Histamine Receptors

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  1. Cyclizine 2HCl

    Catalog No. A16472
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    Histamine H1 receptor antagonist
    Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity. Learn More
  2. Ebrotidine

    Catalog No. A15075
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    H2-receptor antagonist
    Ebrotidine is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection. Learn More
  3. Clemizole hydrochloride

    Catalog No. A15047
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    H1 histamine receptor antagonist
    Clemizole hydrochloride is an antagonist of H1 histamine receptor with an IC50 value of 8 mM for NS4B RNA binding. Learn More
  4. Cetirizine

    Catalog No. A15041
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    H1-receptor antagonist
    Cetirizine, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. Learn More
  5. Ebastine

    Catalog No. A14946
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    H1-histamine receptor antagonist
    Ebastine is a H1 antihistamine with low potential for causing drowsiness. Learn More
  6. A 943931 2HCl

    Catalog No. A13442
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    Histamine H4 receptor antagonist
    A 943931 2HCl is a potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively). Learn More
  7. Immethridine hydrobromide

    Catalog No. A13641
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    histamine H3 receptor agonist
    Immethridine hydrobromide is a strong and highly selective histamine H3 receptor agonist (pEC50 = 9.74) that displays 300-fold selectivity over the H4 receptor (pKi values are 9.07 and 6.61 respectively). Learn More
  8. Astemizole

    Catalog No. A13899
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    H1-receptor antagonist
    Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels. Learn More
  9. Promethazine HCl

    Catalog No. A14248
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    Histamine H1 receptor antagonist
    Promethazine HCl is a potent histamine H1 receptor antagonist. Learn More
  10. JNJ7777120

    Catalog No. A12713
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    Histamine Antagonist
    JNJ7777120 is a potent, selective non-imidazole H4?histamine receptor antagonist. Learn More
  11. Pitolisant hydrochloride

    Catalog No. A15213
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    Nonimidazole inverse agonist
    Pitolisant hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). Learn More
  12. Pitolisant oxalate

    Catalog No. A15214
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    Nonimidazole inverse agonist
    Pitolisant oxalate is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). Learn More
  13. Zaltidine

    Catalog No. A15285
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    H2-receptor antagonist
    Zaltidine is a H2-receptor antagonist, which has the antisecretory action. Learn More
  14. Azatadine dimaleate

    Catalog No. A16418
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    Histamine/cholinergic inhibitor
    Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. Learn More
  15. Antazoline HCl

    Catalog No. A16411
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    Histamine H1 receptor inhibitor
    Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine. Learn More
  16. Alcaftadine

    Catalog No. A16393
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    H1 histamine receptor antagonist
    Alcaftadine is a high affinity ligand for the H1 receptor, with a pKi (8.5) that is comparable with that of other H1 antihistamines. Alcaftadine is also an antagonist for H2 and H4 receptors with no affinity for the H3 receptor. Learn More
  17. Buclizine HCl

    Catalog No. A15666
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    Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family. Learn More
  18. Cyproheptadine hydrochloride

    Catalog No. A16169
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    serotonin/histamine2 antagonist
    Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2. Learn More
  19. Lidocaine hydrochloride

    Catalog No. A16132
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    Histamine H1-receptor agonist
    Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent. Learn More
  20. CarbinoxaMine Maleate

    Catalog No. A16129
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    histamine-H1 receptor blocking agent
    Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties. Learn More
  21. Bavisant dihydrochloride hydrate

    Catalog No. A15016
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    H3 receptor antagonist
    Bavisant dihydrochloride hydrate is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. Learn More
  22. Bavisant dihydrochloride

    Catalog No. A15015
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    H3 receptor antagonist
    Bavisant dihydrochloride is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. Learn More
  23. Metiamide

    Catalog No. A13086
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    Histamine H2-receptor antagonist
    Metiamide is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate compound in the development of the successful anti-ulcer drug cimetidine. Learn More
  24. Clemizole

    Catalog No. A13073
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    H1 histamine receptor antagonist.
    Clemizole is an H1 histamine receptor antagonist. Learn More
  25. Asenapine maleate

    Catalog No. A10091
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    H1 antagonist
    Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors. Learn More
  26. Mizolastine

    Catalog No. A11724
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    Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H1 receptors. Learn More
  27. Lafutidine

    Catalog No. A11714
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    H2 receptor antagonist
    Lafutidine is a second generation H2 receptor antagonist having multimodal mechanism of action. Learn More
  28. Orphenadrine citrate

    Catalog No. A11712
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    Orphenadrine is known to have the following pharmacology: mACh receptor antagonist (anticholinergic); H1 receptor antagonist (antihistamine); NMDA receptor antagonist; NET blocker (norepinephrine reuptake inhibitor); Nav1.7, Nav1.8, and Nav1.9 sodium channel blocker; HERG potassium channel blocker. Learn More
  29. Cyproheptadine hydrochloride

    Catalog No. A11709
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  30. Ciproxifan

    Catalog No. A11360
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    Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist. Learn More
  31. Clemastine fumarate

    Catalog No. A10226
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    Histamine Receptor antagonis
    Clemastine is a selective histamine H1 antagonist. It binds to the histamine H1 receptor, thus blocking the action of endogenous histamine, which leads to temporary relief of the negative symptoms caused by histamine. Learn More
  32. Brompheniramine

    Catalog No. A11699
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    Brompheniramine is a first-generation antihistamine. Brompheniramine works by acting as an antagonist of histamine H1 receptors. It also functions as a moderately effective anticholinergic agent, and is likely an antimuscarinic agent similar to other common antihistamines such as diphenhydramine. Learn More
  33. Azelastine HCl (Allergodil)

    Catalog No. A10117
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    Azelastine is a potent, second-generation, selective, histamine antagonist (histamine-H1-receptor antagonist). Learn More
  34. Cetirizine Dihydrochloride

    Catalog No. A10195
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    Cetirizine is a second-generation antihistamine, a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. Learn More
  35. Chlorpheniramine maleate

    Catalog No. A10205
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    Chlorpheniramine maleate is a first-generation alkylamine antihistamine used in the prevention of the symptoms of allergic conditions such as rhinitis and urticaria. Learn More
  36. Cimetidine

    Catalog No. A10218
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    H2-receptor antagonist
    Cimetidine is a histamine H2-receptor antagonist that inhibits stomach acid production. Learn More
  37. Olopatadine hydrochloride

    Catalog No. A10671
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    Olopatadine hydrochloride is a dual acting histamine H1-receptor antagonist and mast cell stabilizer Learn More
  38. Bepotastine

    Catalog No. A12845
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    Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. Learn More
  39. Bilastine

    Catalog No. A12661
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    Bilastine is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria. Learn More
  40. Fexofenadine HCl

    Catalog No. A11859
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    COX inhibitor/histamine H1 receptor agonist
    Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist Learn More
  41. Loratadine

    Catalog No. A10538
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    Loratadine is a non-sedative antihistamine that inhibits histamine-induced activities of IL-6 and IL-8 secretion in endothelial cells. Loratadine is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Learn More
  42. Rupatadine

    Catalog No. A11222
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    PAFR inhibitor/H1 receptor inhibitor
    Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. Learn More
  43. Rupatadine Fumarate

    Catalog No. A12356
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    PAFR inhibitor/H1 receptor inhibitor
    Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. Learn More
  44. Roxatidine acetate hydrochloride

    Catalog No. A11921
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    Roxatidine Acetate Hydrochloride is a histamine H2-receptor antagonist used in ulcer treatment. This compound has been found to inhibit platelet function in vitro. Learn More
  45. Bepotastine Besilate

    Catalog No. A11340
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    Histamine Receptor antagonist
    Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist. Learn More
  46. Ciproxifan maleate

    Catalog No. A11117
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    H3-receptor antagonist
    Ciproxifan maleate is a potent, selective H3 histamine receptor antagonist. Learn More

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