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 Antagonists
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Histamine Receptor Ligand
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Histamine Receptor Related Products (514)
Related Products (514)
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Tecastemizole (Standard)
0 ImagesSynonyms: Norastemizole (Standard)Tecastemizole (Standard) is the analytical standard of Tecastemizole. This product is intended for research and analytical applications. Tecastemizole (Norastemizole), a major metabolite of Astemizole, is a potent and selective H1 receptor antagonist. Tecastemizole shows anti-inflammatory activities.
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Ranitidine hydrochloride (Standard)
0 ImagesRanitidine hydrochloride (Standard) is the analytical standard of Ranitidine hydrochloride (HY-B0281A). This product is intended for research and analytical applications. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice.
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Astemizole (Standard)
0 ImagesSynonyms: R 43512 (Standard)Astemizole (Standard) is the analytical standard of Astemizole. This product is intended for research and analytical applications. Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects.
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Fexofenadine-d3-1
0 ImagesCat. No.: HY-B0801S4Synonyms: MDL-16455-d3-1; Terfenadine carboxylate-d3-1Fexofenadine-d3-1 fumarate is deuterated labeled Fexofenadine (HY-B0801). Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research.
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Promethazine sulfoxide
0 ImagesPromethazine sulfoxide is a metabolite of the histamine H1 receptor antagonist Promethazine (HY-B1296). It is formed from promethazine by the cytochrome P450 (CYP) isoform CYP2D6.
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JNJ-39758979 (Standard)
0 ImagesCat. No.: HY-101189RCAS No.: 1046447-90-8JNJ-39758979 (Standard) is the analytical standard of JNJ-39758979 (HY-101189). This product is intended for research and analytical applications. JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.
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(S)-Azelastine
0 ImagesCat. No.: HY-B0462DCAS No.: 143228-85-7Synonyms: (+)-Azelastine(S)-Azelastine ((+)-Azelastine) is an antihistamine with antiallergic and antiasthmatic activity. (S)-Azelastine has been shown to downregulate H1R, M1R, and M3R levels. (S)-Azelastine also has the property of inhibiting HNEpC proliferation.
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Elbanizine
0 ImagesElbanizine inhibits histamine, bradykinin, histamin-release from rat mast cells (IC50 of 0.26 μM) and the IgE-mediated passive cutaneous anaphylaxis (PCA) reaction. Elbanizine exhibits antiallergic and antiasthmatic in guinea pig model.
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Burimamide
0 ImagesCat. No.: HY-124517CAS No.: 34970-69-9Burimamide is a blocker of histamine H2-receptor. Burimamide inhibits gastric acid secretion evoked by Pentagastrin (HY-A0261) or Gastrin. Burimamide also has alpha-adrenoceptor blocking activity. Burimamide in combination with the H1-receptor antagonist Mepyramine (HY-B1281) shows anti-inflammatory activity in a rat paw edema model induced by Compound 48/80 (HY-115768).
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SCH-44643
0 ImagesCat. No.: HY-123397CAS No.: 133330-43-5SCH-44643 is an orally active platelet activating factor (PAF) and histamine antagonist.
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Thiethylperazine (Standard)
0 ImagesThiethylperazine (Standard) is the analytical standard of Thiethylperazine. This product is intended for research and analytical applications. Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects.
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Ciproxifan maleate (Standard)
0 ImagesSynonyms: FUB 359 maleate (Standard)Ciproxifan (maleate) (Standard) is the analytical standard of Ciproxifan (maleate). This product is intended for research and analytical applications. Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease.
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Picumast
0 ImagesCat. No.: HY-106706CAS No.: 39577-20-3Synonyms: Auteral; BM 15100Picumast (Auteral; BM 15100) is an orally active antiallergic agent with histamine receptor antagonistic activity. Picumast inhibits allergy-related cascade reactions by suppressing mediator release from tissue mast cells while exerting histamine antagonistic effects. Picumast inhibits allergic reactions in rats, guinea pigs, and cynomolgus monkeys. Picumast can be used in allergy-related research.
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Asenapine-d3,13C
0 ImagesCat. No.: HY-10121S4CAS No.: 1217729-73-1Synonyms: Org 5222-d3,13CAsenapine-d3,13C (Org 5222-d3,13C) is deuterium and 13C labeled Asenapine. 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.
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Antihistamine-1 (Standard)
0 ImagesAntihistamine-1 (Standard) is the analytical standard of Antihistamine-1 (HY-100238). This product is intended for research and analytical applications. Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
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Decloxizine dihydrochloride (Standard)
0 ImagesSynonyms: UCB 1402 dihydrochloride (Standard); NSC289116 dihydrochloride (Standard)Decloxizine (UCB-1402; NSC289116) dihydrochloride (Standard) is the analytical standard of Decloxizine dihydrochloride. This product is intended for research and analytical applications. Decloxizine dihydrochloride is an orally active bronchodilator that can penetrate the blood-brain barrier. Decloxizine dihydrochloride is a piperazine-type H1 histamine receptor antagonist. Decloxizine dihydrochloride selectively blocks H1 histamine receptors, inhibiting histamine-induced capillary dilation, edema, and itching. Decloxizine dihydrochloride has some 5-HT2 receptor antagonistic activity. Decloxizine dihydrochloride can be used in studies of urticaria, allergic rhinitis, and bronchial asthma.
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Azatadine dimaleate (Standard)
0 ImagesSynonyms: Azatadine maleate (Standard)Azatadine dimaleate (Standard) is the analytical standard of Azatadine dimaleate. This product is intended for research and analytical applications. Azatadine dimaleate (Azatadine maleate) is an orally active histamine H1 receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine dimaleate induces sedation and exhibits topical anesthetic properties. Azatadine dimaleate can be used for the research of allergic rhinitis.
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OUP-186
0 ImagesCat. No.: HY-117981CAS No.: 1480830-24-7OUP-186 is a histamine H3 receptor antagonist.
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Cipralisant (Standard)
0 ImagesCat. No.: HY-106993RCAS No.: 213027-19-1Synonyms: GT-2331 (Standard)Cipralisant (Standard) (GT-2331 (Standard)) is the analytical standard of Cipralisant (HY-106993). This product is intended for research and analytical applications. Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research. Cipralisant 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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Oxatomide (Standard)
0 ImagesCat. No.: HY-123205RCAS No.: 60607-34-3Synonyms: KW-4354 (Standard)Oxatomide (Standard) (KW-4354 (Standard)) is the analytical standard of Oxatomide (HY-123205). This product is intended for research and analytical applications. Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases.
