Setler P, Sarau H, McKenzie G
Eur J Pharmacol. 1976 Sep;39(1):117-26. doi: 10.1016/0014-2999(76)90119-9.
In a series of pharmacological tests the ability of 0.6 mg/kg of the anticholinergic scopolamine to decrease the effectiveness of the neuroleptic heloperidol varied widely. Most severely attenuated was production of catalepsy followed in order of decreasing interference by inhibition of amphetamine-induced rotation, inhibition of amphetamine- or apomorphine-induced stereotyped behavior, inhibition of conditioned avoidance responding and lastly attenuation of the haloperidol-induced increase in striatal HVA. By use of such a relatively low dose of scopolamine the behavioral effects of heloperidol were dissociated from effects on dopamine turnover in the striatum. If behavioral tests in animals can be related to the clinical effects of neuroleptic drugs, those effects of haloperidol severely reduced by scopolamine may be related to extrapyramidal effects.
在一系列药理试验中,0.6毫克/千克的抗胆碱能药物东莨菪碱降低抗精神病药物氟哌啶醇有效性的能力差异很大。其中,对僵住症的产生抑制最为严重,其次是按干扰程度递减顺序排列的:抑制苯丙胺诱导的旋转、抑制苯丙胺或阿扑吗啡诱导的刻板行为、抑制条件性回避反应,最后是减弱氟哌啶醇诱导的纹状体高香草酸(HVA)增加。通过使用相对低剂量的东莨菪碱,氟哌啶醇的行为效应与对纹状体多巴胺周转的效应得以分离。如果动物行为试验能与抗精神病药物的临床效应相关联,那么东莨菪碱严重降低的氟哌啶醇那些效应可能与锥体外系效应有关。