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

H1 Receptor Antagonist

H1 Receptor Antagonists (51):

Cat. No. Product Name Effect Purity
  • HY-B0298A
    Clemastine fumarate
    Antagonist 99.95%
    Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist.
  • HY-B1193
    Antagonist 99.91%
    Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM.
  • HY-12532
    Antagonist 99.62%
    Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM.
  • HY-B0801A
    Fexofenadine hydrochloride
    Antagonist 99.70%
    Fexofenadine (MDL-16455) hydrochloride is an orally active and nonsedative H1 receptor antagonist.
  • HY-148825
    NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration.
  • HY-B0539
    Antagonist 99.83%
    Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine.
  • HY-B0725
    Doxepin Hydrochloride
    Antagonist 99.84%
    Doxepin hydrochloride is an orally active tricyclic antidepressant agent.
  • HY-B0781
    Promethazine hydrochloride
    Antagonist ≥98.0%
    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-B0303A
    Diphenhydramine hydrochloride
    Antagonist 99.90%
    Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect.
  • HY-B0352
    Antagonist 99.08%
    Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent.
  • HY-B0674
    Antagonist 99.54%
    Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist.
  • HY-13511A
    Rupatadine Fumarate
    Antagonist 98.77%
    Rupatadine (UR-12592) Fumarate is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively.
  • HY-B0462
    Azelastine hydrochloride
    Antagonist 99.93%
    Azelastine hydrochloridem, an antihistamine, is a potent and selective histamine 1 (H1) antagonist.
  • HY-B0274
    Antagonist 99.13%
    Chlorprothixene is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively.
  • HY-123205
    Antagonist 99.47%
    Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity.
  • HY-10121
    Antagonist 99.93%
    Asenapine (Org 5222), 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).
  • HY-107647
    (S)-(+)-Dimethindene maleate
    Antagonist 99.94%
    (S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78).
  • HY-B0274A
    Chlorprothixene hydrochloride
    Antagonist ≥98.0%
    Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively.
  • HY-121356
    Antagonist 99.12%
    Carebastine is the active metabolite of Ebastine.
  • HY-101232
    Antagonist 99.28%
    Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium).