*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : NI2922170
CHEMICAL NAME : 4H-Imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylic
acid, 8-fluoro-5,6-dihydro-5-methyl-6- oxo-, ethyl
ester
CAS REGISTRY NUMBER : 78755-81-4
BEILSTEIN REFERENCE NO. : 4763661
LAST UPDATED : 199612
DATA ITEMS CITED : 15
MOLECULAR FORMULA : C15-H14-F-N3-O3
MOLECULAR WEIGHT : 303.32
COMPOUND DESCRIPTOR : Drug
Reproductive Effector
Human
SYNONYMS/TRADE NAMES :
* Anexate
* Ethyl
8-fluoro-5-methyl-5,6-dihydro-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine
-3-carboxylate
* Flumazenil
* Flumazepil
* Lanexat
* Ro-15-1788
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Human - man
DOSE/DURATION : 5700 ng/kg/C
TOXIC EFFECTS :
Cardiac - cardiomyopathy including infarction
Cardiac - arrhythmias (including changes in conduction)
Cardiac - change in rate
REFERENCE :
BMJOAE British Medical Journal. (British Medical Assoc., BMA House,
Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year:
304,1415,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 2 mg/kg/2D-I
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions
Behavioral - excitement
Behavioral - aggression
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823-
Volume(issue)/page/year: 339,488,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 4 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Cardiac - EKG changes not diagnostic of specified effects
Cardiac - pulse rate increase, without fall in BP
REFERENCE :
PECAE5 Pediatric Emergency Care. (Williams & Wilkins, 428 E. Preston St.,
Baltimore, MD 21202) V.1- 1985- Volume(issue)/page/year: 11,186,1995
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 4200 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Behavioral - tremor
Behavioral - rigidity (including catalepsy)
REFERENCE :
JTCEEM Journal de Toxicologie Clinique et Experimentale. (SPPIF, B.P.22,
F-41353 Vineuil, France) V.5- 1985- Volume(issue)/page/year: 7,223,1987
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 1360 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540,
08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year:
7,402,1982
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 85 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - rigidity (including catalepsy)
REFERENCE :
JTCEEM Journal de Toxicologie Clinique et Experimentale. (SPPIF, B.P.22,
F-41353 Vineuil, France) V.5- 1985- Volume(issue)/page/year: 7,223,1987
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 1300 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Behavioral - tremor
Behavioral - rigidity (including catalepsy)
REFERENCE :
JTCEEM Journal de Toxicologie Clinique et Experimentale. (SPPIF, B.P.22,
F-41353 Vineuil, France) V.5- 1985- Volume(issue)/page/year: 7,223,1987
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 4 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540,
08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year:
7,402,1982
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : >1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho
Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970-
Volume(issue)/page/year: 23,201,1992
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 143 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - rigidity (including catalepsy)
REFERENCE :
JTCEEM Journal de Toxicologie Clinique et Experimentale. (SPPIF, B.P.22,
F-41353 Vineuil, France) V.5- 1985- Volume(issue)/page/year: 7,223,1987
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >640 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho
Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970-
Volume(issue)/page/year: 23,201,1992
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >30 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho
Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970-
Volume(issue)/page/year: 23,201,1992
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE/DURATION : 2 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Behavioral - tremor
Behavioral - rigidity (including catalepsy)
REFERENCE :
JTCEEM Journal de Toxicologie Clinique et Experimentale. (SPPIF, B.P.22,
F-41353 Vineuil, France) V.5- 1985- Volume(issue)/page/year: 7,223,1987
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 21 mg/kg
SEX/DURATION : female 14-20 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - behavioral
REFERENCE :
PNPPD7 Progress in Neuro-Psychopharmacology and Biological Psychiatry.
(Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.6-
1982- Volume(issue)/page/year: 17,151,1993
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE : 220 mg/kg
SEX/DURATION : female 11-21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - behavioral
REFERENCE :
GEPHDP General Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview
Park, Elmsford, NY 10523) V.6- 1975- Volume(issue)/page/year: 22,43,1991
*** END OF RECORD ***