Title: Oxatomide
CAS Registry Number: 60607-34-3
CAS Name: 1-[3-[4-(Diphenylmethyl)-1-piperazinyl]propyl]-1,3-dihydro-2H-benzimidazol-2-one
Additional Names: 1-[3-[4-(diphenylmethyl)-1-piperazinyl]propyl]-2-benzimidazolinone
Manufacturers' Codes: R-35443
Trademarks: Celtect (Kyowa); Cobiona (Esteve); Dasten (Duncan); Tinset (Janssen)
Molecular Formula: C27H30N4O
Molecular Weight: 426.55
Percent Composition: C 76.03%, H 7.09%, N 13.13%, O 3.75%
Literature References: Orally active anti-allergic agent, related structurally to cinnarizine, q.v., and having a novel biphasic mode of action. Prepn: J. Vandenberk et al., DE 2714437; eidem, US 4250176 (1977, 1981 both to Janssen). Inhibition of release and effects of allergic mediators: F. Awouters et al., Experientia 33, 1657 (1977). In vitro study of inhibition and stimulation of histamine release: M. K. Church et al., Agents Actions 10, 4 (1980). In vivo study: S. Gatti et al., Br. J. Dermatol. 103, 671 (1980). Clinical studies: S. W. Barham, F. Moran, Br. J. Clin. Pract. 34, 323 (1980); E. F. Juniper et al., Clin. Allergy 11, 61 (1981); W. Peremans et al., Dermatologia 162, 42 (1981). Review of pharmacological and clinical studies: D. M. Richards et al., Drugs 27, 210 (1984).
Properties: White powder, mp 153.6°. LD50 in guinea pigs, mice, rats (mg/kg): 320, >2560, >2560 orally; 23, 27, 30 i.v. (Richards).
Melting point: mp 153.6°
Toxicity data: LD50 in guinea pigs, mice, rats (mg/kg): 320, >2560, >2560 orally; 23, 27, 30 i.v. (Richards)
Therap-Cat: Antiallergic; antiasthmatic.
Keywords: Antiallergic; Antiasthmatic (Nonbronchodilator). |