Checkley S A, Thompson C, Burton S, Franey C, Arendt J
Psychopharmacology (Berl). 1985;87(1):116-8. doi: 10.1007/BF00431790.
In six normal male subjects the mydriatic effect of tyramine eye drops was inhibited by 1 day's treatment with desipramine and the (+)- but not the (-)-enantiomer of oxaprotiline. In the same experiment, the secretion of melatonin was increased after treatment with (+)- but not with (-)-oxaprotiline. The effects of (+)-oxaprotiline and of desipramine treatment were similar, as were those of (-)-oxaprotiline and placebo. These findings extend to clinical studies the demonstration in animal experiments of stereo-specificity for the effects of (+)- and (-)-oxaprotiline upon noradrenaline uptake. A comparison of the effects of the two enantiomers should provide an ideal strategy for studying effects of noradrenaline uptake blockade in clinical studies.
在6名正常男性受试者中,地昔帕明以及奥沙普替林的(+)-对映体(而非(-)-对映体)治疗1天可抑制酪胺滴眼液的散瞳作用。在同一实验中,(+)-奥沙普替林治疗后褪黑素分泌增加,而(-)-奥沙普替林治疗后则未增加。(+)-奥沙普替林和地昔帕明治疗的效果相似,(-)-奥沙普替林和安慰剂的效果也相似。这些发现将动物实验中(+)-和(-)-奥沙普替林对去甲肾上腺素摄取影响的立体特异性证明扩展到了临床研究。比较两种对映体的效果应为临床研究中去甲肾上腺素摄取阻断作用的研究提供理想策略。