Marek G J, Li A, Seiden L S
University of Chicago, Department of Pharmacological and Physiological Sciences, IL 60637.
Eur J Pharmacol. 1988 Nov 22;157(2-3):183-8. doi: 10.1016/0014-2999(88)90381-0.
(+)-Oxaprotiline (1.25-10 mg/kg), a highly selective and stereospecifically acting norepinephrine (NE) uptake inhibiting drug, increased the reinforcement rate, decreased the response rate, and enhanced temporal discrimination in rats performing under a differential-reinforcement-of-low-rate 72-s schedule of reinforcement similar to other antidepressant drugs. (-)-Oxaprotiline did not affect the reinforcement rate, response rate or temporal discrimination. Since the most prominent known difference between the oxaprotiline enantiomers is the greater potency for inhibition of norepinephrine (NE) uptake by the (+) enantiomer, the effects of (+)-oxaprotiline in the present studies is probably due to inhibition of NE or epinephrine uptake. The present work also predicts that the therapeutic effects of oxaprotiline in the treatment of affective disorders is due to the (+) enantiomer.
（+）-奥沙普明（1.25 - 10毫克/千克）是一种高度选择性且具有立体特异性作用的去甲肾上腺素（NE）摄取抑制药物，与其他抗抑郁药物类似，在大鼠按照低速率72秒强化差异强化程序进行操作时，它提高了强化率，降低了反应率，并增强了时间辨别能力。（-）-奥沙普明对强化率、反应率或时间辨别能力没有影响。由于奥沙普明对映体之间最显著的已知差异是（+）对映体抑制去甲肾上腺素（NE）摄取的效力更强，因此本研究中（+）-奥沙普明的作用可能是由于抑制了NE或肾上腺素的摄取。本研究还预测，奥沙普明在治疗情感障碍中的治疗作用归因于（+）对映体。
