402; NSC289116) (Standard) is the analytical standard of Decloxizine. This product is intended for research and analytical applications.Decloxizine is an orally active bronchodilator that can penetrate the blood-brain barrier. Decloxizine is a piperazine-type H1 histamine receptor antagonist. Decloxizine selectively blocks H1 histamine receptors, inhibiting histamine-induced capillary dilation, edema, and itching. Decloxizine has some 5-HT2 receptor antagonistic activity. Decloxizine can be used in studies of urticaria, allergic rhinitis, and bronchial asthma.
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(E)-Dothiepin hydrochloride
0 ImagesCat. No.: HY-165378CAS No.: 25627-36-5Synonyms: (E)-Dosulepin hydrochloride; (E)-Dothep hydrochloride(E)-Dothiepin ((E)-Dosulepin;(E)-Dothep) hydrochloride is an antidepressant agent with sedative/anxiolytic activity. (E)-Dothiepin hydrochloride is an inhibitor preferring of noradrenaline uptake than serotonin uptake. (E)-Dothiepin hydrochloride facilitates noradrenergic neurotransmission via inhibiting the neuronal uptake. (E)-Dothiepin hydrochloride is also an antagonist of histamine H1-receptor without cardiotoxicity. (E)-Dothiepin hydrochloride exhibits significant analgesic activity in psychogenic facial pain，idiopathic fibromyalgia syndrome or rheumatoid arthritis.
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Mizolastine (Standard)
0 ImagesMizolastine (Standard) is the analytical standard of Mizolastine. This product is intended for research and analytical applications. Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial.
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AHR-14310C
0 ImagesCat. No.: HY-118910CAS No.: 119810-68-3AHR-14310C is a potent, long-acting, nonsedating H1-antihistamine that prevents antigen-induced mucus formation in sensitive rats.
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Fepradinol oxalate
0 ImagesCat. No.: HY-118854ACAS No.: 1185076-47-4Fepradinol oxalate is an orally active nonsteroidal anti-inflammatory agent. Fepradinol oxalate 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 oxalate 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 oxalate can be used in research related to occlusive contact dermatitis and acute inflammation.
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Tesmilifene fumarate (Standard)
0 ImagesCat. No.: HY-101179RCAS No.: 1185241-83-1Synonyms: DPPE fumarate (Standard)Tesmilifene (fumarate) (Standard) is the analytical standard of Tesmilifene (fumarate). This product is intended for research and analytical applications. Tesmilifene 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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Betahistine EP Impurity C (Standard)
0 ImagesCat. No.: HY-107495RCAS No.: 5452-87-9Synonyms: NSC19005 (Standard)Betahistine EP Impurity C (Standard) is the analytical standard of Betahistine EP Impurity C. This product is intended for research and analytical applications. Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine. Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA).
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Cyclizine-d3
0 ImagesCat. No.: HY-B1397SCAS No.: 1170155-67-5Cyclizine-d3 is deuterium labeled Cyclizine. Cyclizine, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine can be used for the research of nausea, vomiting, and dizziness.
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Cetirizine N-oxide
0 ImagesCat. No.: HY-W653762CAS No.: 1076199-80-8Cetirizine N-oxide is an oxidative degradation product of the histamine H1 receptor antagonist Cetirizine (HY-17042).
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VUF14862
0 ImagesCat. No.: HY-126748CAS No.: 2223023-78-5VUF14862 is a stable and fatigue-resistant photoswitchable GPCR antagonist targeting the histamine H3 receptor (H3R) pathway. VUF14862 binds to H3R with >10-fold increased affinity upon 360 nm irradiation. VUF14862 can be used for spatiotemporal studies of H3R signaling.
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S-1-Propenyl-L-cysteine (Standard)
0 ImagesCat. No.: HY-111827RCAS No.: 52438-09-2S-1-Propenyl-L-cysteine (Standard) is the analytical standard of S-1-Propenyl-L-cysteine. This product is intended for research and analytical applications. S-1-Propenyl-L-cysteine is a stereoisomer of S-allyl-l-cysteine, extracted from garlic, with immunomodulatory effects and reduces blood pressure in a hypertensive animal model. S-1-Propenyl-L-cysteine exhibits antioxidative efficacy through a NO-dependent BACH1 signaling pathway. S-1-Propenyl-L-cysteine is orally active.
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Lodoxamide tromethamine (Standard)
0 ImagesSynonyms: U-42585E (Standard)Lodoxamide (tromethamine) (Standard) is the analytical standard of Lodoxamide (tromethamine). This product is intended for research and analytical applications. Lodoxamide tromethamine (U-42585E) is a medication for the treatment of prophylaxis of mast cell-mediated allergic disease.
