Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
로페프라민
로페프라민 · Amplit · Leo 640 · Gamanil · Lopramine · Lofepramine · Lofepramine - Bio-X ? · Lofepramine in methanol
식별자 및 물리적 특성
| CAS No. | 23047-25-8 |
|---|---|
| 분자식 | C26H27ClN2O |
| 평균 분자량 | 419 g/mol |
| 단동위원소 질량 | 418.1811912 g/mol |
| SMILES | CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 |
| InChIKey | SAPNXPWPAUFAJU-UHFFFAOYSA-N |
| PubChem CID | 3947 |
| ChEMBL | CHEMBL87708 |
| ChEBI | CHEBI:47782 |
| EC No. | 245-396-8 |
| DTXSID | DTXSID2023220 |
| 현지명 | 로페프라민 |
화학 및 물리적 성질
| XLogP | 6.8 |
|---|---|
| 극성 표면적 | 23.6 |
| 수소 결합 공여자 수 | 0 |
| 수소 결합 수용자 수 | 3 |
| 회전 가능 결합 수 | 7 |
| 무거운 원자 수 | 30 |
| 형식 전하 | 0 |
| 복잡도 | 523 |
| LogP(분배 계수) | log Kow = 7.3 /Estimated/ |
| Color/Form | Crystals from methanol or acetone |
| 용해도 | In water, 1.4X10-2 mg/L @ 25 °C /Estimated/클로로포름(약간 용해됨), 메탄올(약간 용해됨) |
| Human Drugs | Pharmaceuticals |
| 녹는점 | 104-406 °C103-105°C |
| 증기압 | 1.5X10-9 mm Hg @ 25 °C /Estimated/0Pa at 25℃ |
| 헨리 상수 | Henry's Law constant = 2.0X10-11 atm-cu m/mol @ 25 °C /Estimated/ |
| Other Experimental Properties | Easily oxidized by air and other oxidizing agents to desipramine and p-chlorbenzoic acidMW: 455.43crystals from butanonemp: 152-154 °Csol in methanol, ethanol, chloroformpractically insol in water. /Hydrochloride/Hydroxyl radical reaction rate constant = 3.0X10-10 cu cm/molec-sec @ 25 °C /Estimated/ |
| 저장 조건 | Store at +4°C |
| 물리적 상태 | 고체 |
| 색상 | 밝은 노란색에서 밝은 베이지색까지 |
| 용해도 | 2.04mg/L at 25℃ |
| 안정성 | 솔루션이 불안정함 |
화학적 성질
Light Yellow Solid
안전 및 규제
| GHS 분류 | DangerH336 (100%): May cause drowsiness or dizziness [Warning Specific target organ toxicity, single exposureNarcotic effects]P260, P261, P264, P270, P271, P304+P340, P308+P316, P319, P321, P403+P233, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 2 reports by companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. |
|---|---|
| 규제 정보 | REACH registered substance: Lofepramine (EC: 245-396-8) |
| Special Reports | Lancaster SG, Gonzalez JPLofepramine: A Review of its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Efficacy in Depressive IllnessDrugs 37: 123-140 (1989) |
| Hazard Classes and Categories | STOT SE 3 (100%) |
| 상호 작용 | Lofepramine may potentiate alcohol sedation.Seizures or arrhythmias may be precipitated /SRP: by flumazenil/ in patients with a serious cyclic antidepressant overdose. /Flumazenil/ |
| Human Toxicity Excerpts | /SIGNS AND SYMPTOMS/ Lofepramine overdose in humans may be associated with tachycardia, hypertension, dry mouth, dilated pupils, ileus, blurred vision, dizziness, flushing, hypersalivation, muscle weakness, and vomiting. Only 1 of 55 cases studied had deep coma requiring ventilation. Hypotension, convulsion, and cardiac arrhythmias were not reported./SIGNS AND SYMPTOMS/ Twenty-one patients ingested between 0.14 and 4.9 g of lofepramine. Seven were asymptomatic (mean dose 1.85 g) and 14 patients had mild symptoms. One had a deep coma, suffered from respiration depression, and required ventilation for 36 hours. Five had mild hypertension, 5 had tachycardia, and several had anticholinergic symptoms. Hypotension, convulsion, and cardiac arrhythmias were not reported. When lofepramine was ingested with other drugs, hypotension, arrhythmias, and coma were observed. |
| Antidote and Emergency Treatment | Measures such as hemodialysis and hemoperfusion are not likely to be of value in view of the high degree of protein binding and the extensive volume of distribution.Treatment of lofepramine overdose is largely symptomatic and supportive. Intubation and ventilation should be provided where indicated. |
용도
개요
Lofepramine is a first generation tricyclic antidepressant that is extensively metabolized to desipramine. It potently inhibits serotonin and norepinephrine transporters (Kds = 70 and 5.4 nM, respectively) and less potently antagonizes serotonin, histamine, and muscarinic receptors.