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

Histamine Receptor Antagonist

Histamine Receptor Antagonists (247):

Cat. No. Product Name Effect Purity
  • HY-B0298A
    Clemastine fumarate
    		Antagonist 99.97%
    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-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-12532
    Astemizole
    		Antagonist 99.62%
    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-30234S
    Clemizole-d4
    		Antagonist 99.82%
    Clemizole-d4 is a deuterium labeled Clemizole. Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication.
  • HY-17610A
    Enerisant hydrochloride
    		Antagonist
    Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively.
  • HY-B0640AR
    Epinastine hydrochloride (Standard)
    		Antagonist
    Epinastine (hydrochloride) (Standard) is the analytical standard of Epinastine (hydrochloride). This product is intended for research and analytical applications. Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action.
  • HY-B0539
    Desloratadine
    		Antagonist 99.83%
    Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities.
  • 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-B0725
    Doxepin Hydrochloride
    		Antagonist 99.79%
    Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant.
    . Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system.
    . Doxepin has also been proposed as a protective factor against oxidative stress.
    .
  • HY-B0377
    Famotidine
    		Antagonist 99.68%
    Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
  • HY-A0077
    Perphenazine
    		Antagonist 99.95%
    Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.
  • HY-B0801A
    Fexofenadine hydrochloride
    		Antagonist 99.86%
    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-B0781
    Promethazine hydrochloride
    		Antagonist ≥98.0%
    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-107647
    (S)-(+)-Dimethindene maleate
    		Antagonist 99.94%
    (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-B0286A
    Chlorpheniramine maleate
    		Antagonist 99.90%
    Chlorpheniramine maleate is a histamine H1 receptor antagonist with an IC50 of 12 nM.
  • 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-13508
    JNJ-7777120
    		Antagonist 99.85%
    JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory.
  • HY-B0674
    Ebastine
    		Antagonist 99.67%
    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-17042A
    Cetirizine dihydrochloride
    		Antagonist 99.53%
    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-B0281A
    Ranitidine hydrochloride
    		Antagonist 99.88%
    Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9.