Di Renzo G, Amoroso S, Taglialatela M, Canzoniero L, Basile V, Fatatis A, Annunziato L
Department of Pharmacology, 2nd School of Medicine, Naples, Italy.
Eur J Pharmacol. 1989 Mar 21;162(2):371-3. doi: 10.1016/0014-2999(89)90302-6.
The present study was undertaken to characterize the type of serotonin (5-HT) receptors involved in the control of prolactin (PRL) secretion in male rats. d-Fenfluramine (10 mg/kg i.p.), a potent 5-HT releaser and quipazine, (20 mg/kg i.p.) a 5-HT agonist, caused a marked increase in serum PRL levels. Ritanserin (200 micrograms/kg i.p.), a specific antagonist of 5-HT2 receptors, administered 1 h before the administration of d-fenfluramine or quipazine, completely prevented the PRL-releasing effect of these drugs. Furthermore, the administration of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH DPAT) (1.5, 3 and 6 mg/kg i.p.), a compound considered to be a prototypical 5-HT1A agonist, failed to induce any change in serum PRL levels. The same lack of effect on PRL secretion was observed after the administration of 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridin-4-yl)-1-H-indole (RU 24969) (1, 3 and 10 mg/kg i.p.), a compound which has been shown to possess a higher selectivity for 5-HT1B receptor subtypes than for 5-HT1A subtypes. These results suggest that 5-HT receptors involved in the control of PRL secretion are of the 5-HT2 type.
本研究旨在确定参与雄性大鼠催乳素(PRL)分泌调控的血清素(5-羟色胺,5-HT)受体类型。强效5-HT释放剂右芬氟拉明(10 mg/kg腹腔注射)和5-HT激动剂喹哌嗪(20 mg/kg腹腔注射)可使血清PRL水平显著升高。在给予右芬氟拉明或喹哌嗪前1小时腹腔注射5-HT2受体特异性拮抗剂利坦色林(200微克/千克),可完全阻断这些药物的PRL释放效应。此外,给予被认为是典型5-HT1A激动剂的8-羟基-2-(二正丙基氨基)四氢萘(8-OH DPAT)(1.5、3和6 mg/kg腹腔注射),未能引起血清PRL水平的任何变化。给予5-甲氧基-3-(1,2,3,6-四氢-4-吡啶基)-1-H-吲哚(RU 24969)(1、3和10 mg/kg腹腔注射)后,对PRL分泌也无影响,该化合物对5-HT1B受体亚型的选择性高于对5-HT1A亚型。这些结果表明,参与PRL分泌调控的5-HT受体为5-HT2型。