9243. Tetrazepam

Nomenclature

CAS number: 10379-14-3
7-Chloro-5-(1-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1,4-benzodiazepin-2-one; 7-chloro-5-(1-cyclohexenyl)-1-methyl-2-oxo-2,3-dihydro-1H-[1,4]benzo[f]diazepine; CB-4261; Musaril (Sanofi-Synthelabo); Muskelat (Azupharma); Myolastan (Sanofi-Synthelabo).
C16H17ClN2O; mol wt 288.77.
C 66.55%, H 5.93%, Cl 12.28%, N 9.70%, O 5.54%.

Description and references

Prepn: Schmitt, NL 6600095 and US 3426014; US 3551412 (1966, 1969, 1970 to Clin-Byla); Schmitt et al., Chim. Ther. 2, 254 (1967). Spectroscopic and chromatographic studies: Lafargue et al., Ann. Pharm. Fr. 28, 343, 477 (1970). GC-MS determn in urine: H. Maurer, K. Pfleger, J. Chromatogr. 422, 85 (1987). Pharmacokinetics: H. Bun et al., Arzneim.-Forsch. 37, 199 (1987). Pharmacology and benzodiazepine receptor study: P. E. Keane et al., J. Pharmacol. Exp. Ther. 245, 692, 699 (1988). Clinical evaluation in post-stroke spasticity: I. Milanov, Acta Neurol. Belg. 92, 5 (1992).

Chemical structure

Properties

Yellow-brown crystals from ethyl acetate, mp 144°. uv max (ethanol): 227 nm (ε 28500). LD50 in mice (mg/kg): 415 i.p.; 2000 orally (Schmitt).

Note

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

Therapeutic Category

Muscle relaxant (skeletal).

Keywords

Muscle Relaxant (Skeletal)