Title: Fludiazepam
CAS Registry Number: 3900-31-0
CAS Name: 7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-1-methyl-2H-1,4-benzodiazepin-2-one
Manufacturers' Codes: ID-540; Ro-5-3438
Trademarks: Erispan (Sumitomo)
Molecular Formula: C16H12ClFN2O
Molecular Weight: 302.73
Percent Composition: C 63.48%, H 4.00%, Cl 11.71%, F 6.28%, N 9.25%, O 5.29%
Literature References: Fluorinated analog of diazepam, q.v. Prepn: E. Reeder et al., DE 1136709; E. Reeder, L. H. Sternbach, US 3371085 (1962, 1968 both to Hoffmann-LaRoche); L. H. Sternbach et al., J. Org. Chem. 27, 3788 (1962). Synthesis and pharmacology: Y. Asami et al., Arzneim.-Forsch. 24, 1563 (1974). Pharmacodynamics: M. Nakamura, H. Fukushima, J. Pharm. Pharmacol. 30, 56, 254 (1978); T. Tsuchiya, H. Fukushima, Eur. J. Pharmacol. 48, 421 (1978). Anxiolytic vs sedative properties: M. Babbini et al., Life Sci. 25, 15 (1979).
Properties: Colorless prisms from n-hexane/isopropanol, mp 88-92°, (Asami); also reported as mp 69-72° (Sternbach). LD50 in mice (mg/kg): 910 orally; 360 i.p.; 1150 s.c. (Asami).
Melting point: mp 88-92°; mp 69-72° (Sternbach)
Toxicity data: LD50 in mice (mg/kg): 910 orally; 360 i.p.; 1150 s.c. (Asami)
NOTE: This is a controlled substance (depressant): 21 CFR, 1308.14.
Therap-Cat: Anxiolytic.
Keywords: Anxiolytic; Benzodiazepine Derivatives. |