HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Etizolam
azepin · Etizola · 4-(2-Chlorophenyl)-2-ethyl-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine · depas · Y-7131 · EtizoL · ahr3219 · ETIZOLAM
Identifikatoren & physikalische Daten
| CAS No. | 40054-69-1 |
|---|---|
| Summenformel | C17H15ClN4S |
| Durchschnittliche Molmasse | 342,8 g/mol |
| Monoisotopische Masse | 342,07059516 g/mol |
| SMILES | CCc1cc2c(s1)-n1c(C)nnc1CN=C2c1ccccc1Cl |
| InChIKey | VMZUTJCNQWMAGF-UHFFFAOYSA-N |
| PubChem CID | 3307 |
| ChEMBL | CHEMBL1289779 |
| ChEBI | CHEBI:31583 |
| EC No. | 662-368-4 |
| DTXSID | DTXSID0023030 |
Chemische & physikalische Eigenschaften
| XLogP | 2,6 |
|---|---|
| Polarare Oberfläche (TPSA) | 71,3 |
| H-Brücken-Donoren | 0 |
| H-Brücken-Akzeptoren | 4 |
| Frei drehbare Bindungen | 2 |
| Schwere Atome | 23 |
| Formalladung | 0 |
| Komplexität | 474 |
| Arzneimittel | DEA NFLIS-Drug Category -> BenzodiazepinesDEA Schedule I Controlled Substance -> DepressantsPharmaceuticals -> Synthetic Cannabinoids or Psychoactive CompoundsPharmaceuticals -> Listed in ZINC15 |
| LogP (Verteilungskoeffizient) | 2.52 |
| Löslichkeit | Practically insolubleDMF: 5 mg/mlDMSO: 5 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/ml |
| Human Drugs | Breast FeedingLactationMilk, HumanHypnotics and SedativesAnti-Anxiety AgentsBenzodiazepines |
| Schmelzpunkt | 147-148147-148℃ |
| Siedepunkt | 264.5°C (rough estimate) |
| Dichte | 1.43 |
| Brechungsindex | 1.6100 (estimate) |
| Flammpunkt | 9°C |
| Lagerbedingungen | -20°C |
| Aggregatzustand | A neat solid |
| pKa (Säurekonstante) | 2.37±0.40(Predicted) |
| CAS Datenbank | 40054-69-1 |
Sicherheit & Vorschriften
| GHS-Einstufung | DangerH315 (60%): Causes skin irritation [Warning Skin corrosion/irritation]P203, P264, P264+P265, P280, P302+P352, P305+P351+P338, P318, P321, P332+P317, P337+P317, P362+P364, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 65 reports by companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. |
|---|---|
| Regulatorische Informationen | DEA schedule I controlled substance |
| Hazard Classes and Categories | Skin Irrit. 2 (60%) |
| Treatment | General supportive measures should be employed, along with intravenous fluids, and an adequate airway maintained. Hypotension may be combated by the use of norepinephrine or metaraminol. Dialysis is of limited value. Flumazenil (Anexate) is a competitive benzodiazepine receptor antagonist that can be used as an antidote for benzodiazepine overdose. In particular, flumazenil is very effective at reversing the CNS depression associated with benzodiazepines but is less effective at reversing respiratory depression. Its use, however, is controversial as it has numerous contraindications. It is contraindicated in patients who are on long-term benzodiazepines, those who have ingested a substance that lowers the seizure threshold, or in patients who have tachycardia or a history of seizures. As a general rule, medical observation and supportive care are the mainstay of treatment of benzodiazepine overdose. Although benzodiazepines are absorbed by activated charcoal, gastric decontamination with activated charcoal is not beneficial in pure benzodiazepine overdose as the risk of adverse effects often outweigh any potential benefit from the procedure. It is recommended only if benzodiazepines have been taken in combination with other drugs that may benefit from decontamination. Gastric lavage (stomach pumping) or whole bowel irrigation are also not recommended. |
| Toxizitätsübersicht | Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. |
| Carcinogen Classification | No indication of carcinogenicity to humans (not listed by IARC). |
| Drug Induced Liver Injury | Drug-Induced Liver Injury Severity and Toxicity (DILIst)EtizolamDILI PositiveDOI:10.1016/j.drudis.2019.09.022 |
| Effects During Pregnancy and Lactation | ◉ Summary of Use during Lactation |
| Wassergefährdungsklasse (WGK) | 1 |
| UN-Transportnummer | UN1230 - class 3 - PG 2 - Methanol, solution |
| R-Sätze (R) | 11-23/24/25-39/23/24/25 |
| Toxizität | LD50 in male, female rats, male, female mice (mg/kg): 3619, 3509, 4358, 4258 orally865, 825, 830, 783 i.p.>5000 s.c. (Tsumagari) |
| Gefahrensymbole | F,T |
| Sicherheitshinweise (S) | 7-16-36/37-45 |
Anwendungen & Verwendung
Beschreibung
Etizolam is a potent thienodiazepine anxiolytic closely related to brotizolam. Pharmacologically, however, its profile most resembles that of diazepam.
Verwenden
Etilozam is a a thienodiazepine benzodiazepine derivative, and has amnesic, anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. Etizolam is an anxiolytic related to that of the classic benzodiazepines. Etizolam has effect on monoamine metabolism in brain. Etilozam can be used for the short-term treatment of insomnia, anxiety or panic attacks.