2. Signaling Pathways
  3. GPCR/G Protein
    Immunology/Inflammation
    Neuronal Signaling
  4. Histamine Receptor

Histamine Receptor

Histamine Receptor

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Histamine Receptors are a class of G protein-coupled receptors with histamine as their endogenous ligand. There are four known histamine receptors: H1 receptor, H2 receptor, H3 receptor, H4 receptor. The H1 receptor is a histamine receptor belonging to the family of Rhodopsin-like G-protein-coupled receptors. This receptor, which is activated by the biogenic amine histamine, is expressed throughout the body, to be specific, in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of Protein Kinase A. Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act asautoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback inhibition of histamine synthesis and release. The Histamine H4 receptor has been shown to be involved in mediating eosinophil shape change and mast cell chemotaxis.

Histamine Receptor Isoform Specific Products:

Histamine Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-17428B
    Tripelennamine citrate
    		Antagonist
    Tripelennamine citrate, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine citrate lessens the allergic response of the organism caused by histamine. Tripelennamine citrate can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions.
    Tripelennamine citrate
  • HY-B0157S
    Ketotifen-13C,d3
    		Inhibitor
    Ketotifen-13C,d3 is deuterium labeled Ketotifen.
    Ketotifen-<sup>13</sup>C,d<sub>3</sub>
  • HY-B0274R
    Chlorprothixene (Standard)
    		Antagonist
    Chlorprothixene (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.
    Chlorprothixene (Standard)
  • HY-B0725R
    Doxepin (Hydrochloride) (Standard)
    		Antagonist
    Doxepin (Hydrochloride) (Standard) is the analytical standard of Doxepin (Hydrochloride). This product is intended for research and analytical applications. Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant.
    . Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system.
    . Doxepin has also been proposed as a protective factor against oxidative stress.
    .
    Doxepin (Hydrochloride) (Standard)
  • HY-162812
    H3R antagonist 4
    		Inhibitor
    H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu2+, Zn2+, Al3+, and Fe2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
    H3R antagonist 4
  • HY-113936
    A-943931
    		Antagonist
    A-943931 is a potent and selective histamine H4 receptor (H4R) antagonist with pKi values of 4.6, 3.8 nM for human and rat H4R, respectively. A-943931 shows anti-inflammatory and antinociceptive efficacy.
    A-943931
  • HY-B0524AS
    Betahistine-d3 dihydrochloride
    		Modulator ≥99.0%
    Betahistine-d3 (dihydrochloride) is the deuterium labeled Betahistine dihydrochloride. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].
    Betahistine-d<sub>3</sub> dihydrochloride
  • HY-155614
    KSK68
    		Antagonist
    KSK68 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.
    KSK68
  • HY-149335
    Sigma-1 receptor antagonist 5
    		Antagonist
    Sigma-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.
    Sigma-1 receptor antagonist 5
  • HY-136818
    DA 4643 dihydrochloride
    		Antagonist
    DA 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.
    DA 4643 dihydrochloride
  • HY-B0801S2
    Fexofenadine-d3
    Fexofenadine-d3 is the deuterium labeled Fexofenadine[1]. Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research[2][3][4].
    Fexofenadine-d<sub>3</sub>
  • HY-B1557A
    Betazole dihydrochloride
    		Agonist
    Betazole (Ametazole) dihydrochloride, a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole dihydrochloride induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole dihydrochloride has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity.
    Betazole dihydrochloride
  • HY-B0539S1
    Desloratadine-d9
    		Antagonist
    Desloratadine-d9 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
    Desloratadine-d<sub>9</sub>
  • HY-115833
    Histamine H4 receptor antagonist-2
    		Antagonist
    Histamine H4 receptor antagonist-2 serves as a potent activator of p53, demonstrating significant antitumor efficacy.
    Histamine H4 receptor antagonist-2
  • HY-A0178AR
    Isothipendyl (hydrochloride) (Standard)
    		Antagonist
    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.
    Isothipendyl (hydrochloride) (Standard)
  • HY-156973
    Tiopropamine
    Tiopropamine is an anti-inflammatory agent, with potential effect on histamine receptor.
    Tiopropamine
  • HY-123829
    LY2624803
    		Inhibitor
    LY2624803 is a 5-HT2A and histamine, H1 receptor antagonist.
    LY2624803
  • HY-155615
    KSK67
    		Antagonist
    KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain.
    KSK67
  • HY-107561
    A-943931 hydrochloride
    		Antagonist
    A-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 .
    A-943931 hydrochloride
  • HY-109968A
    Irdabisant hydrochloride
    		Antagonist
    Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment.
    Irdabisant hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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