Gronier B, Jeanningros R
Unité de Psychiatrie Biologique, CNRS, Faculté de Médecine, Marseille, France.
Fundam Clin Pharmacol. 1992;6(2):89-95. doi: 10.1111/j.1472-8206.1992.tb00099.x.
The effect of chronic treatment with amineptine (200 mg daily), a tricyclic antidepressant drug selectively blocking dopamine uptake, on 3H-imipramine binding, was investigated in platelets of major depressed patients in conjunction with changes in clinical state. Before treatment, depressed patients had a significantly lower Bmax (P less than 0.01) than age- and gender-matched healthy controls. After only 1 week of amineptine administration, Bmax values increased significantly (P less than 0.01) and reached the control value concomitantly with a large and significant clinical improvement (P less than 0.01). After 1 month, Bmax was still significantly different from the pretreatment value (P less than 0.05), and not significantly different from the control value, while the improvement in clinical status persisted. No significant changes in Kd values were observed during treatment. We also verified that amineptine did not displace 3H-imipramine binding from platelets either in depressed or in control subjects. The results show that the successful treatment with amineptine, an antidepressant drug devoid of affinity for the tritiated imipramine platelet binding site, can rapidly lead to its density normalization.
研究了选择性阻断多巴胺摄取的三环类抗抑郁药阿米替林（每日200毫克）长期治疗对重度抑郁症患者血小板中3H-丙咪嗪结合的影响，并结合临床状态的变化进行观察。治疗前，抑郁症患者的Bmax显著低于年龄和性别匹配的健康对照者（P<0.01）。仅给予阿米替林1周后，Bmax值显著升高（P<0.01），并达到对照值，同时临床症状有显著改善（P<0.01）。1个月后，Bmax仍与治疗前值有显著差异（P<0.05），与对照值无显著差异，而临床状态的改善持续存在。治疗期间未观察到Kd值有显著变化。我们还证实，阿米替林在抑郁症患者或对照受试者中均未取代血小板上的3H-丙咪嗪结合。结果表明，对与氚化丙咪嗪血小板结合位点无亲和力的抗抑郁药阿米替林的成功治疗可迅速使其密度恢复正常。
