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-16289
    Lodoxamide tromethamine
    		Inhibitor 99.83%
    Lodoxamide tromethamine (U-42585E) is a medication for the treatment of prophylaxis of mast cell-mediated allergic disease.
    Lodoxamide tromethamine
  • HY-P991252
    XmAb-7195
    		Inhibitor 99.98%
    XmAb-7195 (AIMab-7195) is a human monoclonal antibody (mAb) targeting IGHE. XmAb-7195 can be used in Food hypersensitivity, Allergic asthma, Allergic rhinitis, Atopic dermatitis and Conjunctivitis research.
    XmAb-7195
  • HY-B1510
    Acrivastine
    		Inhibitor 99.86%
    Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.
    Acrivastine
  • HY-B1067
    Antazoline hydrochloride
    		Inhibitor 99.60%
    Antazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV.
    Antazoline hydrochloride
  • HY-12394
    Dothiepin
    		Inhibitor 98.50%
    Dothiepin (Dosulepin; Dothep) is an antidepressant agent with sedative/anxiolytic activity. Dothiepin is an inhibitor preferring of noradrenaline uptake than serotonin uptake. Dothiepin facilitates noradrenergic neurotransmission via inhibiting the neuronal uptake. Dothiepin is also an antagonist of histamine H1-receptor without cardiotoxicity. Dothiepin exhibits significant analgesic activity in psychogenic facial pain，idiopathic fibromyalgia syndrome or rheumatoid arthritis.
    Dothiepin
  • HY-B0971
    Pheniramine maleate
    		Inhibitor 99.94%
    Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects.
    Pheniramine maleate
  • HY-B1165
    Cyproheptadine (hydrochloride sesquihydrate)
    		Inhibitor 99.74%
    Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.
    Cyproheptadine (hydrochloride sesquihydrate)
  • 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-U00027
    Quinotolast sodium
    		Inhibitor 98.38%
    Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.
    Quinotolast sodium
  • HY-B0520
    Benztropine
    		Inhibitor 98.12%
    Benztropine (Benzatropine; Benzotropine) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
    Benztropine
  • HY-B0170A
    Azatadine dimaleate
    		Inhibitor 99.85%
    Azatadine dimaleate (Azatadine maleate) is an orally active histamine H1 receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine dimaleate induces sedation and exhibits topical anesthetic properties. Azatadine dimaleate can be used for the research of allergic rhinitis.
    Azatadine dimaleate
  • HY-A0128A
    Buclizine dihydrochloride
    		Inhibitor 99.62%
    Buclizine dihydrochloride is an orally active antihistamine antiallergic compound. Buclizine dihydrochloride is a potent teratogen in the rat and shows anti-tumor activity.
    Buclizine dihydrochloride
  • HY-117046A
    AVN-101 hydrochloride
    		Inhibitor 99.59%
    AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.
    AVN-101 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-N8593
    Undecane
    		Inhibitor 99.66%
    Undecane is a potent cAMP agonist with anti-allergic and anti-inflammatory activities. Undecane inhibits degranulation and the secretion of histamine and TNF-α. Undecane reverses the increased levels of p38 phosphorylation, NF-κB transcriptional activity and target cytokine/chemokine genes, including thymus and activation-regulated chemokine (TARC), macrophage-derived chemokine (MDC) and interleukin-8 (IL-8). Undecane can be used for the study of skin inflammatory disorders, such as atopic dermatitis.
    Undecane
  • HY-B1895
    Levodropropizine
    		Inhibitor 99.89%
    Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.
    Levodropropizine
  • HY-100238
    Antihistamine-1
    		Inhibitor 99.08%
    Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
    Antihistamine-1
  • HY-121422
    JZP-361
    		Inhibitor 99.63%
    JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research.
    JZP-361
  • HY-B0801S
    Fexofenadine-d6
    		Inhibitor 99.28%
    Fexofenadine-d6 (MDL-16455-d6) is deuterium labeled Fexofenadine, which is an antihistamine pharmaceutical agent.
    Fexofenadine-d<sub>6</sub>
  • HY-13405
    Tiaramide hydrochloride
    		Inhibitor 98.70%
    Tiaramide (RHC 2592-A) hydrochloride is an analgesic agent with antiallergic activity, and is also a non-steroidal, anti-inflammatory compound. Tiaramide hydrochloride inhibits histamine release.
    Tiaramide hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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