6221. Mizolastine

Nomenclature

CAS number: 108612-45-9
2-[[1-[1-[(4-Fluorophenyl)methyl]-1H-benzimidazol-2-yl]-4-piperidinyl]methylamino]-4(1H)-pyrimidinone; 2-[[1-[1-(p-fluorobenzyl)-2-benzimidazolyl]-4-piperidinyl]methylamino]-4(3H)-pyrimidinone; SL-85.0324; Mizollen (Lorex); Zolim (Schwarz).
C24H25FN6O; mol wt 432.49.
C 66.65%, H 5.83%, F 4.39%, N 19.43%, O 3.70%.

Description and references

Nonsedating-type histamine H1-receptor antagonist. Prepn: JP Kokai 87 61979; P. Manoury et al., US 4912219 (1987, 1990 both to Synthelabo). Receptor binding study: J. Benavides et al., Arzneim.-Forsch. 45, 551 (1995). HPLC determn in plasma: V. Ascalone et al., J. Chromatogr. 619, 275 (1993). Clinical pharmacokinetics: P. Rosenzweig et al., Ann. Allergy 69, 135 (1992). Effect on psychomotor performance: J. S. Kerr et al., Eur. J. Clin. Pharmacol. 47, 331 (1994). Clinical trial in allergic rhinitis: F. Leynadier et al., Ann. Allergy Asthma Immunol. 76, 163 (1996).

Chemical structure

Properties

Crystals from ethanol, mp 217°. Sol in methanol.

Therapeutic Category

Antihistaminic.

Keywords

Antihistaminic