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

H1 Receptor

 

H1 Receptor Related Products (152):

Cat. No. Product Name Effect Purity
  • HY-A0027AS
    Fenspiride-d5
    		Antagonist
    Fenspiride-d5 is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
  • HY-B1397B
    Cyclizine lactate
    		Antagonist
    Cyclizine lactate, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine lactate can be used for the research of nausea, vomiting, and dizziness.
  • HY-B0548AS1
    Hydroxyzine-d4 dihydrochloride
    		Antagonist 98.0%
    Hydroxyzine-d4 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder.
  • HY-10121B
    Asenapine citrate
    		Antagonist
    Asenapine citrate, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine citrate can be used in the research of schizophrenia and bipolar disorder.
  • HY-B0674S
    Ebastine-d5
    		Antagonist
    Ebastine-d5 is the deuterium labeled Ebastine. 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-B0971A
    Pheniramine
    		Antagonist
    Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects.
  • 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-107567
    Carcinine
    		Antagonist
    Carcinine (β-Alanylhistamine) is a selective and orally active histamine H3 receptor antagonist with a Ki of 0.2939 μM. Carcinine can reduce histamine content. Carcinine exhibits anti-oxidant activity and neuroprotective effects. Carcinine shows positive inotropic effect and can reduce blood sugar and blood lipid levels. Carcinine can be used for the researches of inflammation, neurological, cardiovascular and metabolic disease, such as retinal damage, seizure and diabetes.
  • HY-A0027A
    Fenspiride
    		Antagonist
    Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
  • HY-106957
    Efletirizine
    		Antagonist
    Efletirizine (EFZ) is an orally active antihistamine with high selectivity and affinity to the H1-receptor. Efletirizine can be used for allergic disease research.
  • HY-119995
    Chloropyramine
    		Antagonist
    Chloropyramine is competitive reversible H1 receptor antagonist. Chloropyramine also has anti-tumour activity in breast cancer. Chloropyramine can be used for the research of allergic conditions, such as conjunctivitis and bronchial asthma.
  • 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-A0069A
    Doxylamine
    		Antagonist
    Doxylamine, a first generation antihistamine, is a histamine (H1) receptor antagonist. Doxylamine is also a local analgesic agent and effective hypnotic agent.
  • HY-17042AS1
    Cetirizine-d8 dihydrochloride
    		Antagonist
    Cetirizine-d8 (dihydrochloride) is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-167897
    UR-AK49
    		Agonist
    UR-AK49 (compound 11) is a human histamine H1 and H2 receptor agonist. UR-AK49 has an EC50 of 23 nM in a GTPase assay with hH2R-Gsalpha fusion protein expressed in Sf9 insect cells. UR-AK49 can be used in neuro-related research.
  • HY-B2178
    Emedastine difumarate
    		Agonist
    Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
  • HY-B0164S
    Mizolastine-13C,d3
    		Antagonist
    Mizolastine-13C,d3 is the 13C- and deuterium labeled Mizolastine.
  • HY-B0781S
    Promethazine-d4 hydrochloride
    		Antagonist 98.0%
    Promethazine-d4 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
  • HY-B0548S1
    Hydroxyzine-d8
    		Antagonist 99.0%
    Hydroxyzine-d8 is deuterium labeled Hydroxyzine. Hydroxyzine is a histamine H1-receptor antagonist.
  • 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.