3873. Etizolam

Nomenclature

CAS number: 40054-69-1
4-(2-Chlorophenyl)-2-ethyl-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine; 1-methyl-6-o-chlorophenyl-8-ethyl-4H-s-triazolo[3,4-c]thieno[2,3-e]-1,4-diazepine; Y-7131; Depas (Yoshitomi).
C17H15ClN4S; mol wt 342.85.
C 59.55%, H 4.41%, Cl 10.34%, N 16.34%, S 9.35%.

Description and references

Prepn: M. Nakanishi et al., DE 2229845; eidem, US 3904641 (1972, 1973 both to Yoshitomi). Pharmacology and toxicity studies: T. Tsumagari et al., Arzneim.-Forsch. 28, 1158 (1978). Effect on monoamine metabolism in brain: M. Setoguchi et al., ibid. 1165; on rage responses in cats: T. Fukuda, T. Tsumagari, Jpn. J. Pharmacol. 33, 885 (1983).

Chemical structure

Properties

Crystals from toluene, mp 147-148°. LD50 in male, female rats, male, female mice (mg/kg): 3619, 3509, 4358, 4258 orally; 865, 825, 830, 783 i.p.; >5000 s.c. (Tsumagari).

Therapeutic Category

Anxiolytic.

Keywords

Anxiolytic; Benzodiazepine Derivatives