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

H1 Receptor Inhibitor

H1 Receptor Inhibitors (25):

Cat. No. Product Name Effect Purity
  • 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-B0188A
    Mianserin hydrochloride
    		Inhibitor 99.95%
    Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy.
  • HY-B0157
    Ketotifen
    		Inhibitor 99.94%
    Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.
  • 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-A0069
    Doxylamine succinate
    		Inhibitor 99.76%
    Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia.
  • HY-B0188
    Mianserin
    		Inhibitor 99.42%
    Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy.
  • HY-B1215
    Dimenhydrinate
    		Inhibitor 99.89%
    Dimenhydrinate is an orally active H1-antihistamine consisting of Diphenhydramine (HY-B0303) and 8-Chlorotheophylline. Dimenhydrinate is used to prevent nausea, vomiting, dizziness, and vertigo associated with motion sickness.
  • HY-B1483
    Methapyrilene hydrochloride
    		Inhibitor 99.88%
    Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • HY-B0157AS
    Ketotifen-d3 fumarate
    		Inhibitor 99.23%
    Ketotifen-d3 (fumarate) is the deuterium labeled Ketotifen fumarate. Ketotifen (HC 20511) fumarate is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks.
  • HY-B0349A
    Meclizine
    		Inhibitor
    Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease.
  • HY-B0349B
    Meclizine dihydrochloride monohydrate
    		Inhibitor
    Meclizine (Meclozine) dihydrochloride monohydrate, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease.
  • HY-17042AS
    Cetirizine-d4 dihydrochloride
    		Inhibitor
    Cetirizine-d4 (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-A0069AS
    Doxylamine-d5
    		Inhibitor
    Doxylamine-d5 is deuterium labeled Doxylamine (HY-A0069A). Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia.
  • HY-182439
    AZD3778
    		Inhibitor
    AZD3778 (Compound 8) is an inhibitor of CCR3 and histamine H1 receptor (histamine H1 receptor), with IC50 values of 8.1 nM and 40 nM, respectively. AZD3778 inhibits the binding of eosinophil chemokines to CCR3, as well as the binding of histamine to histamine H1 receptor. AZD3778 exhibits anti-eosinophilic activity. AZD3778 alleviates symptoms associated with allergic rhinitis. AZD3778 can be used in research related to allergic rhinitis and asthma.