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

Histamine Receptor Antagonist

Histamine Receptor Antagonists (240):

Cat. No. Product Name Effect Purity
  • HY-B0527
    Amitriptyline
    		Antagonist 99.94%
    Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
  • HY-12537
    Peptide 401
    		Antagonist 98.26%
    Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT).
  • HY-B1296
    Promethazine
    		Antagonist 99.67%
    Promethazine is an orally active histamine receptor antagonist. Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects.
  • HY-B0478A
    Trazodone
    		Antagonist 99.84%
    Trazodone (AF-1161 free base) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone has anti-depressant and anti-insomnious activity. Trazodone exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects.
  • HY-B1693
    Levomepromazine
    		Antagonist 99.98%
    Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting.
  • HY-19705B
    Adriforant hydrochloride
    		Antagonist ≥98.0%
    Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
  • HY-B0478
    Trazodone hydrochloride
    		Antagonist 99.60%
    Trazodone hydrochloride (AF-1161) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone hydrochloride has anti-depressant and anti-insomnious activity. Trazodone hydrochloride exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects.
  • 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.
  • HY-B0286
    Chlorpheniramine
    		Antagonist 99.86%
    Chlorpheniramine is a H1 antihistamines commonly used in allergic diseases research.
  • 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.
  • HY-B2168
    Mequitazine
    		Antagonist 99.99%
    Mequitazine is a potent, and long-acting histamine H1 antagonist.
  • 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.
  • HY-B1303A
    Mebhydrolin
    		Antagonist 99.78%
    Mebhydrolin is a specific histamine H1 receptor antagonist.
  • HY-15538
    Ebrotidine
    		Antagonist 98.51%
    Ebrotidine(FI 3542) is a competitive H2-receptor antagonist (Ki= 127.
  • HY-17610
    Enerisant
    		Antagonist 99.79%
    Enerisant (TS-091) 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-B0527AS
    Amitriptyline-d6 hydrochloride
    		Antagonist 99.65%
    Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
  • HY-B0160
    Lafutidine
    		Antagonist 99.56%
    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.
  • HY-111130
    Methapyrilene
    		Antagonist 99.66%
    Methapyrilene is a histamine antagonist, a pyridine chemical with anticholinergic activity. Methapyrilene can cause target organ-specific epigenetic alterations, such as a decrease in DNA methylation levels. Methapyrilene induces hepatocellular carcinoma in rats.
  • HY-W010841R
    Levocetirizine dihydrochloride (Standard)
    		Antagonist
    Levocetirizine (dihydrochloride) (Standard) is the analytical standard of Levocetirizine (dihydrochloride). This product is intended for research and analytical applications. Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.
  • 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.