1450. Brotizolam

Nomenclature

CAS number: 57801-81-7
2-Bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine; 2-bromo-4-(o-chlorophenyl)-9-methyl-6H-thieno[3,2-f]-s-triazolo[4,3-a][1,4]diazepine; 8-bromo-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo[3,4-c]thieno[2,3-e]-1,4-diazepine; WE-941-BS; Lendorm (Boehringer, Ing.); Lendormin (Boehringer, Ing.); Mederantil (Boehringer, Ing.); Nimbisan (Solvay); Sintonal (Europharma).
C15H10BrClN4S; mol wt 393.69.
C 45.76%, H 2.56%, Br 20.30%, Cl 9.01%, N 14.23%, S 8.14%.

Description and references

One of a class of triazolo-1,4-thienodiazepines having psychotropic activity. Prepn: K. H. Weber et al., DE 2410030; eidem, US 4094984 (1975, 1978 to Boehringer, Ing.); eidem, Ann. 8, 1257 (1978). Pharmacodynamics: J. Gruenberger et al., Curr. Ther. Res. 24, 427 (1978). Bioavailability: B. Saletu et al., Arzneim.-Forsch. 29, 700 (1979). Pharmaco-EEG study: M. Fink, P. Irwin, Clin. Pharmacol. Ther. 30, 336 (1981). Toxicity studies: C. Hewett et al., Arzneim.-Forsch. 36, 592 (1986). Series of articles on pharmacology, pharmacokinetics, toxicology: ibid. 517-620. Veterinary trial as appetite stimulant: A. van Miert et al., J. Vet. Pharmacol. Ther. 12, 147 (1989). Review of pharmacology and clinical efficacy: M. S. Langley, S. P. Clissold, Drugs 35, 104-122 (1988).

Chemical structure

Properties

Colorless crystals from ethanol, mp 212-214°. LD50 in mice, rats (mg/kg): >10000, >10000 orally; 920, 1000 i.p. (Hewett).

Therapeutic Category

Sedative, hypnotic.

Therapeutic Category (Veterinary)

Appetite stimulant.

Keywords

Sedative/Hypnotic; Benzodiazepine Derivatives