Lingjaerde O
Acta Psychiatr Scand Suppl. 1985;320:10-9. doi: 10.1111/j.1600-0447.1985.tb08069.x.
Inhibition of active serotonin uptake into neurones and platelets is a common effect of tricyclic and related antidepressants, and has been regarded as one of the more important mechanisms of action of such drugs. However, as is shown in this survey, the antidepressants vary widely in their potency as inhibitors of platelet serotonin uptake, and they also differ in the type of inhibition kinetics, from purely competitive to mixed competitive/noncompetitive. The therapeutic relevance of this effect is discussed. Serotonin uptake inhibition seems to be one of several mechanisms for obtaining the required normalization of monoamine dysfunction in depression. Analysis of efflux from platelets preloaded with a moderate amount of 14C-serotonin provides information on the storage and compartmentation of serotonin in the platelets, and on the rate of efflux from the different compartments. When present during the preloading phase, some antidepressants seem to produce a relative increase in serotonin in the granular storage compartment when compared to the smaller cytoplasmic compartment. This effect is in some respects opposite to that exerted by reserpine, and possibly may be pharmacologically relevant.
抑制神经元和血小板对活性5-羟色胺的摄取是三环类及相关抗抑郁药的常见作用，并且这一作用被视为这类药物更重要的作用机制之一。然而，正如本次调查所示，这些抗抑郁药作为血小板5-羟色胺摄取抑制剂的效力差异很大，而且它们在抑制动力学类型上也有所不同，从单纯竞争性抑制到混合竞争性/非竞争性抑制。文中讨论了这一作用的治疗相关性。5-羟色胺摄取抑制似乎是使抑郁症中单胺功能障碍恢复正常所需的几种机制之一。对预先加载适量14C-5-羟色胺的血小板的流出情况进行分析，可提供有关5-羟色胺在血小板中的储存和区室化信息，以及不同区室的流出速率信息。在预加载阶段存在某些抗抑郁药时，与较小的细胞质区室相比，颗粒储存区室中的5-羟色胺似乎会相对增加。这一作用在某些方面与利血平的作用相反，并且可能在药理学上具有相关性。
