Waldmeier P C, Delini-Stula A A
Eur J Pharmacol. 1979 May 15;55(4):363-73. doi: 10.1016/0014-2999(79)90110-9.
A study was made of the effects of serotonin uptake inhibition and receptor blockade on the increase in rat striatal homovanillic acid and 3,4-dihydroxyphenylacetic acid and on some behavioural responses induced by haloperidol. The serotonin uptake inhibitors CGP 6085 A (4-(5,6-dimethyl-2-benzofuranyl)-piperidine-HCl), citalopram (Lu 10-171), fluoxetine (Lilly 110140), and clomipramine potentiated the increase in striatal deaminated dopamine metabolites after the neuroleptic. In contrast, the serotonin antagonists methysergide, mianserin and cinanserin antagonized the acceleration of dopamine turnover induced by haloperidol. The catalepsy induced by this neuroleptic was potentiated by CGP 6085 A and citalopram. These 5-HT uptake inhibitors also potentiated the antagonism by haloperidol of apomorphine-induced stereotypies. These results seem to make it worthwhile to test a combination of haloperidol and a serotonin antagonist in schizophrenic patients to see whether the ratio of the therapeutic effect to the extrapyramidal side effects can be improved.
研究了血清素摄取抑制和受体阻断对大鼠纹状体高香草酸和3,4 - 二羟基苯乙酸增加的影响，以及对氟哌啶醇诱导的一些行为反应的影响。血清素摄取抑制剂CGP 6085 A（4 - (5,6 - 二甲基 - 2 - 苯并呋喃基)-哌啶 - HCl）、西酞普兰（Lu 10 - 171）、氟西汀（礼来110140）和氯米帕明增强了神经阻滞剂作用后纹状体脱氨基多巴胺代谢产物的增加。相反，血清素拮抗剂麦角新碱、米安色林和西那色林拮抗氟哌啶醇诱导的多巴胺周转加速。CGP 6085 A和西酞普兰增强了这种神经阻滞剂诱导的僵住症。这些5 - HT摄取抑制剂还增强了氟哌啶醇对阿扑吗啡诱导的刻板行为的拮抗作用。这些结果似乎表明，在精神分裂症患者中测试氟哌啶醇和血清素拮抗剂的组合，以观察治疗效果与锥体外系副作用的比例是否可以改善是值得的。
