Flumazenil
Title: Flumazenil
CAS Registry Number: 78755-81-4
CAS Name: 8-Fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl ester
Additional Names: ethyl-8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate; flumazepil
Manufacturers' Codes: Ro-15-1788
Trademarks: Anexate (Roche); Lanexat (Roche); Mazicon (Roche); Romazicon (Roche)
Molecular Formula: C15H14FN3O3
Molecular Weight: 303.29
Percent Composition: C 59.40%, H 4.65%, F 6.26%, N 13.85%, O 15.83%
Literature References: Imidazodiazepine which selectively blocks the central effects of classic benzodiazepines. Prepn: W. Haefely et al., EP 27214; M. Gerecke et al., US 4316839 (1981, 1982 both to Hoffmann-La Roche). Specific inhibition of benzodiazepine-receptor binding: W. Hunkeler et al., Nature 290, 514 (1981). Electrophysiological study in animals: P. Pole et al., Arch. Pharmacol. 316, 317 (1981). Antagonist, agonist and inverse agonist properties: S. E. File et al., Psychopharmacology 89, 113 (1986). HPLC determn in human plasma: U. Timm, M. Zell, Arzneim.-Forsch. 33, 358 (1983). Clinical reversal of benzodiazepine-induced sedation: A. Darragh et al., Lancet 2, 8 (1981); eidem, ibid. 1042; B. Ricou et al., Br. J. Anaesth. 58, 1005 (1986). Clinical evaluation in drug overdose: G. F. O'Sullivan et al., Clin. Pharmacol. Ther. 42, 254 (1987).
Properties: Crystals from alcohol, mp 201-203°. LD50 in mice, rats (mg/kg): 4000, 1360 i.p.; 4300, 6000 orally (Hunkeler).
Melting point: mp 201-203°
Toxicity data: LD50 in mice, rats (mg/kg): 4000, 1360 i.p.; 4300, 6000 orally (Hunkeler)
Therap-Cat: Benzodiazepine antagonist.
Keywords: Benzodiazepine Antagonist.

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