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 Activators
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Histamine Receptor Modulators
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Histamine Receptor Controls
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Histamine Receptor Ligand
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Histamine Receptor Related Products (514)
Related Products (514)
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C-Type Natriuretic Peptide (CNP) (1-22), human TFA
0 ImagesC-Type Natriuretic Peptide (CNP) (1-22), human (TFA),a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human (TFA) inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor.
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Histamine (Standard)
0 ImagesHistamine (Standard) is the analytical standard of Histamine (HY-B1204). This product is intended for research and analytical applications. Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.
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Adriforant hydrochloride
0 ImagesSynonyms: PF-3893787 hydrochlorideAdriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
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Carcainium chloride
0 ImagesSynonyms: QX 572; RSD 931Carcainium chloride (QX 572) is a quaternary derivative of Lidocaine. Antitussive effect.
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Lodoxamide tromethamine
0 ImagesSynonyms: U-42585ELodoxamide tromethamine (U-42585E) is a medication for the treatment of prophylaxis of mast cell-mediated allergic disease.
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XmAb-7195
0 ImagesCat. No.: HY-P991252Purity: 99.98%Synonyms: AIMab-7195XmAb-7195 (AIMab-7195) is a human monoclonal antibody (mAb) targeting IGHE. XmAb-7195 can be used in Food hypersensitivity, Allergic asthma, Allergic rhinitis, Atopic dermatitis and Conjunctivitis research.
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Dropropizine
0 ImagesSynonyms: (±)-Dropropizine; UCB-196Dropropizine ((±)-Dropropizine; UCB-196) is an orally effective, peripherally selective antitussive that inhibits the activity of peripheral receptors and afferent nerves in the respiratory tract. Dropropizine acts on the cough reflex pathway, does not pass the blood-brain barrier, and has no central nervous system side effects. Dropropizine mainly regulates the level of sensory neuropeptides and inhibits the afferent signal transmission of the cough reflex, thereby alleviating the symptoms of dry cough, and has both mild local anesthetic and antihistamine activity. Dropropizine is mainly used for symptomatic research on dry cough caused by respiratory diseases.
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Samelisant
0 ImagesSynonyms: SUVN-G3031Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders.
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Mequitazine
0 ImagesSynonyms: LM-209Mequitazine is a potent, and long-acting histamine H1 antagonist.
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Alimemazine hemitartrate
0 ImagesAlimemazine hemitartrate (Trimeprazine hemitartrate) is an antagonist of the histamine (HA) receptor that can be taken orally and also acts as a partial agonist at other GPCR receptors. Alimemazine hemitartrate has effects that include anti-serotonin, antispasmodic, antihistamine, sedation, hypnotic, antiviral, and anti-nausea properties. Alimemazine hemitartrate promotes the growth of pancreatic β-cells in mice and improves diabetes in mice.
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Antazoline hydrochloride
0 ImagesAntazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV.
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Dothiepin
0 ImagesDothiepin (Dosulepin; Dothep) is an antidepressant agent with sedative/anxiolytic activity. Dothiepin is an inhibitor preferring of noradrenaline uptake than serotonin uptake. Dothiepin facilitates noradrenergic neurotransmission via inhibiting the neuronal uptake. Dothiepin is also an antagonist of histamine H1-receptor without cardiotoxicity. Dothiepin exhibits significant analgesic activity in psychogenic facial pain，idiopathic fibromyalgia syndrome or rheumatoid arthritis.
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Tecastemizole
0 ImagesSynonyms: NorastemizoleTecastemizole (Norastemizole), a major metabolite of Astemizole, is a potent and selective H1 receptor antagonist. Tecastemizole shows anti-inflammatory activities.
