Hyttel J
Psychopharmacology (Berl). 1977 Jan 31;51(2):205-7. doi: 10.1007/BF00431742.
The changes in 14C-dopamine accumulation formed from 14C-tyrosine in mice after treatment with three neuroleptics, cis (Z)-flupenthixol, fluphenazine, and haloperidol, were followed for 6 days. The neuroleptics all changed DA synthesis rate in the same way, initially causing an increase which was followed by a decrease after approximately 3 days. The results are compared with pharmacological results (Christensen et al., 1976) and there seems to be a very close correlation between receptor blockade and increase in DA synthesis on the one hand and on the other hand receptor supersensitivity and decrease in DA synthesis, as was also shown previously for teflutixol (Hyttel, 1975). It is concluded that the changes in receptor activity are always followed by compensatory changes in DA synthesis rate.
在用三种抗精神病药物顺式(Z)-氟哌噻吨、氟奋乃静和氟哌啶醇治疗小鼠后,对由14C-酪氨酸形成的14C-多巴胺积累变化进行了6天的跟踪研究。所有抗精神病药物均以相同方式改变多巴胺合成速率,最初导致增加,约3天后则下降。将这些结果与药理学结果(克里斯蒂安森等人,1976年)进行比较,一方面受体阻断与多巴胺合成增加之间,另一方面受体超敏反应与多巴胺合成减少之间似乎存在非常密切的相关性,这一点先前在替氟噻吨的研究中也已得到证实(许特尔,1975年)。得出的结论是,受体活性的变化总是伴随着多巴胺合成速率的代偿性变化。