Title: Quazepam
CAS Registry Number: 36735-22-5
CAS Name: 7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione
Manufacturers' Codes: Sch-16134
Trademarks: Doral (Wallace); Dormalin (Schering-Plough); Oniria (Lifepharma); Prosedar (Schering-Plough); Quazium (Schering); Selepam (Schering-Plough)
Molecular Formula: C17H11ClF4N2S
Molecular Weight: 386.79
Percent Composition: C 52.79%, H 2.87%, Cl 9.17%, F 19.65%, N 7.24%, S 8.29%
Literature References: Benzodiazepine hypnotic. Prepn: M. Steinman, DE 2138773; idem, US 3845039 (1972, 1974 both to Schering Corp.); M. Steinman et al., J. Med. Chem. 16, 1354 (1973). Pharmacology: A. Barnett et al., Arzneim.-Forsch. 32, 1452 (1982); E. Ongini et al., ibid. 1456. GC determn in plasma: J. M. Hilbert et al., J. Pharm. Sci. 73, 516 (1984). Pharmacokinetics: M. Chung et al., Clin. Pharm. Ther. 35, 520 (1984). Metabolism: N. Zampaglione et al., Drug Metab. Dispos. 13, 25 (1985). Clinical trials in insomnia: J. W. Goethe, G. Kader, Curr. Ther. Res. 32, 150 (1982); M. Mamelak et al., J. Clin. Pharmacol. 24, 65 (1984). Toxicology: H. E. Black et al., Arzneim.-Forsch. 37, 906 (1987).
Properties: Crystals from methylene chloride-hexane, mp 137.5-139°. LD50 in mice (mg/kg): >1370 i.v., >5000 orally (Orgini). LD50 in male, female mice, rats (mg/kg): 845, 921, 3072, 2749 i.p. (Black).
Melting point: mp 137.5-139°
Toxicity data: LD50 in mice (mg/kg): >1370 i.v., >5000 orally (Orgini); LD50 in male, female mice, rats (mg/kg): 845, 921, 3072, 2749 i.p. (Black)
NOTE: This is a controlled substance (depressant): 21 CFR, 1308.14.
Therap-Cat: Sedative, hypnotic.
Keywords: Sedative/Hypnotic; Benzodiazepine Derivatives. |