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 Ligand
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Histamine Receptor Related Products (517)
Related Products (517)
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(±)-Carbinoxamine-d6
0 ImagesCat. No.: HY-B1589SCAS No.: 1216872-59-1(±)-Carbinoxamine-d6 is the deuterium labeled (±)-Carbinoxamine (HY-B1589). (±)-Carbinoxamine is a blood-brain barrier-permeable histamine H1 receptor antagonist. (±)-Carbinoxamine blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. (±)-Carbinoxamine inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. (±)-Carbinoxamine can be used in research on allergic rhinitis, influenza, etc.
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N-Desmethyl diphenhydramine-d3 (hydrochloride)
0 ImagesCat. No.: HY-139519SCAS No.: 1794759-12-8N-Desmethyl diphenhydramine-d3 (hydrochloride) is the deuterium labeled N-Desmethyl diphenhydramine hydrochloride.
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Linetastine
0 ImagesCat. No.: HY-123103CAS No.: 159776-68-8Linetastine is an orally active and potent 5-Lipoxygenase inhibitor. Linetastine shows antihistamine activity. Linetastine inhibits leukotriene production and antagonizes the effect of histamine. Linetastine inhibits the release of leukotrienes B4 and C4 from calcium ionophore-stimulated human leukocytes.
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CP19
0 ImagesCat. No.: HY-146815CAS No.: 1018148-68-9
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Platelet aggregation-IN-3
0 ImagesCat. No.: HY-176060CAS No.: 1029802-21-8Platelet aggregation-IN-3 (Compound 5) is a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. Platelet aggregation-IN-3 can inhibit platelet aggregation induced by ADP and collagen and can also modulate tumour cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is promising for research of antiplatelet therapy in cardiovascular diseases and the prevention of cancer-related thrombosis and tumour metastasis.
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Alcaftadine carboxylic acid-d3 sodium
0 ImagesCat. No.: HY-124356ASAlcaftadine carboxylic acid-d3 (sodium) is deuterium labeled Alcaftadine carboxylic acid. Alcaftadine carboxylic acid is a broad-spectrum antihistamine compound with high affinity for histamine H1 and H2 receptors and low affinity for H4 receptors. Alcaftadine carboxylic acid has also demonstrated effects on modulating immune cell recruitment and stabilizing mast cells. Alcaftadine carboxylic acid is more effective than placebo in preventing ocular itching associated with allergic conjunctivitis and is at least as effective as olopatadine 0.01%.
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Chlorpheniramine (Standard)
0 ImagesChlorpheniramine (Standard) is the analytical standard of Chlorpheniramine. This product is intended for research and analytical applications. Chlorpheniramine is a H1 antihistamines commonly used in allergic diseases research.
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UCL-1972
0 ImagesCat. No.: HY-124389CAS No.: 220728-17-6UCL-1972 is an antagonist of Histamine H3 receptor. UCL-1972 can be studied in research on cognitive diseases.
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Acrivastine-d7
0 ImagesCat. No.: HY-B1510SCAS No.: 172165-56-9Synonyms: BW825C d7Acrivastine-d7 is a deuterium labeled Acrivastine. Acrivastine is a short acting histamine 1 receptor antagonist.
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Azelastine-d3
0 ImagesCat. No.: HY-W744206CAS No.: 758637-88-6Azelastine-d3 is the deuterium labeled Azelastine (HY-B0462A). Azelastine, an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2.
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R 58639
0 ImagesCat. No.: HY-178727CAS No.: 99157-83-2R 58639 is a histamine H1 receptor antagonist. R 58639 can be used for the study of gastric ulcers.
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A-331440
0 ImagesCat. No.: HY-12191CAS No.: 392338-13-5A-331440 is a potent and selective histamine H3 receptor antagonist that regulates neurotransmitter release by inhibiting presynaptic H3 receptors. In preclinical studies involving mice on a high-fat diet, A-331440 demonstrated dose-dependent effects on weight reduction and fat loss. At 5 mg/kg, it effectively decreased body weight comparable to dexfenfluramine, while at 15 mg/kg, it significantly reduced body fat and improved insulin tolerance, similar to mice on a low-fat diet. These findings suggest that A-331440 holds promise as an antiobesity agent by modulating histaminergic pathways involved in food intake and metabolic regulation.
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Wy 45086
0 ImagesCat. No.: HY-182431CAS No.: 87476-50-4Wy 45086 is a histamine H2 receptor antagonist. Wy 45086 blocks the H2 receptor signaling pathway and inhibits gastric acid secretion in experimental animals. Wy 45086 can be used in ulcer-related research.
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Sequifenadine
0 ImagesCat. No.: HY-W281862CAS No.: 57734-69-7Sequifenadine is a H1-antihistamine. Sequifenadine has the potential for the research of inflammatory eye disease with allergic symptoms.
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Azacyclonol (Standard)
0 ImagesAzacyclonol (Standard) is the analytical standard of Azacyclonol. This product is intended for research and analytical applications. Azacyclonol (γ-pipradol), a metabolite of Terfenadine, is a central depressant agent. Azacyclonol is a ganglion-blocking agent. Azacyclonol can be used to diminish psychoses-induced hallucinations.
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H3R antagonist 1
0 ImagesH3R antagonist 1 is a histamine receptor 3 (H3R) inverse agonist. H3R antagonist 1 increases the expression levels of myelin-associated glycoprotein (MAG) and myeline basic protein (MBP) in differentiating oligodendrocytes. H3R antagonist 1 can be used for the study of multiple sclerosis.
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Chlorphenoxamine hydrochloride
0 ImagesChlorphenoxamine hydrochloride, an antihistamine and anticholinergic agent is a GPCR antagonist. Chlorphenoxamine hydrochloride inhibits multiple lethal viral diseases, such as SARS-CoV, MERS-CoV, EBOV and malaria. Chlorphenoxamine hydrochloride shows anti-filovirus activity against both EBOV and Marburg virus (MARV) with IC50s of 1.1 μM and 6.2 μM, respectively. Chlorphenoxamine hydrochloride is used for allergic conditions, urticaria, viral diseases and Parkinson’s disease.
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Dimethothiazine mesylate
0 ImagesCat. No.: HY-A0157ACAS No.: 13115-40-7Synonyms: Dimetotiazine mesylate; Fonazine mesylateDimethothiazine mesylate is an orally active tricyclic anti-histamine, anti-5-HT agent with a high activity against decerebrate rigidity, a little sedative activity and little soporific action. Dimethothiazine mesylate can reduce or abolish the effects of both static and dynamic fusimotor activity on the muscle spindle in decerebrate cat. Dimethothiazine mesylate can be used to research hemicrania and spasticity.
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Aplysamine-1
0 ImagesCat. No.: HY-117500CAS No.: 159026-30-9Aplysamine-1 acts as an antagonist for the histamine H3 receptor.
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Asenapine-13C,d3
0 ImagesCat. No.: HY-10121S2CAS No.: 2747915-30-4Synonyms: Org 5222-13C,d3Asenapine-13C,d3 is 13C and deuterated labeled Asenapine (HY-10121). Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
