Histamine Receptors

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  1. Decloxizine

    Catalog No. A20964
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    histamine 1 receptor antagonist
    Decloxizine(UCB-1402; NSC289116) is a histamine 1 receptor antagonist. Learn More
  2. H4 Receptor antagonist 1

    Catalog No. A18929
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    histamine H4 receptor inverse agonist
    H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM. Learn More
  3. Chlorcyclizine hydrochloride

    Catalog No. A18025
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    histamine H1 antagonist
    Chlorcyclizine hydrochloride is a histamine H1 antagonist. Learn More
  4. Toreforant

    Catalog No. A21058
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    histamine H4 receptor (H4R) antagonist
    Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM. Learn More
  5. PF-03654746

    Catalog No. A21429
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    histamine H3 receptor antagonist
    PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration. Learn More
  6. PF-03654746 Tosylate

    Catalog No. A21434
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    histamine H3 receptor antagonist
    PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. Learn More
  7. JNJ-5207852

    Catalog No. A21480
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    histamine H3 receptor antagonist
    JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively. Learn More
  8. Niperotidine

    Catalog No. A21981
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    histamine H2-receptor antagonist
    Niperotidine is a histamine H2-receptor antagonist. Learn More
  9. GSK189254A

    Catalog No. A22005
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    histamine H3 receptor antagonist
    GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively. Learn More
  10. Buclizine HCl

    Catalog No. A15666
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    Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family. Learn More
  11. 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
  12. 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
  13. 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
  14. 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
  15. 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
  16. Zaltidine

    Catalog No. A15285
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    H2-receptor antagonist
    Zaltidine is a H2-receptor antagonist, which has the antisecretory action. Learn More
  17. 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
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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
  23. Mequitazine

    Catalog No. A18206
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    Histamine H1 antagonist
    Mequitazine is a potent histamine H1 antagonist or antihistamine. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. Learn More
  24. Mebhydrolin napadisylate

    Catalog No. A17997
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    histamine H1-receptor antagonist
    Diazoline is a histamine H1-receptor antagonist. Learn More
  25. Acrivastine

    Catalog No. A17746
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    Histamine 1 receptor antagonist
    Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis. Learn More
  26. Diphenylpyraline hydrochloride

    Catalog No. A17717
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    antihistamine
    Diphenylpyraline hydrochloride is a first-generation antihistamine with anticholinergic effects of the diphenylpiperidine class. Learn More
  27. Hydroxyzine pamoate

    Catalog No. A17712
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    Histamine H1 receptor antagonist
    Hydroxyzine pamoate is an histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. Learn More
  28. Levocetirizine Dihydrochloride

    Catalog No. A17440
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    Histamine H1 receptor antagonist
    Levocetirizine dihydrochloride is a L-isomer of cetirizine and histamine H1 receptor antagonist. It incrases levels of CD4+ CD25+ T cells and decreases levels of eosinophils, decreasing allergy symptoms. Learn More
  29. Terfenadine

    Catalog No. A17373
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    H1 histamine receptor antagonist
    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 and induces p73, Noxa. Learn More
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. Bepotastine Besilate

    Catalog No. A11340
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    Histamine Receptor antagonist
    Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist. 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. 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
  38. 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
  39. 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
  40. 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
  41. Orphenadrine citrate

    Catalog No. A11712
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    NMDA receptor antagonist
    Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker. Learn More
  42. Cyproheptadine hydrochloride

    Catalog No. A11709
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    Cyproheptadine hydrochloride is a histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM. Learn More
  43. Ciproxifan

    Catalog No. A11360
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    Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist. Learn More
  44. 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
  45. 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
  46. 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
  47. 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
  48. 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
  49. 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
  50. 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

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