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 Agonists
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Histamine Receptor Antagonists
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Histamine Receptor Ligand
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Histamine Receptor Related Products (515)
Related Products (515)
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Lafutidine
0 ImagesSynonyms: FRG-8813Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H2RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease.
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Terfenadine (Standard)
0 ImagesSynonyms: (±)-Terfenadine (Standard); MDL-991 (Standard)Terfenadine (Standard) is the analytical standard of Terfenadine. This product is intended for research and analytical applications. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
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Conessine
0 ImagesConessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy.
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Methapyrilene
0 ImagesMethapyrilene is a histamine antagonist, a pyridine chemical with anticholinergic activity. Methapyrilene can cause target organ-specific epigenetic alterations, such as a decrease in DNA methylation levels. Methapyrilene induces hepatocellular carcinoma in rats.
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Histamine dehydrogenase, Microorganism
0 ImagesCat. No.: HY-E70517CAS No.: 89190-47-6Histamine dehydrogenase, Microorganism (EC 1.4.99) is a homodimeric enzyme which catalyzes oxidative deamination of histamine in the presence of electron carrier.
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Repirinast
0 ImagesCat. No.: HY-109544CAS No.: 73080-51-0Synonyms: MY-5116Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma.
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Azatadine dimaleate
0 ImagesAzatadine dimaleate (Azatadine maleate) is an orally active histamine H1 receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine dimaleate induces sedation and exhibits topical anesthetic properties. Azatadine dimaleate can be used for the research of allergic rhinitis.
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Levocetirizine dihydrochloride (Standard)
0 ImagesSynonyms: (R)-Cetirizine dihydrochloride (Standard)Levocetirizine (dihydrochloride) (Standard) is the analytical standard of Levocetirizine (dihydrochloride). This product is intended for research and analytical applications. Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.
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Levomepromazine maleate
0 ImagesSynonyms: Methotrimeprazine maleateLevomepromazine maleate (Methotrimeprazine maleate) is an orally active antipsychotic compound and Ca2+ release inducer. Levomepromazine maleate inhibits SERCA pump and induces an increase in cytoplasmic Ca2+ levels. Levomepromazine maleate has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine maleate can induce adaptive ER stress and autophagy. In addition, Levomepromazine maleate has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine maleate can be used in the study psychiatric disorders and relieving nausea and vomiting.
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Levodropropizine
0 ImagesSynonyms: (S)-(-)-Dropropizine; DF-526Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.
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Marmin
0 ImagesMarmin is a histamine receptor inhibitor and tracheal smooth muscle relaxant. Marmin antagonizes histamine- and methacholine-induced contraction of tracheal smooth muscle. Marmin inhibits histamine release from mast cells, and also blocks extracellular calcium influx via voltage-dependent calcium channels as well as calcium release from intracellular calcium stores, thereby effectively inhibiting calcium-mediated smooth muscle contraction. Marmin slightly enhances the relaxant effect of isoprenaline, and induces epithelial-dependent tracheal smooth muscle relaxation independent of nitric oxide, cGMP or β2-adrenergic pathways through the release of prostaglandin E2.
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Amitriptyline-d6 hydrochloride
0 ImagesAmitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
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Chlorpheniramine maleate (Standard)
0 ImagesSynonyms: Chlorphenamine maleate (Standard)Chlorpheniramine (maleate) (Standard) is the analytical standard of Chlorpheniramine (maleate). This product is intended for research and analytical applications. Chlorpheniramine maleate is a histamine H1 receptor antagonist with an IC50 of 12 nM.
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Methdilazine hydrochloride
0 ImagesMethdilazine hydrochloride is an orally active antibiotic (histamine antagonist). Methdilazine hydrochloride can inhibit various mycobacterium with MIC values at 5-15 μg/mL in vitro and in vivo, which can be used for the research of infectious diseases.
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Diphenhydramine (Standard)
0 ImagesDiphenhydramine (Standard) is the analytical standard of Diphenhydramine. This product is intended for research and analytical applications. Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
