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-B1483
    Methapyrilene hydrochloride
    		Antagonist 99.88%
    Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo
    Methapyrilene hydrochloride
  • HY-B0801S
    Fexofenadine-d6
    		Inhibitor 99.28%
    Fexofenadine-d6 is deuterium labeled Fexofenadine, which is an antihistamine pharmaceutical agent.
    Fexofenadine-d<sub>6</sub>
  • HY-120124
    Samelisant
    		Antagonist 98.65%
    Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders.
    Samelisant
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride
    		Inhibitor 99.65%
    Amitriptyline-d6 (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
    Amitriptyline-d<sub>6</sub> hydrochloride
  • HY-101189
    JNJ-39758979
    		Antagonist 99.71%
    JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.
    JNJ-39758979
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    		Inhibitor 99.03%
    Amitriptyline (hydrochloride) (Standard) is the analytical standard of Amitriptyline (hydrochloride). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
    Amitriptyline hydrochloride (Standard)
  • HY-147276
    Izuforant
    		Antagonist 98.88%
    Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC50 of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC50 of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies.
    Izuforant
  • HY-127167
    3',4'-Dihydroxyflavone
    		98.61%
    3',4'-Dihydroxyflavone is a flavonoid. 3',4'-Dihydroxyflavone has antiallergic activity with an IC50 value of 30 μM. 3',4'-Dihydroxyflavone can be used for the research of type I allergy.
    3',4'-Dihydroxyflavone
  • HY-12752A
    Alimemazine hemitartrate
    		Agonist 98.44%
    Alimemazine hemitartrate (Trimeprazine hemitartrate) is an antagonist of the histamine (HA) receptor that can be taken orally and also acts as a partial agonist at other GPCR receptors. Alimemazine hemitartrate has effects that include anti-serotonin, antispasmodic, antihistamine, sedation, hypnotic, antiviral, and anti-nausea properties. Alimemazine hemitartrate promotes the growth of pancreatic β-cells in mice and improves diabetes in mice.
    Alimemazine hemitartrate
  • HY-P2636
    Cholecystokinin Precursor (24-32) (rat)
    		99.54%
    Cholecystokinin Precursor (24-32) (rat) is a cholecystokinin precursor that can be expressed in the heart, lungs, and kidneys as well as in the gastrointestinal tract and brain. Cholecystokinin is a brain-gut peptide that stimulates gallbladder contraction and pancreatic exocrine secretion and also acts as a neurotransmitter.
    Cholecystokinin Precursor (24-32) (rat)
  • HY-15539
    Niperotidine
    		Antagonist 98.49%
    Niperotidine is a histamine H2-receptor antagonist.
    Niperotidine
  • HY-B1101A
    Pimethixene maleate
    		Antagonist 99.94%
    Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
    Pimethixene maleate
  • HY-N7503
    Psoralenoside
    		Inhibitor 99.84%
    Psoralenoside is a benzofuran glycoside from Psoralea corylifolia. Psoralenoside exhibits high binding affinities against histaminergic H1, calmodulin, and voltage-gated L-type calcium channels (E-value≥-6.5 Kcal/mol). Psoralenoside shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.
    Psoralenoside
  • HY-109544
    Repirinast
    		Inhibitor
    Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma.
    Repirinast
  • HY-B0160
    Lafutidine
    		Antagonist 99.95%
    Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H2RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease.
    Lafutidine
  • HY-B0548
    Hydroxyzine
    		Antagonist 99.72%
    Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder.
    Hydroxyzine
  • HY-B0170A
    Azatadine dimaleate
    		Inhibitor 99.85%
    Azatadine dimaleate is an histamine and cholinergic inhibitor with IC50 of 6.
    Azatadine dimaleate
  • HY-19489S
    (±)-Levomepromazine-d6
    		Antagonist 99.23%
    (±)-Levomepromazine-d6 is the deuterium labeled Methotrimeprazine, which is a D3 dopamine and Histamine H1 receptor antagonist.
    (±)-Levomepromazine-d<sub>6</sub>
  • HY-13511
    Rupatadine
    		Antagonist 99.70%
    Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria.
    Rupatadine
  • HY-109074
    Seliforant
    		Antagonist
    Seliforant (SENS-111) is a selective and orally histamine H4 receptor antagonist.
    Seliforant
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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