CAS Number78755-81-4
SynonymsRomazicon; Lanexat; Anexate; Ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate; Ro-15-1788; Ro 15-1788; YM-684; Ro 1722; Ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate; Mazicon; Flumazenil; FMZ; Flumazepil; Ethyl-8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate; MFCD00242764
Molecular FormulaC15H14FN3O3
Molecular Weight303.29
Purity98%
Density1.4±0.1 g/cm3
Boiling Point528.0±50.0 °C at 760 mmHg
Melting Point201-203°C
Appearancesolid | white
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 78755-81-4 |
| Catalog No. | 2A-9010554 |
| Chinese Name | 氟吗西尼 |
| Synonyms | Romazicon; Lanexat; Anexate; Ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate; Ro-15-1788; Ro 15-1788; YM-684; Ro 1722; Ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate; Mazicon; Flumazenil; FMZ; Flumazepil; Ethyl-8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate; MFCD00242764 |
| Molecular Formula | C15H14FN3O3 |
| Molecular Weight | 303.29 |
| Purity | 98 |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 528.0±50.0 °C at 760 mmHg |
| Melting Point | 201-203°C |
| Appearance | solid | white |
| Water Solubility | 128 mg/L |
| Storage Condition | 2-8°C |
| Application | Flumazenil is a competitive GABAA receptor antagonist used to treat benzodiazepine overdose. |
| HTC | 2933990090 |
| PubChem ID | 329749857 |
| MDL Number | MFCD00242764 |
| SMILES | CCOC(=O)c1ncn-2c1CN(C)C(=O)c3cc(F)ccc-23 |
| 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,3,7H2,1-2H3 |
| InChI Key | OFBIFZUFASYYRE-UHFFFAOYSA-N |
| NACRES Code | NA.24 |
| UNSPSC | 41116107 |
| MSDS | msds/10554_1_78755_81_4.pdf |
| Use of | Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses. Properties Articles70 Name flumazenil Synonym More Synonyms Flumazenil Biological Activity Description Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses. Related Catalog Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor Signaling Pathways >> Neuronal Signaling >> GABA Receptor Research Areas >> Neurological Disease References [1]. Hoffman EJ, et al. Flumazenil: a benzodiazepine antagonist. Clin Pharm. 1993 Sep;12(9):641-56; quiz 699-701. [3]. Fernandez-Guasti A, et al. Flumazenil blocks the anxiolytic action of allopregnanolone. Eur J Pharmacol. 1995 Jul 25;281(1):113-5. [4]. Loscher W, et al. Effects of the non-NMDA antagonists NBQX and the 2,3-benzodiazepine GYKI 52466 on different seizure types in mice: comparison with diazepam and interactions with flumazenil. Br J Pharmacol. 1994 Dec;113(4):1349-57. [5]. Moy SS, et al. Flumazenil blockade of anxiety following ethanol withdrawal in rats. Psychopharmacology (Berl). 1997 Jun;131(4):354-60. Chemical & Physical Properties Molecular Formula C15H14FN3O3 Exact Mass 303.101929 PSA 64.43000 Appearance of Characters solid | white Index of Refraction 1.634 InChIKey OFBIFZUFASYYRE-UHFFFAOYSA-N Toxicological Information CHEMICAL IDENTIFICATION RTECS NUMBER : 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 LAST UPDATED : DATA ITEMS CITED : MOLECULAR FORMULA : C15-H14-F-N3-O3 MOLECULAR WEIGHT : 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 : SPECIES OBSERVED : Human - woman DOSE/DURATION : 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 : 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 : SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 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 : TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 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 : SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 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 : TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 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 : 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 : SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 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 : 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 : SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 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 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 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 Safety Information Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter Hazard Codes Xi RIDADR NONH for all modes of transport WGK Germany 2 RTECS NI2922170 HS Code 2933990090 Synthetic Route (E)-(dimethylam... 428507-28-2 2-chloro-7-fluo... 193693-31-1 Flumazenil 78755-81-4 Literature: Rogers-Evans, Mark; Spurr, Paul; Hennig, Michael Tetrahedron Letters, 2003 , vol. 44, # 11 p. 2425 - 2428 Hexamethyldisil... 4,N,N-Trimethyl... (E)-(dimethylam... 428507-28-2 2-chloro-7-fluo... 193693-31-1 Literature: US5670640 A1, ; ethyl N-((dimet... 30766-78-0 Hexamethyldisil... 4,N,N-Trimethyl... 2-chloro-7-fluo... 193693-31-1 Literature: US5670640 A1, ; Precursor & DownStream Precursor 9 CAS#:428507-28-2 (E)-(dimethylam... CAS#:193693-31-1 2-chloro-7-fluo... CAS#:999-97-3 Hexamethyldisilazane CAS#:99-97-8 4,N,N-Trimethyl... DownStream 2 CAS#:133368-73-7 3'-fluoropropyl... CAS#:84378-44-9 Flumazenil acid |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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