8029. Quazepam

Nomenclature

CAS number: 36735-22-5
7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione; Sch-16134; Doral (Wallace); Dormalin (Schering-Plough); Oniria (Lifepharma); Prosedar (Schering-Plough); Quazium (Schering); Selepam (Schering-Plough).
C17H11ClF4N2S; mol wt 386.79.
C 52.79%, H 2.87%, Cl 9.17%, F 19.65%, N 7.24%, S 8.29%.

Description and 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. Pharmacol. 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).

Chemical structure

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).

Note

This is a controlled substance (depressant): 21 CFR, 1308.14.

Therapeutic Category

Sedative, hypnotic.

Keywords

Sedative/Hypnotic; Benzodiazepine Derivatives