A histamine H1 receptor antagonist
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Mizolastine

Item No. 9000566

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[1-[1-[(4-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-4-piperidinyl]methylamino]-4(3H)-pyrimidinone
CAS Number
108612-45-9
Synonyms
  • SL 850324
Molecular Formula
C24H25FN6O
Formula Weight
432.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 10 mg/mlDMF: slightly solubleDMSO: slightly soluble
λmax
217, 289 nm
SMILES
FC(C=C1)=CC=C1CN2C(N3CCC(N(C)C(N4)=NC=CC4=O)CC3)=NC5=CC=CC=C52FC(C=C1)=CC=C1CN2C(N3CCC(N(C)C(N4)=NC=CC4=O)CC3)=NC5=CC=CC=C52
InChi Code
InChI=1S/C24H25FN6O/c1-29(23-26-13-10-22(32)28-23)19-11-14-30(15-12-19)24-27-20-4-2-3-5-21(20)31(24)16-17-6-8-18(25)9-7-17/h2-10,13,19H,11-12,14-16H2,1H3,(H,26,28,32)
InChi Key
PVLJETXTTWAYEW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    250 mg

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    Cayman Chemical
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    Product Description

    Mizolastine is a histamine H1 receptor antagonist (Ki = 0.001 µM).1 It is selective for histamine H1 over histamine H2 and H3 receptors (Kis = >100 µM for both), as well as the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D, 5-HT2, and 5-HT3, dopamine D1 and D2, α1- and α2-adrenergic, adenosine, and muscarinic receptors in radioligand binding assays (Kis = >1 µM for all). Mizolastine (0.1, 0.3, and 1 mg/kg) reduces histamine release from bronchial mast cells in ovalbumin-sensitized guinea pigs. It reduces histamine-induced paw edema in rats, skin edema in dogs, and bronchoconstriction in guinea pigs (ED50s = 0.5, 0.07, and 0.03 mg/kg, respectively). Mizolastine also inhibits passive cutaneous anaphylaxis, as well as lethal shock induced by compound 48/80 (Item No. 22173) in rats (ED50s = 1.6 and 0.07 mg/kg, respectively). Formulations containing mizolastine have been used in the treatment of allergic rhinitis and urticaria.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Selve, N., Pichat, P., Goldhill, J., et al. Pharmacological profile of mizolastine, a novel histamine H1 receptor antagonist. Mast cells and basophils 625-640 (2000).