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-14270
    Lodoxamide
    		Inhibitor 98.07%
    Lodoxamide (U-42585E free acid) is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.
    Lodoxamide
  • HY-B0188
    Mianserin
    		Inhibitor 99.42%
    Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy.
    Mianserin
  • HY-A0075
    Decloxizine dihydrochloride
    		Antagonist 99.69%
    Decloxizine (UCB-1402; NSC289116) 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.
    Decloxizine dihydrochloride
  • HY-14277A
    Levocabastine hydrochloride
    		Antagonist 99.37%
    Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).
    Levocabastine hydrochloride
  • HY-B0310
    Nizatidine
    		Antagonist 98.94%
    Nizatidine is a potent and orally active histamine H2 receptor antagonist, can be used for the research of stomach and intestines ulcers. Nizatidine works by decreasing the secretion of gastric acid the stomach makes and prevent ulcers from coming back after they have healed in animal models.
    Nizatidine
  • HY-B1215
    Dimenhydrinate
    		Inhibitor 99.89%
    Dimenhydrinate is an orally active H1-antihistamine consisting of Diphenhydramine (HY-B0303) and 8-Chlorotheophylline. Dimenhydrinate is used to prevent nausea, vomiting, dizziness, and vertigo associated with motion sickness.
    Dimenhydrinate
  • HY-14111
    GSK189254A
    		Antagonist 98.59%
    GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
    GSK189254A
  • 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-107560
    4-Methylhistamine dihydrochloride
    		Agonist 99.35%
    4-Methylhistamine hydrochloride is the dihydrochloride 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.
    4-Methylhistamine dihydrochloride
  • HY-103093
    Zotepine
    		Antagonist 99.80%
    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-19705B
    Adriforant hydrochloride
    		Antagonist 98.0%
    Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
    Adriforant hydrochloride
  • HY-13511A
    Rupatadine Fumarate
    		Antagonist 99.99%
    Rupatadine (UR-12592) Fumarate is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine Fumarate can be used for the research of allergic rhinitis and urticaria.
    Rupatadine Fumarate
  • HY-106000
    GSK239512
    		Antagonist 99.09%
    GSK239512 is a potent and brain penetrated H3 receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD).
    GSK239512
  • HY-108411
    Emedastine
    		Antagonist 98.02%
    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-B0303AS1
    Diphenhydramine-d5 hydrochloride
    		Antagonist 99.84%
    Diphenhydramine-d5 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB).
    Diphenhydramine-d<sub>5</sub> hydrochloride
  • HY-14447
    Bilastine
    		Antagonist 99.91%
    Bilastine is an oral histamine H1-receptor antagonist. Bilastine can be used for allergic rhinitis and urticaria studies, and it also improves diabetic nephropathy in mice, showing safety for the central nervous system.
    Bilastine
  • HY-101005
    N-Methylhistamine dihydrochloride
    		Agonist 99.99%
    N-Methylhistamine (Nα-Methylhistamine) dihydrochloride is a potent agonist of the histamine H3 receptor, exhibiting significant implications in the diagnosis and management of mastocytosis. N-Methylhistamine (dihydrochloride) also serves as a biomarker for assessing mast cell accumulation in clinical evaluations.
    N-Methylhistamine dihydrochloride
  • 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 99.69%
    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-N10182
    Spinacetin
    		Inhibitor 99.98%
    Spinacetin is a natural product that can be isolated from Inula japonica. Spinacetin inhibits the release of histamine. Spinacetin has anti-inflammatory activity.
    Spinacetin
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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