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 (515)
Related Products (515)
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Methimepip dihydrobromide
0 ImagesCat. No.: HY-107554CAS No.: 817636-54-7Methimepip dihydrobromide is a potent and selective histamine H3 receptor agonist with an EC50 of 0.316nM.
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Oxomemazine (Standard)
0 ImagesCat. No.: HY-136587RCAS No.: 3689-50-7Oxomemazine (Standard) is the analytical standard of Oxomemazine (HY-136587). This product is intended for research and analytical applications. Oxomemazine is a phenothiazine-based histamine H1-receptor blocker. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites. Oxomemazine is an antihistamine and anticholinergic agent used for the study of cough treatment. Oxomemazine is protective against anaphylactic microshock in guinea pigs.
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Dihexyverine hydrochloride
0 ImagesDihexyverine hydrochloride is a compound belonging to the amino alcohol ester class. Dihexyverine hydrochloride possesses anticholinergic, smooth muscle relaxant, antihistaminic, and antiemetic effects. Dihexyverine hydrochloride can also shorten the duration of labor. Dihexyverine hydrochloride can be used in research related to gastrointestinal spasms, obstetrics, and other fields.
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Levodropropizine-d8
0 ImagesCat. No.: HY-B1895SSynonyms: (S)-(-)-Dropropizine-d8; DF-526-d8Levodropropizine-d8 is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.
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Cipralisant (enantiomer)
0 ImagesCat. No.: HY-106993BCAS No.: 223420-11-9Synonyms: GT-2331 (enantiomer)Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant (HY-106993), Cipralisant is an orally active, potent, selective, and high affinity histamine H3 receptor antagonist (rat Ki=0.47 nM). Cipralisant (enantiomer) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Benztropine-d3 mesylate
0 ImagesCat. No.: HY-B0520AS1CAS No.: 202529-16-6Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
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Mirtazapine-d4 hydrochloride
0 ImagesCat. No.: HY-B0352S3CAS No.: 1215587-73-7Mirtazapine-d4 hydrochloride is deuterated labeled Mirtazapine (HY-B0352). Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
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Pheniramine maleate (Standard)
0 ImagesSynonyms: Prophenpyridamine maleate (Standard); Tripoton maleate (Standard); Pheniramine maleate (Standard)Pheniramine (maleate) (Standard) is the analytical standard of Pheniramine (maleate). This product is intended for research and analytical applications. Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects.
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Cassiaside C2
0 ImagesCat. No.: HY-N15704CAS No.: 218155-49-8Cassiaside C2 is a naphthopyrone with a strong antiallergic activity. Cassiaside C2 inhibits the histamine release from rat peritoneal exudate mast cells induced by antigen-antibody reaction.
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Methdilazine hydrochloride (Standard)
0 ImagesCat. No.: HY-B1690ARCAS No.: 1229-35-2Thioridazine (Standard) is the analytical standard of Thioridazine. This product is intended for research and analytical applications. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
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Lafutidine-d10
0 ImagesCat. No.: HY-B0160SCAS No.: 1795136-26-3Lafutidine-d10 is deuterium labeled Lafutidine. Lafutidine (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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MY-1250
0 ImagesCat. No.: HY-129272CAS No.: 63768-47-8MY-1250 is a histamine release inhibitor. MY-1250 is the major active metabolite of Repirinast (HY-109544). MY-1250 stimulates adenylate cyclase to increase intracellular cyclic adenosine monophosphate levels, reduce intracellular ATP levels, inhibit antigen-induced intracellular calcium store mobilization, and induce phosphorylation of the 78 kDa protein. MY-1250 inhibits antigen- and phospholipase A2-induced release of histamine and slow-reacting substance of anaphylaxis from mast cells, lung tissue fragments and basophils. MY-1250 can be used in research related to allergic diseases and bronchial asthma.
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Pitolisant-d5 hydrochloride
0 ImagesCat. No.: HY-12199BSCAS No.: 2740634-42-6Synonyms: Ciproxidine-d5 hydrochloride; BF 2649-d5 hydrochloridePitolisant-d5 hydrochloride (Ciproxidine-d5 hydrochloride) is the deuterium labeled Pitolisant hydrochloride (HY-12199B). 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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Ketotifen (Standard)
0 ImagesCat. No.: HY-B0157RCAS No.: 34580-13-7Synonyms: HC 20-511 (Standard)Ketotifen (Standard) is the analytical standard of Ketotifen. This product is intended for research and analytical applications. Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.
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Cimetidine hydrochloride (Standard)
0 ImagesCat. No.: HY-14289ARCAS No.: 70059-30-2Synonyms: SKF-92334 hydrochloride (Standard)Cimetidine (hydrochloride) (Standard) is the analytical standard of Cimetidine (hydrochloride). This product is intended for research and analytical applications. Cimetidine (SKF-92334) hydrochloride is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity.
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REV 2871
0 ImagesCat. No.: HY-106076CAS No.: 80263-73-6Synonyms: Eclazolast; CHBZREV 2871 (Eclazolast; CHBZ) is a potent and oral activity antiallergic agent. REV 2871 also is an irreversibility histamine release (HR) inhibitor.
