Histamine Receptors

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  1. Histamine/cholinergic inhibitor

    Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.
  2. Histamine H1 receptor antagonist

    Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
  3. H1-receptor antagonist

    Tripelennamine hydrochloride, a H1-receptor antagonist, is a psychoactive drug and member of the pyridine andethylenediamine classes that is used as an antipruritic and first-generation antihistamine.
  4. H4 receptor antagonist

    JNJ-39758979 is histamine H4 receptor antagonists with a Ki of 12.5 nM.
  5. histamine H3 receptors agonist

    S38093 is an inverse agonist at histamine H3 receptors. CAS: 862896-30-8 (Free base) 1222097-72-4 (HCl)
  6. 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.
  7. 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.
  8. histamine H1 receptor antagonist

    Emedastine Difumarate is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. This medication is an antihistamine, prescribed for allergic conjunctivitis.
  9. 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.
  10. antihistamine

    Diphenylpyraline hydrochloride is a first-generation antihistamine with anticholinergic effects of the diphenylpiperidine class.
  11. Histamine H2-receptor antagonist

    Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion.
  12. Histamine 1 receptor antagonist

    Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.
  13. hemagglutinin (HA)-receptor antagonist

    Alimemazine hemitartrate is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.
  14. Lodoxamide Tromethamide is a mast-cell stabilizer, inhibiting type I immediate hypersensitivity reaction by preventing the antigen-stimulated calcium influx into mast cells and the release of slow-reacting substances of anaphylaxis (SRS-A).
  15. histamine H1-receptor antagonist

    Diazoline is a histamine H1-receptor antagonist.
  16. histamine H1 antagonist

    Chlorcyclizine hydrochloride is a histamine H1 antagonist.
  17. 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.
  18. 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.
  19. nonsedating H1 antagonist

    Rocastine is a selective, nonsedating H1 antagonist, acting as an antihistamine.
  20. histamine H1 receptor antagonist

    ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective ?? site (guinea pig brain) with Ki of 0.45 μM.
  21. H4R antagonist

    H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM.
  22. H3 receptor antagonist

    S 38093 is a brain-penetrant antagonist of H3 receptor, with Ki of 8.8, 1.44 and 1.2 ?M for rat, mouse and human H3 receptors, respectively.
  23. histamine H3 receptor antagonist

    Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity disorder.
  24. H1 receptor antagonist

    Wy 49051 is a potent, orally active H1 receptor antagonist, with IC50 of 44 nM.
  25. histamine H1 receptor antagonist

    Pirolate is a histamine H1 receptor antagonist.

  26. histamine H4 receptor agonist

    VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
  27. 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.
  28. histamine H2-receptor antagonist

    CP-66948 is a histamine H2-receptor antagonist with gastric antisecretory activity and mucosal protective properties.
  29. histamine H2 receptor antagonist

    BMY-25271 is a histamine H2 receptor antagonist.
  30. histamine 1 receptor antagonist

    Decloxizine(UCB-1402; NSC289116) is a histamine 1 receptor antagonist.
  31. histamine H4 receptor antagonist

    Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM.
  32. human H3 receptor antagonist

    Bavisant (JNJ-31001074) 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.
  33. histamine H3 receptor antagonist

    PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration.
  34. histamine H3 receptor antagonist

    PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration.
  35. 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.
  36. Alimemazine D6 is deuterium labeled Alimemazine, which is an antihistamine.
  37. LTC4 inhibitor

    Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  38. histamine H2-receptor antagonist

    Niperotidine is a histamine H2-receptor antagonist.
  39. 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.
  40. histamine H1 receptor antagonist

    Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM.
  41. histamine H3R antagonist/inverse agonist

    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR.
  42. histamine H1 receptor agonist and H3 receptor antagonist

    Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine. Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA).
  43. antagonist of histamine H1

    Cyclizine is an antagonist of histamine H1. Cyclizine is an antihistamine drug that can be used to treat nausea, vomiting and dizziness associated with motion sickness, vertigo and post-operatively following administration of general anaesthesia and opioids.

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