Simonovic M, Gudelsky G A, Meltzer H Y
J Neural Transm. 1984;59(2):143-9. doi: 10.1007/BF01255412.
8-OH- DPAT (8-hydroxy-2-[di-n-propylamino] tetralin) is a novel aminotetralin derivative which has been proposed to be a serotonin (5-HT) agonist devoid of dopamine agonist effects. We now report that the administration of 8-OH- DPAT , like known 5-HT agonists, produced a rapid elevation of serum prolactin concentrations in male rats. The prolactin response to 8-OH- DPAT , like that induced by other 5-HT agonists, was greatly potentiated in animals pretreated with the tryptophan hydroxylase inhibitor, para-chlorophenylalanine. However, the 8-OH- DPAT -induced elevation of serum prolactin concentrations in untreated rats was not dose-dependent and was modest in magnitude compared to that produced by known 5-HT agonists. In contrast to the stimulatory effects of 8-OH- DPAT on prolactin secretion in vivo 8-OH- DPAT suppressed the secretion of prolactin from anterior pituitary tissue in vitro, and this effect was blocked by haloperidol. The results of the present study are supportive of the view that 8-OH- DPAT has dopamine agonist, as well as 5-HT agonist, properties.
8-羟基-2-[二正丙基氨基]四氢萘（8-OH-DPAT）是一种新型氨基四氢萘衍生物，被认为是一种无多巴胺激动剂作用的血清素（5-HT）激动剂。我们现在报告，与已知的5-HT激动剂一样，给雄性大鼠注射8-OH-DPAT会导致血清催乳素浓度迅速升高。与其他5-HT激动剂诱导的情况一样，用色氨酸羟化酶抑制剂对氯苯丙氨酸预处理的动物中，对8-OH-DPAT的催乳素反应大大增强。然而，在未处理的大鼠中，8-OH-DPAT诱导的血清催乳素浓度升高不依赖剂量，与已知的5-HT激动剂产生的升高幅度相比适中。与8-OH-DPAT在体内对催乳素分泌的刺激作用相反，8-OH-DPAT在体外抑制垂体前叶组织的催乳素分泌，且这种作用被氟哌啶醇阻断。本研究结果支持8-OH-DPAT具有多巴胺激动剂以及5-HT激动剂特性这一观点。
