Mexazolam
Title: Mexazolam
CAS Registry Number: 31868-18-5
CAS Name: 10-Chloro-11b-(2-chlorophenyl)-2,3,7,11b-tetrahydro-3-methyloxazolo[3,2-d][1,4]benzodiazepin-6(5H)-one
Additional Names: 10-chloro-11b-(o-chlorophenyl)-2,3,7,11b-tetrahydro-3-methyloxazolo[3,2-d][1,4]benzodiazepin-6(5H)-one
Manufacturers' Codes: CS-386
Trademarks: Melex (Sankyo); Melium (Han Wha); Sedoxil (Bial)
Molecular Formula: C18H16Cl2N2O2
Molecular Weight: 363.24
Percent Composition: C 59.52%, H 4.44%, Cl 19.52%, N 7.71%, O 8.81%
Literature References: Prepn from 2-amino-2¢,5-dichlorobenzophenone: R. Tachikawa et al., DE 1812252; eidem, US 3772371 (1969, 1973 to Sankyo). Synthesis via Schiff base, physical properties: T. Miyadera et al., J. Med. Chem. 14, 520 (1971). Acid-base equilibrium: M. Ikeda, T. Nagai, Chem. Pharm. Bull. 30, 3810 (1982). Effect on socially induced suppression in monkeys: T. Kamioka et al., Psychopharmacology 52, 17 (1977). Toxicity studies: H. Masuda et al., Sankyo Kenkyusho Nempo 30, 175 (1978), C.A. 90, 180217d. Clinical effects on anxiety and pyschomotor performance in generalised anxiety disorder: L. Ferreira et al., Clin. Drug Invest. 23, 235 (2003).
Properties: Crystals, mp 172-175°. pKa 6.69. LD50 in male, female mice; male, female rats (mg/kg): 4687, 4571, 810, 4500 orally; >6000, >6000, >4000, >4000 i.p. or s.c. (Masuda).
Melting point: mp 172-175°
pKa: pKa 6.69
Toxicity data: LD50 in male, female mice; male, female rats (mg/kg): 4687, 4571, 810, 4500 orally; >6000, >6000, >4000, >4000 i.p. or s.c. (Masuda)
Therap-Cat: Anxiolytic.
Keywords: Anxiolytic; Benzodiazepine Derivatives.

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