183. Afloqualone

Nomenclature

CAS number: 56287-74-2
6-Amino-2-(fluoromethyl)-3-(2-methylphenyl)-4(3H)-quinazolinone; 6-amino-2-fluoromethyl-3-(o-tolyl)-4(3H)-quinazolinone; HQ-495; Arofuto (Tanabe).
C16H14FN3O; mol wt 283.30.
C 67.83%, H 4.98%, F 6.71%, N 14.83%, O 5.65%.

Description and references

A centrally acting muscle relaxant. Prepn: I. Inoue et al., DE 2449113; eidem, US 3966731 (1975, 1976 to Tanabe); J. Tani et al., J. Med. Chem. 22, 95 (1979). Pharmacology: T. Ochiai, R. Ishida, Jpn. J. Pharmacol. 31, 491 (1981); 32, 427 (1982). Metabolism: N. Otsuka et al., J. Pharmacobio-Dyn. 5, S-59 (1982); S. Furuuchi et al., Drug Metab. Dispos. 11, 371 (1983).

Chemical structure

Properties

Pale yellow prisms from 2-propanol, mp 195-196°. LD50 in mice (mg/kg): 315.1 i.p. (Tani).

Therapeutic Category

Muscle relaxant (skeletal).

Keywords

Muscle Relaxant (Skeletal)