Nefazodone Hydrochloride
TFA ≥Serazone · NEFAZODONE · Isatin ≥Indole ≥BMY 13754-1 · Hecameg ≥>=98% (HPLC) · Chromone ≥Piperine &ge
Identifikatoren & physikalische Daten
| CAS No. | 82752-99-6 |
|---|---|
| Summenformel | C25H33Cl2N5O2 |
| Durchschnittliche Molmasse | 506,5 g/mol |
| Monoisotopische Masse | 505,20113066 g/mol |
| SMILES | CCc1nn(CCCN2CCN(c3cccc(Cl)c3)CC2)c(=O)n1CCOc1ccccc1.Cl |
| InChIKey | DYCKFEBIOUQECE-UHFFFAOYSA-N |
| PubChem CID | 54911 |
| ChEMBL | CHEMBL1200492 |
| ChEBI | CHEBI:7495 |
| EC No. | 875-483-1 |
| DTXSID | DTXSID8046088 |
Chemische & physikalische Eigenschaften
| Polarare Oberfläche (TPSA) | 51,6 |
|---|---|
| H-Brücken-Donoren | 1 |
| H-Brücken-Akzeptoren | 5 |
| Frei drehbare Bindungen | 10 |
| Schwere Atome | 34 |
| Formalladung | 0 |
| Komplexität | 649 |
| Human Drugs | FDA approved drugs -> Active ingredient |
| Schmelzpunkt | 186-188°C |
| Lagerbedingungen | Inert atmosphere,Room Temperature |
| Löslichkeit | DMSO: ~11 mg/mL at 60 °C |
| Aggregatzustand | solid |
| Farbe | white |
| Merck | 14,6438 |
| InChI | 1S/C25H32ClN5O2.ClH/c1-2-24-27-31(25(32)30(24)18-19-33-23-10-4-3-5-11-23)13-7-12-28-14-16-29(17-15-28)22-9-6-8-21(26)20-22/h3-6,8-11,20H,2,7,12-19H2,1H3 |
| InChIKey | DYCKFEBIOUQECE-UHFFFAOYSA-N |
| SMILES | O=C1N(CCCN2CCN(C3=CC=CC(Cl)=C3)CC2)N=C(CC)N1CCOC4=CC=CC=C4.Cl |
| CAS Datenbank | 82752-99-6(CAS DataBase Reference) |
Sicherheit & Vorschriften
| GHS-Einstufung | WarningH315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]P261, P264, P264+P265, P271, P280, P302+P352, P304+P340, P305+P351+P338, P319, P321, P332+P317, P337+P317, P362+P364, P403+P233, P405, and P501 (click each P-code to see the statement)The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory. |
|---|---|
| Regulatorische Informationen | Nefazodone hydrochloride: Does not have an individual approval but may be used under an appropriate group standard |
| Hazard Classes and Categories | Skin Irrit. 2 (100%) |
| Treatment | Treatment should consist of those general measures employed in the management of overdosage with any antidepressant. Ensure an adequate airway, oxygenation, and ventilation. Monitor cardiac rhythm and vital signs. General supportive and symptomatic measures are also recommended. Induction of emesis is not recommended. Gastric lavage with a large-bore orogastric tube with appropriate airway protection, if needed, may be indicated if performed soon after ingestion, or in symptomatic patients. Activated charcoal should be administered. Due to the wide distribution of nefazodone in body tissues, forced diuresis, dialysis, hemoperfusion, and exchange transfusion are unlikely to be of benefit. No specific antidotes for nefazodone are known. (L1712) |
| Gesundheitliche Auswirkungen | Serious side effects include an allergic reaction, fainting, or painful/prolonged erection. [Wikipedia] |
| Expositionspfade | Nefazodone is rapidly and completely absorbed. Its absolute bioavailability is low (about 20%). |
| Toxizitätsübersicht | Within the serotonergic system, nefazodone acts as an antagonist at type 2 serotonin (5-HT<sub>2</sub>) post-synaptic receptors and, like fluoxetine-type antidepressants, inhibits pre-synaptic serotonin (5-HT) reuptake. These mechanisms increase the amount of serotonin available to interact with 5-HT receptors. Within the noradrenergic system, nefazodone inhibits norepinephrine uptake minimally. Nefazodone also antagonizes alpha(1)-adrenergic receptors, producing sedation, muscle relaxation, and a variety of cardiovascular effects. Nefazodone's affinity for benzodiazepine, cholinergic, dopaminergic, histaminic, and beta or alpha(2)-adrenergic receptors is not significant. |
Anwendungen & Verwendung
Beschreibung
Nefazodone, a second generation trazodone type antidepressant, was launched in Canada. Nefazodone acts as both a potent 5-HT2 receptor antagonist and as a serotonin (5-HT) reuptake inhibitor. This combination effect appears to enhance 5-HTIA-mediated neurotransmission. Distinct from the first generation agents such as tricyclic antidepressants, nefazodone has very selective serotonergic effects with negligible affinity for cholinergic and histamine receptors, and low affinity for a1 -adrenergic receptors. Therefore, it has a superior toxicity profile that does not produce agitation, insomnia, and lacks cardiac side effects.
Verwenden
A selective serotonin 5-HT2 receptor antagonist. A novel antidepressant that shows no cardiac toxicity or anticholinergic activity common with tricyclic antidepressants.