Mizolastine

Mizolastine is a histamine H1 receptor antagonist (Ki = 0.001 µM). 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, alpha1- and alpha2-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 (Cay-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.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: (Request formulation change), A crystalline solid. Solubility: Chloroform: 10 mg/ml, DMF: slightly soluble, DMSO: slightly soluble. lambdamax: 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.