Kubota M, Ueno K, Yamano M, Kitagawa H
Laboratory of Biochemical Pharmacology & Biotoxicology, Faculty of Pharmaceutical Sciences, Chiba University, Japan.
Yakubutsu Seishin Kodo. 1989 Sep;9(3):289-92.
It has been known that many antidepressant drugs which have serotonin (5-HT) antagonistic activities and 5-HT antagonists can induce the reduction of 5-HT2 receptor binding by their acute or successive administration. We investigated the effects of repeated treatment with 5-HT agonists on 5-HT2 receptors in rat cerebral cortex. We used citalopram as selective 5-HT uptake inhibitor, 5-hydroxytryptophan as 5-HT precursor, and 5-methoxy-N,N'-dimethyltryptamine as 5-HT2 agonist. The 5-HT2 receptor density was decreased by repeated treatment with these respective drugs. So it may be supposed that the reduction of 5-HT2 receptor binding is induced not only by 5-HT antagonists but also by 5-HT agonists.
已知许多具有5-羟色胺(5-HT)拮抗活性的抗抑郁药和5-HT拮抗剂,通过急性或连续给药可诱导5-HT2受体结合减少。我们研究了5-HT激动剂重复治疗对大鼠大脑皮层5-HT2受体的影响。我们使用西酞普兰作为选择性5-HT摄取抑制剂,5-羟色氨酸作为5-HT前体,5-甲氧基-N,N'-二甲基色胺作为5-HT2激动剂。用这些各自的药物重复治疗可降低5-HT2受体密度。因此可以推测,5-HT2受体结合减少不仅是由5-HT拮抗剂引起的,也是由5-HT激动剂引起的。