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 (517)
Related Products (517)
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Fenethazine
0 ImagesFenethazine (Phenethazine) is a compound with antihistamine activity. It is an effective antihistamine. Its congeners also have anticholinergic effects and can be used to inhibit Parkinson's disease.
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Mequitazine-d8 hydrobromide
0 ImagesCat. No.: HY-B2168SSynonyms: LM-209-d8 hydrobromideMequitazine-d8 hydrobromide is deuterated labeled Mequitazine (HY-B2168). Mequitazine is a potent, and long-acting histamine H1 antagonist.
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Donetidine
0 ImagesCat. No.: HY-142090CAS No.: 99248-32-5Synonyms: SK&F 93574Donetidine (SK&F 93574) is an antagonist for histamine H2 receptor, that promotes histamine release in beagle dog models.
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ADS1017
0 ImagesCat. No.: HY-170444CAS No.: 1383657-36-0ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pKi of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin (HY-10448)-or Oxaliplatin (HY-17371)-induced pain models.
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Azelastine-d4 hydrochloride
0 ImagesCat. No.: HY-B0462S1CAS No.: 2747915-85-9Azelastine-d4 (hydrochloride) is deuterium-labeled Azelastine (hydrochloride) (HY-B0462).
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Eukovoside
0 ImagesCat. No.: HY-N17566CAS No.: 83475-36-9Eukovoside is a cinnamic acid derivative found in Euphrasia regelii with anti-inflammatory, antioxidant, antibacterial, antiallergic, and antihistamine activity. Eukovoside can be used for the research of hyperglycemic diseases, eye inflammation, upper respiratory passages inflammation, hay fever, conjunctivitis, colds, influenza, sinusitis.
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Levomepromazine hydrochloride
0 ImagesLevomepromazine (Methotrimeprazine) hydrochloride is an orally active antipsychotic compound and Ca2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca2+ levels. Levomepromazine hydrochloride has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine hydrochloride can induce adaptive ER stress and autophagy. In addition, Levomepromazine hydrochloride has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine hydrochloride can be used in the study psychiatric disorders and relieving nausea and vomiting.
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Dimethothiazine hydrochloride
0 ImagesCat. No.: HY-A0157BCAS No.: 34396-64-0Synonyms: Dimetotiazine hydrochloride; Fonazine hydrochlorideDimethothiazine hydrochloride 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 hydrochloride can reduce or abolish the effects of both static and dynamic fusimotor activity on the muscle spindle in decerebrate cat. Dimethothiazine hydrochloride can be used to research hemicrania and spasticity.
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(R)-Azelastine hydrochloride
0 ImagesCat. No.: HY-B0462CCAS No.: 153408-28-7(R)-Azelastine hydrochloride, an antihistamine, has been demonstrated to down-regulate the levels of H1R, M1R, and M3R, while also inhibiting the proliferation of HNEpC.
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Linadryl
0 ImagesLinadryl is a compound with antihistamine and other effects. It has a variable effect on gastric acid secretion after oral administration, and its effect is about half that of Diphenhydramine (HY-B0303).
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Contilisant
0 ImagesCat. No.: HY-123928CAS No.: 2135615-68-6Contilisant is a permeable antioxidant and neuroprotectant agent. Contilisant exhibits high nM affinity at H3R. Contilisant inhibits monoamine oxidases and cholinesterases. Contilisant has a binding affinity of 65.23 nM towards hS1R. Contilisant can significantly restore cognitive deficit induced by Aβ1-42 in the radial maze assay of Alzheimer’s animal model.
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GS 283
0 ImagesCat. No.: HY-114743CAS No.: 149440-36-8GS 283 is a compound with calcium antagonist and weak histamine and muscarinic receptor blocking activity, with activity in modulating contraction of guinea pig and rat tracheal smooth muscle. GS 283 inhibits contractions induced by carbachol, histamine (guinea pig only), and high H+ in guinea pig and rat tracheal smooth muscle, inhibits Ca2+-induced contractions in guinea pig tracheal smooth muscle, and at high concentrations completely abolishes contractions induced by carbachol in Ca2+-free medium.
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4-AcO-DALT hydrochloride
0 ImagesCat. No.: HY-172339Synonyms: 4-Acetoxy DALT hydrochloride4-AcO-DALT hydrochloride is a tryptamine compound with psychoactive effects. 4-AcO-DALT hydrochloride inhibits 5-HT receptors, alpha receptors, dopamine receptors, histamine receptor 1 (H1), muscarinic M2 receptor and Sigma 2 receptor. 4-AcO-DALT hydrochloride shows Ki values of 582 nM, 2689 nM, 2099 nM, 2116 nM, 958 nM, 137 nM, 824 nM, 479 nM, 406 nM, 874 nM, 4190 nM, 482 nM, 214 nM, 803 nM, 4522 nM, 1907 nM for 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5-HT7A, H1, Sigma 2, α2A, α2B, α2C, D2, D3 receptors.
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Alimemazine-d6 hydrochloride
0 ImagesCat. No.: HY-12752BSCAS No.: 1352792-16-5Synonyms: Trimeprazine-d6 hydrochlorideAlimemazine-d6 hydrochloride (Trimeprazine-d6 hydrochloride) is the deuterium labeled Alimemazine (HY-12752). Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties.
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Azapetine
0 ImagesAzapetine is an antagonist of α1-adrenoceptor, with an IC50 of 0.205 μM at rat α1-adrenoceptor and an IC50 of 1.3 μM at rat α2-adrenoceptor, and exhibits higher selectivity for α1-adrenoceptor than for α2-adrenoceptor. Azapetine functionally blocks postsynaptic α1-adrenoceptors, and at higher concentrations, it blocks presynaptic α2-adrenoceptors, central α-adrenoceptors, and H2 histamine receptors. Azapetine is used in related research on hypotension.
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RS-51324
0 ImagesCat. No.: HY-123398CAS No.: 69811-30-9
