2. Signaling Pathways
  3. GPCR/G Protein
    Immunology/Inflammation
    Neuronal Signaling
  4. Histamine Receptor
  5. H1 Receptor Isoform

H1 Receptor

 

H1 Receptor Related Products (138):

Cat. No. Product Name Effect Purity
  • HY-B0298A
    Clemastine fumarate
    		Antagonist 99.93%
    Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects.
  • HY-17043
    Loratadine
    		Agonist 99.98%
    Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
  • HY-12532
    Astemizole
    		Antagonist 99.77%
    Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects.
  • HY-B0539
    Desloratadine
    		Antagonist 99.88%
    Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (Ki=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria.
  • HY-B1193
    Terfenadine
    		Antagonist 99.91%
    Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
  • HY-17042B
    (S)-Cetirizine dihydrochloride
    		Antagonist
    (S)-Cetirizine dihydrochloride ((S)-P071) is an orally active antagonist of the histamine H1 receptor with a Ki value of 39.1 nM. (S)-Cetirizine dihydrochloride exerts anti-allergic activity by binding to the histamine H1 receptor and blocking the action of histamine. (S)-Cetirizine dihydrochloride is promising for research of allergic diseases such as allergic rhinitis.
  • HY-14517
    H3R antagonist 5
    		Agonist
    H3R antagonist 5 (Compound 1b) is a selective histamine H3 receptor inverse agonist with a IC50 of 0.54 nM and the ability to cross the blood-brain barrier. H3R antagonist 5 can be used in central nervous system-related research.
  • HY-170789
    H1R ligand-1
    		Ligand
    H1R ligand-1 (Compound fragment 1) is a high-affinity ligand for the human histamine H1 receptor (H1R). H1R ligand-1 can be used as a scaffold to design and synthesize a set of derivatives to explore H1R binding kinetics.
  • HY-B0527A
    Amitriptyline hydrochloride
    		Inhibitor 99.94%
    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.
  • HY-B0303A
    Diphenhydramine hydrochloride
    		Antagonist 99.98%
    Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB).
  • HY-107647
    (S)-(+)-Dimethindene maleate
    		Antagonist 99.80%
    (S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48).
  • HY-B0801A
    Fexofenadine hydrochloride
    		Antagonist 99.94%
    Fexofenadine (MDL-16455) hydrochloride is an orally active and nonsedative H1 receptor antagonist. Fexofenadine hydrochloride can be used in allergic rhinitis and chronic idiopathic urticarial research.
  • HY-B0674
    Ebastine
    		Antagonist 99.95%
    Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research.
  • HY-10791
    Ritanserin
    		Inhibitor 99.68%
    Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
  • HY-17042A
    Cetirizine dihydrochloride
    		Antagonist 99.58%
    Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-B0286A
    Chlorpheniramine maleate
    		Antagonist 99.67%
    Chlorpheniramine maleate is a histamine H1 receptor antagonist with an IC50 of 12 nM.
  • HY-B0157A
    Ketotifen fumarate
    		Inhibitor 99.88%
    Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.
  • HY-B0352
    Mirtazapine
    		Antagonist 99.94%
    Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
  • HY-B0781
    Promethazine hydrochloride
    		Antagonist 99.20%
    Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.
  • HY-B0801
    Fexofenadine
    		Antagonist 99.84%
    Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research.