Title: Flutoprazepam
CAS Registry Number: 25967-29-7
CAS Name: 7-Chloro-1-(cyclopropylmethyl)-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one
Manufacturers' Codes: KB-509; ID-1937
Trademarks: Restar (Sumitomo); Restas (Kanebo)
Molecular Formula: C19H16ClFN2O
Molecular Weight: 342.79
Percent Composition: C 66.57%, H 4.70%, Cl 10.34%, F 5.54%, N 8.17%, O 4.67%
Literature References: Benzodiazepine derivative. Prepn: H. Yamamoto et al., GB 1253368; eidem, US 3925364 (1971, 1975 both to Sumitomo). New process: T. Okamoto et al., DE 2151540; eidem, US 3832344 (1972, 1974 both to Sumitomo). Stability and degradation mechanism in aqueous solns: K. Akimoto et al., Int. J. Pharm. 3, 109 (1979). Pharmacokinetics and metabolism: A. Kozaki et al., Yakugaku Zasshi 102, 1177 (1982), C.A. 98, 119080q (1983). Pharmacology of flutoprazepam and metabolites: K. Oki et al., Arch. Int. Pharmacodyn. Ther. 269, 180 (1984). Acute toxicity study: H. Takebe et al., Oyo Yakuri 20, 1055 (1980), C.A. 95, 73630b (1981).
Properties: Crystals, mp 118-122°. LD50 in male, female mice, rats (mg/kg): 2640, 2430, 13760, 10060 orally; 2400, 2110, 2460, 2230 i.p.; >5000 s.c. all species (Takebe).
Melting point: mp 118-122°
Toxicity data: LD50 in male, female mice, rats (mg/kg): 2640, 2430, 13760, 10060 orally; 2400, 2110, 2460, 2230 i.p.; >5000 s.c. all species (Takebe)
Therap-Cat: Anxiolytic.
Keywords: Anxiolytic; Benzodiazepine Derivatives. |