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-101198
    Clobenpropit dihydrobromide
    		Modulator 98.99%
    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-12206
    Thioperamide
    		Antagonist 99.91%
    Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide inhibits [3H]histamine synthesis with a Ki of 31 nM.
    Thioperamide
  • HY-148825
    NP10679
    		Antagonist 99.42%
    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-B0524A
    Betahistine dihydrochloride
    		Modulator 99.82%
    Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA).
    Betahistine dihydrochloride
  • 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-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-B0970
    Diphenylpyraline hydrochloride
    		Inhibitor 99.94%
    Diphenylpyraline hydrochloride is a potent histamine H1?receptor antagonist. Diphenylpyraline hydrochloride acts as an orally active antihistamine agent?with antimuscarinic and antiallergic effects. Diphenylpyraline hydrochloride can be used for the relief of allergic conditions including rhinitis and hay fever, and in pruritic skin disorders in vivo.
    Diphenylpyraline hydrochloride
  • HY-B0538A
    Pemirolast potassium
    		Antagonist 99.93%
    Pemirolast potassium (TWT-8152) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.
    Pemirolast potassium
  • 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-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-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-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-B1557
    Betazole
    		Agonist
    Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active histamine H2 receptor agonist. Betazole induces gastric acid secretion and causes an immediate and significant increase in common bile duct pressure. Betazole is used as a diagnostic agent known as histalog for investigating gastric acid secretory capacity.
    Betazole
  • HY-B1303A
    Mebhydrolin
    		Antagonist 99.78%
    Mebhydrolin is a specific histamine H1 receptor antagonist.
    Mebhydrolin
  • HY-15538
    Ebrotidine
    		Antagonist 98.51%
    Ebrotidine(FI 3542) is a competitive H2-receptor antagonist (Ki= 127.
    Ebrotidine
  • HY-B0310
    Nizatidine
    		Antagonist 99.68%
    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-101232
    Tiotidine
    		Antagonist 99.28%
    Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
    Tiotidine
  • 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-B0480
    Brompheniramine maleate
    		Antagonist 99.78%
    Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.
    Brompheniramine maleate
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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