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 (514)
Related Products (514)
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BL 6341A
0 ImagesCat. No.: HY-169833CAS No.: 78441-84-6BL 6341A is an antagonist for histamine H2 receptor with Ki of 3.5-4.4 nM, that inhibits histamine-induced acid secretion and cAMP formation. BL 6341A can be used in research of gastric acid secretion related diseases, such as gastric ulcer or gastroesophageal reflux.
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DF-1111301
0 ImagesCat. No.: HY-106924CAS No.: 127842-07-3DF 1111301 is a new antiallergic compound endowed of antihistamine-H1 and anti-PAF activities.
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3-Hydroxy desloratadine
0 Images3-Hydroxy desloratidine is a metabolite of Desloratidine.
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Promethazine-d4
0 ImagesCat. No.: HY-B1296S1CAS No.: 1173147-64-2Synonyms: (±)-Promethazine-d4; N,N-dimethyl-1-phenothiazin-10-yl-propan-2-amine-d4
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(+)-Dropropizine
0 ImagesCat. No.: HY-B1032ACAS No.: 99291-24-4Synonyms: (R)-Dropropizine(+)-Dropropizine ((R)-Dropropizine), an isomer of Dropropizine (HY-B1032), is an orally active histamine receptor inhibitor with anti-allergic effects. (+)-Dropropizine reduces a cough by modulation of neuropeptides involved in the cough reflex and by interfering with stimulus activation of peripheral endings of sensory nerves. (+)-Dropropizine is promising for research of dry cough caused by respiratory diseases.
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Proterguride
0 ImagesCat. No.: HY-106465CAS No.: 77650-95-4Proterguride is a potent dopamine receptor agonist. Proterguride also shows antagonistic properties at the histamine H(1) receptor and alpha(1)-adrenoceptor and partially agonize serotonergic 5-HT2A/B receptor. Proterguride can be used for the research of neurological disease, such as Parkinson's disease .
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VUF14480
0 ImagesCat. No.: HY-165453CAS No.: 1605304-31-1VUF14480 is a partial agonist of histamine H4 (hH4) receptor-mediated G protein signalling and β-arrestin2 recruitment. VUF14480 binds covalently to hH4 receptor (pKi: 6.3 for hH4-WT receptor). VUF14480 partially induces hH4 receptor-mediated G protein activation and β-arrestin2 recruitment. VUF14480 can be used in the research of inflammatory diseases.
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VUF10497
0 ImagesCat. No.: HY-118336CAS No.: 1080623-12-6VUF10497 is a potent histamine H4 receptor (H4R) inverse agonist with anti-inflammatory activity.
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Alcaftadine carboxylic acid
0 ImagesCat. No.: HY-124356CAS No.: 147083-93-0Alcaftadine 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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Sch-40338
0 ImagesCat. No.: HY-116435CAS No.: 117796-62-0Sch-40338 is a dual antagonist of platelet-activating factor (PAF) and histamine with an IC50 of 0.59 μM (PAF-induced platelet aggregation) and a Ki of 5.4 μM (Histamine H₁ receptor binding). Sch-40338 can be used for the study of allergic disease.
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Mecamylamine hydrochloride (Standard)
0 ImagesMecamylamine (hydrochloride) (Standard) is the analytical standard of Mecamylamine (hydrochloride). This product is intended for research and analytical applications. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.
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Cinnarizine-d8
0 ImagesCinnarizine-d8 is a deuterium labeled Cinnarizine. Cinnarizine is an antihistamine and a calcium channel blocker.
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AHR-13268D
0 ImagesCat. No.: HY-123432CAS No.: 130838-11-8AHR-13268D is an oral active antiallergic and antihistaminic agent, with bioavailable approximately 88%. AHR-13268D is a potent inhibitor of histamine release from rat peritoneal mast cells, with the IC50 of 0.51 nM.
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Panaxydiol
0 ImagesCat. No.: HY-N3114CAS No.: 63910-76-9Panaxydiol exhibits histamine-release inhibition activity. Panaxydiol 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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Mifentidine
0 ImagesCat. No.: HY-19007CAS No.: 83184-43-4Synonyms: DA 4577Mifentidine (DA 4577) is a potent and selective H2 Receptor antagonist. Mifentidine has an anti-secretion effect and can antagonize the acid-promoting activity of histamine with EC50 3.28 μM.
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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.
