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 Ligand
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Histamine Receptor Related Products (517)
Related Products (517)
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Benztropine mesylate (Standard)
0 ImagesSynonyms: Benzatropine mesylate (Standard); Benzotropine mesylate (Standard); Benztropine methanesulfonate (Standard)Benztropine (mesylate) (Standard) is the analytical standard of Benztropine (mesylate). This product is intended for research and analytical applications. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
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Ketotifen-13C,d3
0 ImagesCat. No.: HY-B0157SCAS No.: 2748522-40-7Synonyms: HC 20-511-13C,d3Ketotifen-13C,d3 is deuterium labeled Ketotifen.
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Chlorprothixene (Standard)
0 ImagesChlorprothixene (Standard) is the analytical standard of Chlorprothixene. This product is intended for research and analytical applications. Chlorprothixene is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity.
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(Z)-Thiothixene-d8
0 ImagesCat. No.: HY-W748758Synonyms: NSC 108165-d8; Navan-d8; Navane-d8(Z)-Thiothixene-d8 (NSC 108165-d8; Navan-d8; Navane-d8) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
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Levomepromazine-d6 hydrochloride
0 ImagesCat. No.: HY-166562SSynonyms: Methotrimeprazine-d6 hydrochlorideLevomepromazine-d6 hydrochloride (Methotrimeprazine-d6 hydrochloride) is the deuterium labeled Levomepromazine hydrochloride. Levomepromazine (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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KSK68
0 ImagesCat. No.: HY-155614CAS No.: 2566715-91-9KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain.
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Sigma-1 receptor antagonist 5
0 ImagesCat. No.: HY-149335CAS No.: 2952808-33-0Sigma-1 receptor antagonist 5 (compound 12)，a 4-pyridylpiperidine derivative with analgesic activity，is an antagonist of sigma receptor (Ki=4.5 nM (σ1R)，10 nM (σ2R)) and histamine H3 (hH3R，Ki=7.7 nM，IC50=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models.
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DA 4643 dihydrochloride
0 ImagesCat. No.: HY-136818CAS No.: 95833-19-5DA 4643 (hydrochloride) is an H2 receptor antagonist with the chemical name 2-guanidino-4 (3-methylaminomethyleneiminophenyl) thiazole dihydrochloride. It has a weak interaction with cytochrome P-450 and has a less inhibitory effect on P-450 than cimetidine and tiotidine. DA 4643 (hydrochloride) is able to inhibit both enzymatic and non-enzymatic lipid peroxidation reactions. This inhibition may not be achieved by inhibiting agent metabolizing enzymes, but rather due to the antioxidant properties of the compound itself. Compared with other H2 receptor antagonists such as cimetidine, ranitidine and tiotidine, DA 4643 (hydrochloride) shows a unique effect in lipid peroxidation inhibition. These properties make DA 4643 (hydrochloride) a potential H2 receptor antagonist with multiple mechanisms of action.
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Fexofenadine-d3
0 ImagesCat. No.: HY-B0801S2Synonyms: MDL-16455-d3; Terfenadine carboxylate-d3Fexofenadine-d3 is the deuterium labeled Fexofenadine. 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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Histamine H4 receptor antagonist-2
0 ImagesCat. No.: HY-115833CAS No.: 379247-14-0Histamine H4 receptor antagonist-2 serves as a potent activator of p53, demonstrating significant antitumor efficacy.
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Isothipendyl hydrochloride (Standard)
0 ImagesCat. No.: HY-A0178ARCAS No.: 1225-60-1Synonyms: NSC 169186 (Standard)Isothipendyl (hydrochloride) (Standard) is the analytical standard of Isothipendyl (hydrochloride). This product is intended for research and analytical applications. Isothipendyl hydrochloride (), an azaphenothiazine derivative, is a potent histamine 1 (H1) receptor antagonist.othipendyl is a primary metabolite.
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Tiopropamine
0 ImagesCat. No.: HY-156973CAS No.: 39516-21-7Tiopropamine is an anti-inflammatory agent, with potential effect on histamine receptor.
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A-943931 hydrochloride
0 ImagesCat. No.: HY-107561CAS No.: 1227675-50-4A-943931 (Compound 10) is a histamine H4 receptor antagonists. A-943931 has improved pharmacotropic and in vivo efficacy in models of pain and inflammation. A-943931 can be used in vivo anti-inflammatory and anti-nociception research .
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Gallocatechin-3-O-(3″-O-methyl)-gallate
0 ImagesCat. No.: HY-171338CAS No.: 264147-80-0Synonyms: GCG3″MeGallocatechin-3-O-(3''-O-methyl)-gallate (GCG3''Me) is a catechin polyphenol. Gallocatechin-3-O-(3''-O-methyl)-gallate inhibits histamine release. Gallocatechin-3-O-(3''-O-methyl)-gallate can be used in allergy-related studies.
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Quifenadine hydrochloride
0 ImagesCat. No.: HY-W492795CAS No.: 10447-38-8Quifenadine hydrochloride is an H1-histamine receptor blocker and can be used in the research of anti-arrhythmia.
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Undecane-d24
0 ImagesCat. No.: HY-N8593SCAS No.: 164858-54-2Undecane-d24 is the deuterium labeled Undecane (HY-N8593).Undecane is a potent cAMP agonist with anti-allergic and anti-inflammatory activities. Undecane inhibits degranulation and the secretion of histamine and TNF-α. Undecane reverses the increased levels of p38 phosphorylation, NF-κB transcriptional activity and target cytokine/chemokine genes, including thymus and activation-regulated chemokine (TARC), macrophage-derived chemokine (MDC) and interleukin-8 (IL-8). Undecane can be used for the study of skin inflammatory disorders, such as atopic dermatitis.
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Aceprometazine
0 ImagesCat. No.: HY-A0243CAS No.: 13461-01-3Synonyms: 1664CB; AcepromethazineAceprometazine (1664CB) is an orally active antipsychotic. Aceprometazine can be used in the study of psychiatric disorders, such as depression.
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Zaltidine dihydrochloride
0 ImagesCat. No.: HY-15541ACAS No.: 90274-23-0Synonyms: CP-5736 dihydrochlorideZaltidine (CP-5736) dihydrochloride is a highly specific H2 receptor antagonist with antisecretion activity. Zaltidine dihydrochloride reduces the stimulant effect of histamine on gastric acid secretion by binding to histamine H2 receptors on gastric parietal cells, thus reducing gastric acid production. Zaltidine dihydrochloride can be used in the study of gastric acid-related diseases such as duodenal ulcers.
