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 (517)
Related Products (517)
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Histamine H4 receptor antagonist-1
0 ImagesHistamine H4 receptor antagonist-1 is an antagonist of histamine H4 receptor extracted from patent WO2010108059A1 compound 60.
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Cimetidine sulfoxide
0 ImagesCat. No.: HY-136338CAS No.: 54237-72-8Synonyms: Cimetidine sulphoxideCimetidine sulfoxide (Cimetidine sulphoxide) is a sulfoxide metabolite of Cimetidine. Cimetidine is a histamine H2-receptor antagonist. Cimetidine has the potential for peptic ulcer disease and upper gastrointestinal haemorrhage treatment.
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Noberastine
0 ImagesSynonyms: R 64947Noberastine is a potent Histamine H1 antagonist. Noberastine has specific peripheral antihistamine activity .
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4-Methylhistamine hydrochloride
0 ImagesCat. No.: HY-W580721ACAS No.: 84103-51-54-Methylhistamine hydrochloride is the hydrochloride salt of 4-Methylhistamine (HY-W580721). 4-Methylhistamine hydrochloride is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki of 50 nM. 4-Methylhistamine hydrochloride has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine hydrochloride can potently activate the hH4R (pEC50 = 7.4). 4-Methylhistamine hydrochloride can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation.
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Niaprazine (Standard)
0 ImagesNiaprazine (Standard) is the analytical standard of Niaprazine. This product is intended for research and analytical applications. Niaprazine is a histamine H1-receptor antagonist. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research.
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Mequitazine (Standard)
0 ImagesSynonyms: LM-209 (Standard)Mequitazine (Standard) is the analytical standard of Mequitazine. This product is intended for research and analytical applications. Mequitazine is a potent, and long-acting histamine H1 antagonist.
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Mianserin hydrochloride (Standard)
0 ImagesSynonyms: Org GB 94 (Standard)Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy.
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Levodropropizine (Standard)
0 ImagesSynonyms: (S)-(-)-Dropropizine (Standard); DF-526 (Standard)Levodropropizine (Standard) is the analytical standard of Levodropropizine. This product is intended for research and analytical applications. Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.
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Fexofenadine-d6 Methyl Ester
0 ImagesCat. No.: HY-B0801S1CAS No.: 1286458-00-1Fexofenadine-d6 Methyl Ester is the deuterium labeled Fexofenadine Methyl Ester.
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Samelisant free base
0 ImagesCat. No.: HY-122608CAS No.: 1394808-82-2Synonyms: SUVN-G3031 free baseSamelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders.
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Mecamylamine
0 ImagesMecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.
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Adriforant
0 ImagesCat. No.: HY-19705CAS No.: 943057-12-3Synonyms: PF-3893787PF-3893787 is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
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S 38093 hydrochloride
0 ImagesCat. No.: HY-104003ACAS No.: 1222097-72-4S 38093 hydrochloride is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.
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Famotidine solution
0 ImagesCat. No.: HY-FLB0377CAS No.: 76824-35-6Synonyms: MK-208 solutionFamotidine solution is mainly composed of Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.
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Pemirolast
0 ImagesCat. No.: HY-137863CAS No.: 69372-19-6Pemirolast is an orally active antiallergic agent. Pemirolast attenuates Paclitaxel (HY-B0015) hypersensitivity reactions. Pemirolast can be used for bronchial asthma and conjunctivitis research-.
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Teverelix
0 ImagesCat. No.: HY-105173CAS No.: 151272-78-5Synonyms: EP 24332Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer.
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(E/Z)-Triprolidine-d8 hydrochloride
0 ImagesCat. No.: HY-B1808SCAS No.: 1795134-06-3(E/Z)-Triprolidine-d8 (hydrochloride) is the deuterium labeled (E/Z)-Triprolidine hydrochloride.
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Promethazine-d6 hydrochloride
0 ImagesCat. No.: HY-B1296SCAS No.: 1189947-02-1Synonyms: (±)-Promethazine-d6 hydrochloridePromethazine-d6 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist.
