A histamine H1 receptor antagonist (Ki = 0.001 µM); selective for histamine H1 over histamine H2 and H3 receptors (Kis = >100 µM for both)

Mizolastine – 1 g

Brand:
Cayman
CAS:
108612-45-9
Storage:
-20
UN-No:
Non-Hazardous - /

Mizolastine is a histamine H1 receptor antagonist (Ki = 0.001 µM).{54289} 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.  

 

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SKU: 9000566 - 1 g Category:

Description

A histamine H1 receptor antagonist (Ki = 0.001 µM); selective for histamine H1 over histamine H2 and H3 receptors (Kis = >100 µM for both), as well as 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); reduces histamine release from bronchial mast cells in ovalbumin-sensitized guinea pigs at 0.1, 0.3, and 1 mg/kg; 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); inhibits passive cutaneous anaphylaxis, as well as compound 48/80-induced lethal shock in rats (ED50s = 1.6 and 0.07 mg/kg, respectively)

Formal name: 2-[[1-[1-[(4-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-4-piperidinyl]methylamino]-4(3H)-pyrimidinone

Synonyms:  SL 850324

Molecular weight: 432.5

CAS: 108612-45-9

Purity: ≥98%

Formulation: A crystalline solid

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