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Substance Name: Flumazenil [USAN:USP:INN:BAN]
RN: 78755-81-4
UNII: 40P7XK9392
InChIKey: OFBIFZUFASYYRE-UHFFFAOYSA-N
Note
- A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.
Molecular Formula
- C15-H14-F-N3-O3
Molecular Weight
- 303.2916
- All
- Classifications
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- Names & Synonyms
- Registry Numbers
- Structure Descriptors
- Toxicity
- Physical Properties
Classification Codes
- Antagonist (to Benzodiazepine)
- Antidotes
- Drug / Therapeutic Agent
- GABA Agents
- GABA Modulators
- Human Data
- Neurotransmitter Agents
- Protective Agents
- Reproductive Effect
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Links to Resources
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Names and Synonyms
Name of Substance
- Flumazenil
- Flumazenil [USAN:USP:INN:BAN]
MeSH Heading
- Flumazenil
Synonyms
- 4H-Imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylic acid, 8-fluoro-5,6-dihydro-5-methyl-6-oxo-, ethyl ester
- Anexate
- BRN 4763661
- Ethyl 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylate
- Ethyl 8-fluoro-5-methyl-5,6-dihydro-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylate
- Flumazenil
- Flumazenilo
- Flumazenilo [Spanish]
- Flumazenilum
- Flumazenilum [Latin]
- Flumazepil
- Flumazil
- Lanexat
- NSC 759193
- Ro 15-1788/000
- Ro 151788
- Ro-15-1788
- Romazicon
- UNII-40P7XK9392
Systematic Name
- 4H-Imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylic acid, 8-fluoro-5,6-dihydro-5-methyl-6-oxo-, ethyl ester
Registry Numbers
CAS Registry Number
- 78755-81-4
FDA UNII
- 40P7XK9392
System Generated Number
- 0078755814
Structure Descriptors
InChI
InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3InChIKey
OFBIFZUFASYYRE-UHFFFAOYSA-NSmiles
CCOC(=O)Toxicity
Organism | Test Type | Route | Reported Dose (Normalized Dose) | Effect | Source |
---|---|---|---|---|---|
dog | LDLo | intravenous | > 30mg/kg (30mg/kg) | Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 23, Pg. 201, 1992. | |
dog | LDLo | oral | > 640mg/kg (640mg/kg) | Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 23, Pg. 201, 1992. | |
man | LDLo | intravenous | 5700ng/kg/C (0.0057mg/kg) | CARDIAC: CARDIOMYOPATHY INCLUDING INFARCTION CARDIAC: ARRHYTHMIAS (INCLUDING CHANGES IN CONDUCTION) CARDIAC: CHANGE IN RATE | British Medical Journal. Vol. 304, Pg. 1415, 1992. |
mouse | LD50 | intraperitoneal | 4gm/kg (4000mg/kg) | Drugs of the Future. Vol. 7, Pg. 402, 1982. | |
mouse | LD50 | intravenous | 143mg/kg (143mg/kg) | BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD BEHAVIORAL: REGIDITY | Journal de Toxicologie Clinique et Experimentale. Vol. 7, Pg. 223, 1987. |
mouse | LD50 | oral | 1300mg/kg (1300mg/kg) | BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) BEHAVIORAL: REGIDITY BEHAVIORAL: TREMOR | Journal de Toxicologie Clinique et Experimentale. Vol. 7, Pg. 223, 1987. |
mouse | LDLo | subcutaneous | > 1gm/kg (1000mg/kg) | Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 23, Pg. 201, 1992. | |
rabbit | LD50 | oral | 2gm/kg (2000mg/kg) | BEHAVIORAL: TREMOR BEHAVIORAL: REGIDITY BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) | Journal de Toxicologie Clinique et Experimentale. Vol. 7, Pg. 223, 1987. |
rat | LD50 | intraperitoneal | 1360mg/kg (1360mg/kg) | Drugs of the Future. Vol. 7, Pg. 402, 1982. | |
rat | LD50 | intravenous | 85mg/kg (85mg/kg) | BEHAVIORAL: REGIDITY BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD | Journal de Toxicologie Clinique et Experimentale. Vol. 7, Pg. 223, 1987. |
rat | LD50 | oral | 4200mg/kg (4200mg/kg) | BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) BEHAVIORAL: REGIDITY BEHAVIORAL: TREMOR | Journal de Toxicologie Clinique et Experimentale. Vol. 7, Pg. 223, 1987. |
women | TDLo | intravenous | 4ug/kg (0.004mg/kg) | CARDIAC: EKG CHANGES NOT DIAGNOSTIC OF ABOVE CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD | Pediatric Emergency Care. Vol. 11, Pg. 186, 1995. |
women | TDLo | oral | 2mg/kg/2D-I (2mg/kg) | BEHAVIORAL: EXCITEMENT BEHAVIORAL: AGGRESSION BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS" | Lancet. Vol. 339, Pg. 488, 1992. |
Physical Properties
Physical Property | Value | Units | Temp (deg C) | Source |
---|---|---|---|---|
Melting Point | 201-203 | deg C | EXP | |
log P (octanol-water) | 1 | (none) | EXP | |
Water Solubility | 128 | mg/L | 25 | EST |
Vapor Pressure | 8.30E-10 | mm Hg | 25 | EST |
Henry's Law Constant | 9.89E-17 | atm-m3/mole | 25 | EST |
Atmospheric OH Rate Constant | 3.63E-11 | cm3/molecule-sec | 25 | EST |
Physical property data is provided to ChemIDplus by SRC, Inc.