HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Camazepam
B-5333 · Albego · SB-5833 · KTH-497 · camazepam · dl-CaMazepaM · RaceMic CaMazepaM · camazepam USP/EP/BP
Identifikatoren & physikalische Daten
| CAS No. | 36104-80-0 |
|---|---|
| Summenformel | C19H18ClN3O3 |
| Durchschnittliche Molmasse | 371,8 g/mol |
| Monoisotopische Masse | 371,1036691 g/mol |
| SMILES | CN(C)C(=O)OC1N=C(c2ccccc2)c2cc(Cl)ccc2N(C)C1=O |
| InChIKey | PXBVEXGRHZFEOF-UHFFFAOYSA-N |
| PubChem CID | 37367 |
| ChEMBL | CHEMBL1095282 |
| ChEBI | CHEBI:135570 |
| EC No. | 252-866-6 |
| DTXSID | DTXSID50865803 |
| Lokaler Name | Camazepam |
Chemische & physikalische Eigenschaften
| XLogP | 2,8 |
|---|---|
| Polarare Oberfläche (TPSA) | 62,2 |
| H-Brücken-Donoren | 0 |
| H-Brücken-Akzeptoren | 4 |
| Frei drehbare Bindungen | 3 |
| Schwere Atome | 26 |
| Formalladung | 0 |
| Komplexität | 574 |
| Arzneimittel | DEA NFLIS-Drug Category -> BenzodiazepinesDEA Schedule IV Controlled Substance -> Depressants |
| Human Drugs | Pharmaceuticals |
| Schmelzpunkt | 173-174173-174° |
| Siedepunkt | 568.3±50.0 °C(Predicted) |
| Dichte | 1.2902 (rough estimate) |
| Brechungsindex | 1.6470 (estimate) |
| Löslichkeit | Chloroform (Slightly), Methanol (Slightly) |
| Aggregatzustand | Solid |
| pKa (Säurekonstante) | 2.21±0.50(Predicted) |
| Farbe | White to Off-White |
| Stabilität | Light Sensitive |
Sicherheit & Vorschriften
| Regulatorische Informationen | DEA schedule IV controlled substance |
|---|---|
| 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. |
| Expositionspfade | Almost completely absorbed into the bloodstream after oral administration. 90% bioavailability can be achieved in humans. |
| Toxizitätsübersicht | Camazepam has been shown to bind competitively to benzodiazepine receptors in the brain with a relatively low affinity in animal models. This binding of benzodiazepine receptors by camazepam and its active metabolites is responsible for its anticonvulsant effects. Notably, only three metabolites were shown to exert anticonvulsant activity, temazepam, oxazepam, and hydroxy camazepam. The anxiolytic properties of camazepam are also attributed to their ability to bind benzodiazepine receptors, also known as GABA receptors. When benzodiazepines bind to GABA receptors they increase the efficiency with which the inhibitory neurotransmitter GABA binds. |
| Carcinogen Classification | No indication of carcinogenicity to humans (not listed by IARC). |
| UN-Transportnummer | 3249 |
| Toxizität | LD50 in mice, rats (mg/kg): 970, >4000 orally (Ferrini) |
Anwendungen & Verwendung
Verwenden
Anxiolytic. Controlled substance (depressant).