Gnirss F A
Psychopathology. 1986;19 Suppl 2:231-8. doi: 10.1159/000285161.
In the context of the questions under discussion here, three findings from this study should be briefly emphasised: Neurophysiological parameters investigated in healthy subjects receiving single doses of the two enantiomers of oxaprotiline in an acute experiment, performed in the sleep laboratory under defined conditions, revealed marked qualitative and quantitative differences between the effects of these enantiomers. Since the two enantiomers are practically devoid of any anticholinergic or antiserotonergic effect and display similar antihistaminic and sedative-antiaggressive activity, it is reasonable to assume that the differences in their effects on the sleep parameters measured are attributable to the difference in their pharmacodynamic profiles with respect to inhibition of noradrenaline uptake. REM sleep parameters correlate significantly with the effect of the d-(+)-enantiomer, i.e. with its selective effect on inhibition of noradrenaline uptake.
在本文所讨论问题的背景下,本研究的三项发现应予以简要强调:在睡眠实验室特定条件下对健康受试者进行的急性实验中,给予单剂量奥沙普明两种对映体后所研究的神经生理参数显示,这些对映体的作用在性质和数量上存在显著差异。由于这两种对映体几乎没有任何抗胆碱能或抗5-羟色胺能作用,且表现出相似的抗组胺和镇静抗攻击活性,因此可以合理推测,它们对所测量睡眠参数的作用差异归因于其在抑制去甲肾上腺素摄取方面的药效学特征差异。快速眼动睡眠参数与d-(+)-对映体的作用显著相关,即与其对抑制去甲肾上腺素摄取的选择性作用相关。