米安色林对映体及代谢产物的潜在治疗作用。
The potential therapeutic role of the enantiomers and metabolites of mianserin.
作者信息
Pinder R M, Van Delft A M
出版信息
Br J Clin Pharmacol. 1983;15 Suppl 2(Suppl 2):269S-276S. doi: 10.1111/j.1365-2125.1983.tb05875.x.
Abstract
1 S(+)-mianserin is the more potent enantiomer of mianserin in pharmacological tests indicative for antidepressant activity. Pharmacological tests indicative for sedation suggest that sedative effects are similar for mianserin and its enantiomers. 2 Of the three compounds, mianserin had the optimal therapeutic ratio of antidepressant-like activity versus sedative properties when assessed by computerised EEG in healthy volunteers participating in a double-blind placebo-controlled single dose trial. 3 Of the known metabolites, desmethylmianserin and 8-hydroxymianserin substantially retain pharmacological properties indicative for antidepressant activity but are less active than mianserin in tests indicative for sedation. Mianserin-N-oxide is inactive or only weakly active in most pharmacological tests. 4 Desmethylmianserin occurs in human plasma after both single and multiple dosage to an extent of about one-third that of mianserin. 5 Mianserin has optimal efficacy as the racemate. Desmethylmianserin and 8-hydroxymianserin are pharmacologically active metabolites and may contribute to the overall antidepressant effects of mianserin.
摘要
- S(+)-米安色林是米安色林在指示抗抑郁活性的药理试验中活性更强的对映体。指示镇静作用的药理试验表明，米安色林及其对映体的镇静作用相似。2. 在参与双盲安慰剂对照单剂量试验的健康志愿者中，通过计算机脑电图评估时，三种化合物中米安色林在抗抑郁样活性与镇静特性方面具有最佳治疗指数。3. 在已知代谢物中，去甲米安色林和8-羟基米安色林基本上保留了指示抗抑郁活性的药理特性，但在指示镇静的试验中活性低于米安色林。米安色林-N-氧化物在大多数药理试验中无活性或活性微弱。4. 单次和多次给药后，去甲米安色林在人血浆中的含量约为米安色林的三分之一。5. 米安色林作为外消旋体具有最佳疗效。去甲米安色林和8-羟基米安色林是具有药理活性的代谢物，可能对米安色林的整体抗抑郁作用有贡献。
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1
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Neuropharmacology. 1980 Jul;19(7):657-61. doi: 10.1016/0028-3908(80)90040-4.
2
Neuropharmacological properties of amitriptyline, nortriptyline and their metabolites.
Acta Pharmacol Toxicol (Copenh). 1980 Jul;47(1):53-7. doi: 10.1111/j.1600-0773.1980.tb02025.x.
3
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Naunyn Schmiedebergs Arch Pharmacol. 1980 Apr;311(3):255-61. doi: 10.1007/BF00569405.
4
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Encephale. 1981;7(4 Suppl):371-80.
5
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7
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8
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9
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