Title: Israpafant
CAS Registry Number: 117279-73-9
CAS Name: 4-(2-Chlorophenyl)-6,9-dimethyl-2-[2-[4-(2-methylpropyl)phenyl]ethyl]-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
Additional Names: (±)-4-(o-chlorophenyl)-2-(p-isobutylphenethyl)-6,9-dimethyl-6H-thieno[3,2-f]-s-triazolo[4,3-a][1,4]diazepine
Manufacturers' Codes: Y-24180
Trademarks: Pafnol (Yoshitomi)
Molecular Formula: C28H29ClN4S
Molecular Weight: 489.07
Percent Composition: C 68.76%, H 5.98%, Cl 7.25%, N 11.46%, S 6.56%
Literature References: Platelet activating factor (PAF) antagonist. Prepn: T. Tahara et al., EP 268242; eidem, US 4820703 (1988, 1989 both to Yoshitomi). Pharmacology: M. Terasawa et al., Prostaglandins 40, 553 (1990). Receptor binding study: S. Takehara et al., ibid. 571. Clinical evaluation in asthma: S. Hozawa et al., Am. J. Respir. Crit. Care Med. 152, 1198 (1995).
Properties: Colorless crystals from isopropyl ether, mp 129.5-131.5°. Sol in propylene glycol.
Melting point: mp 129.5-131.5°
Therap-Cat: Antiasthmatic.
Keywords: Antiasthmatic (Nonbronchodilator); Platelet Activating Factor Antagonist. |