2416. Clotiazepam

Nomenclature

CAS number: 33671-46-4
5-(2-Chlorophenyl)-7-ethyl-1,3-dihydro-1-methyl-2H-thieno[2,3-e]-1,4-diazepin-2-one; Y-6047; Clozan (Roerig); Rise (Yoshitomi); Rize (Yoshitomi); Rizen (Formenti); Tienor (Farmaka); Trecalmo (Bayer); Veratran (Latema).
C16H15ClN2OS; mol wt 318.82.
C 60.28%, H 4.74%, Cl 11.12%, N 8.79%, O 5.02%, S 10.06%.

Description and references

A thienodiazepine tranquilizer with biological activity similar to the benzodiazepines. Prepn: M. Nakanishi et al., DE 2107356; eidem, US 3849405 (1971, 1974 both to Yoshitomi); eidem, J. Med. Chem. 16, 214 (1973). Pharmacology: eidem, Arzneim.-Forsch. 22, 1905 (1972). Effects on biogenic amine metabolism: eidem, ibid. 1914. Metabolism: eidem, Yakugaku Zasshi 93, 311 (1973), C.A. 79, 13397r (1973). Clinical studies: S. Sieberns, Fortschr. Med. 97, 1705 (1979).

Chemical structure

Properties

Crystals from hexane, mp 105-106°. LD50 in mice (mg/kg): 440 i.p., 636 orally (Nakanishi).

Note

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

Therapeutic Category

Anxiolytic.

Keywords

Anxiolytic; Benzodiazepine Derivatives