9604. Triazolam

Nomenclature

CAS number: 28911-01-5
8-Chloro-6-(2-chlorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine; 8-chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine; clorazolam; U-33030; Halcion (Pharmacia & Upjohn); Songar (Valeas).
C17H12Cl2N4; mol wt 343.21.
C 59.49%, H 3.52%, Cl 20.66%, N 16.32%.

Description and references

Prepn: J. B. Hester, DE 2012190; eidem, US 3701782 (1970, 1972 both to Upjohn); J. B. Hester et al., J. Med. Chem. 14, 1078 (1971). Pharmacology: T. Furukawa et al., Igaku Kenkyu 45, 285 (1975), C.A. 84, 130354p. Metabolism: F. S. Eberts, Drug Metab. Dispos. 5, 547 (1977). HPLC determn in urine: T. Inoue, S. Suzuki, J. Chromatogr. 422, 197 (1987). Clinical studies: K. K. Okawa, G. S. Allens, J. Int. Med. Res. 6, 343 (1978); A. J. Bowen, ibid. 337; A. J. Puech et al., Therapie 33, 287 (1978). Toxicity: Pharm. Weekbl. 113, 725 (1978). Review of pharmacology and therapeutic efficacy: G. E. Pakes et al., Drugs 22, 81-110 (1981).

Chemical structure

Properties

Tan crystals from 2-propanol, mp 233-235°. Sol in alcohol. Poorly sol in water. LD50 in mice, rats (mg/kg): >100, >5000 orally (Pharm. Weekblad.).

Note

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

Therapeutic Category

Sedative, hypnotic.

Keywords

Sedative/Hypnotic; Benzodiazepine Derivatives