50-49-7 3-(10,11-二氢-5H-二苯并[b,f]氮杂卓-5-基)-N,N-二甲基丙-1-胺
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安全说明
毒害物质数据:50-49-7(Hazardous Substances Data) 毒性:A tertiary amine tricyclic antidepressant that is thought to exert its therapeutic effect by inhibiting the reuptake of serotonin and norepinephrine centrally. A major metabolite is N-desmethylimipramine (desipramine), also used as an antidepressant drug. Desipramine differs from imipramine in being a better blocker of norepinephrine, rather than serotonin, uptake. Side effects, including sedation and drowsiness, dry mouth, urinary retention, constipation, and orthostatic hypotension, are probably due to the anticholinergic, anti-α-adrenergic, and antihistaminergic receptor-blocking properties. Imipramine should not be used in conjunction with a monoamine oxidase inhibitor or other treatment that increases catecholamine concentrations (e.g., drugs containing sympathomimetic amines). Imipramine should be avoided in patients with cardiovascular disease or seizure disorder, or in those who may abuse alcohol, as imipramine lowers seizure threshold, can produce cardiovascular toxicity and may potentiate the effects of alcohol. Imipramine intoxication can include CNS abnormalities (e.g., drowsiness, stupor, coma, and extrapyramidal symptoms), cardiac arrhythmia, and respiratory depression. Children appear to be particularly vulnerable to the cardiotoxic and seizure-inducing effects of high doses of imipramine. The oral LD50 in female rats is 305 mg/kg.
用途与制备
主要作为医药中间体或原料药使用,具体用途需结合下游制剂进一步确定。
医药
由邻硝基甲苯经缩合、还原得2,2′-氨基联苄与1-氯-3-二甲氨基丙烷缩合、成盐制得。