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

Histamine Receptor

Histamine Receptor

Related Products

PDF 3.72 MB

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-108411
    Emedastine
    		Antagonist 98.01%
    Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
    Emedastine
  • HY-P1237A
    C-Type Natriuretic Peptide (CNP) (1-22), human TFA
    		Inhibitor 98.10%
    C-Type Natriuretic Peptide (CNP) (1-22), human (TFA),a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human (TFA) inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor.
    C-Type Natriuretic Peptide (CNP) (1-22), human TFA
  • HY-B0895
    Hydroxyzine pamoate
    		Antagonist 99.85%
    Hydroxyzine pamoate is a histamine receptor H1 antagonist, one of the salt forms of Hydroxyzine, soluble in dimethyl formamide and chloroform but insoluble in water and alcohol.
    Hydroxyzine pamoate
  • HY-B0426A
    Olopatadine hydrochloride
    		Inhibitor 99.71%
    Olopatadine hydrochloride (ALO4943A) is a histamine blocker used to treat allergic conjunctivitis.
    Olopatadine hydrochloride
  • HY-B0164
    Mizolastine
    		Antagonist 99.82%
    Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial.
    Mizolastine
  • HY-B0157
    Ketotifen
    		Inhibitor 99.74%
    Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.
    Ketotifen
  • HY-103093
    Zotepine
    		Antagonist 99.85%
    Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo.
    Zotepine
  • HY-B1305
    Chloropyramine hydrochloride
    		Antagonist 99.64%
    Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
    Chloropyramine hydrochloride
  • HY-16567
    Asenapine hydrochloride
    		Antagonist 99.95%
    Asenapine (Org 5222) hydrochloride, 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 hydrochloride can be used in the research of schizophrenia and bipolar disorderr.
    Asenapine hydrochloride
  • HY-W014941
    (R)-(-)-α-Methylhistamine dihydrochloride
    		Agonist 99.62%
    (R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats.
    (R)-(-)-α-Methylhistamine dihydrochloride
  • HY-148825
    NP10679
    		Antagonist 98.40%
    NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.
    NP10679
  • HY-B1301
    Triprolidine hydrochloride monohydrate
    		Antagonist 99.92%
    Triprolidine hydrochloride monohydrate, a first-generation antihistamine, is an oral active histamine H1 antagonist. Triprolidine hydrochloride monohydrate can be used for the research of allergic rhinitis. Triprolidine hydrochloride monohydrate exhibits spinal motor and sensory block in rats.
    Triprolidine hydrochloride monohydrate
  • HY-B1062
    Dexchlorpheniramine maleate
    		Inhibitor ≥98.0%
    Dexchlorpheniramine maleate is an orally taken anti-histamine that has anti-inflammatory, anti-irritant, anti-allergic, and skin barrier effects. Dexchlorpheniramine maleate inhibits myocardial contraction in rats. Dexchlorpheniramine maleate can be used in studies of allergic rhinitis.
    Dexchlorpheniramine maleate
  • HY-B0538A
    Pemirolast potassium
    		Antagonist 99.99%
    Pemirolast potassium is an orally active antiallergic agent. Pemirolast potassium attenuates Paclitaxel (HY-B0015) hypersensitivity reactions. Pemirolast potassium can be used for bronchial asthma and conjunctivitis research-.
    Pemirolast potassium
  • HY-14537
    Latrepirdine dihydrochloride
    		Antagonist 99.65%
    Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β (Aβ) secretion.
    Latrepirdine dihydrochloride
  • HY-101198
    Clobenpropit dihydrobromide
    		Modulator 99.76%
    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
    Clobenpropit dihydrobromide
  • HY-B1478
    Dimaprit dihydrochloride
    		Agonist 99.91%
    Dimaprit dihydrochloride is a selective histamine H2 receptor agonist, it also inhibits nNOS with an IC50 of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion.
    Dimaprit dihydrochloride
  • HY-107568
    Iodophenpropit dihydrobromide
    		Antagonist 99.70%
    Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [125I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM).
    Iodophenpropit dihydrobromide
  • HY-B0640A
    Epinastine hydrochloride
    		Antagonist 99.73%
    Epinastine hydrochloride (WAL801 hydrochloride) is a selective and orally active histamine H1 receptor antagonist, CD96/PVR inhibitor and mast cell stabilizer. Epinastine hydrochloride has high affinity for neuronal octopamine receptors in locusts (Ki = 2 nM) and honeybees (Ki = 1.1 nM). Epinastine hydrochloride inhibits TARC, IL-8, and IL-4. Epinastine hydrochloride activates anti-colon cancer immunity and inhibits Substance P (HY-P0201)-induced scratching behavior and increased vascular permeability. Epinastine hydrochloride can be used in the research of allergic diseases.
    Epinastine hydrochloride
  • HY-15289
    Ciproxifan maleate
    		Antagonist 99.68%
    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.
    Ciproxifan maleate
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.