Fuchs V, Coper H, Strauss S, Rommelspacher H
Naunyn Schmiedebergs Arch Pharmacol. 1986 Oct;334(2):133-7. doi: 10.1007/BF00505812.
Apomorphine-induced stereotypic behavior was investigated in rats treated with diazepam or haloperidol and with the combination of both drugs in a one day trial or subchronically. The drugs were administered via the drinking water. Diazepam dose-dependently reduced apomorphine stereotypies after the subchronic (6 days) but not after the acute treatment. Haloperidol suppressed apomorphine-induced stereotypic behavior dose-dependently after acute as well as after subchronic administration apparently without the development of tolerance. This discrepancy to other studies may be explained by the concomitant increase in maximum number of D2-receptors in the striatum. The apomorphine antagonistic effect of haloperidol was attenuated when the neuroleptic was administered subchronically in combination with the benzodiazepine. This finding was unexpected since both drugs reduced apomorphine-induced stereotypic behavior when administered alone. The further increase in maximum number of D2-receptors due to combined treatment with low doses of diazepam, suggesting a sort of "over adaptation", possibly explains the haloperidol-antagonistic action of diazepam in the behavioral experiments. Binding studies on dopamine (D1), 5-hydroxytryptamine (5-HT2) and benzodiazepine receptors revealed that modification of the apomorphine-induced stereotypies by the combined treatment with haloperidol and diazepam cannot be explained by interactions of the drugs at the level of the D1, 5-HT2 or benzodiazepine-receptors.
在一日试验或亚慢性试验中,研究了用安定或氟哌啶醇以及两种药物联合治疗的大鼠中阿扑吗啡诱导的刻板行为。药物通过饮用水给药。亚慢性(6天)给药后,安定剂量依赖性地减少了阿扑吗啡刻板行为,但急性治疗后没有。氟哌啶醇在急性和亚慢性给药后均剂量依赖性地抑制阿扑吗啡诱导的刻板行为,显然没有耐受性的发展。与其他研究的这种差异可能是由于纹状体中D2受体最大数量的同时增加。当抗精神病药物与苯二氮卓类药物亚慢性联合给药时,氟哌啶醇的阿扑吗啡拮抗作用减弱。这一发现出乎意料,因为两种药物单独给药时均能减少阿扑吗啡诱导的刻板行为。低剂量安定联合治疗导致D2受体最大数量进一步增加,提示一种“过度适应”,这可能解释了安定在行为实验中的氟哌啶醇拮抗作用。对多巴胺(D1)、5-羟色胺(5-HT2)和苯二氮卓受体的结合研究表明,氟哌啶醇和安定联合治疗对阿扑吗啡诱导的刻板行为的改变不能用药物在D1、5-HT2或苯二氮卓受体水平的相互作用来解释。