Sayers A C, Bürki H R, Ruch W, Asper H
Psychopharmacology (Berl). 1976 Dec 21;51(1):15-22. doi: 10.1007/BF00426315.
The effects of haloperidol, alone and in combination with atropine, were compared with the effects of clozapine, alone and in combination with physostigmine, in a variety of tests commonly used to characterize neuroleptic compounds. It was found that clozapine in combination with physostigmine did not present the profile of activity of a classical neuroleptic agent; neither did haloperidol in combination with atropine present that of clozapine. In fact, some effects of haloperidol (catalepsy) were antagonized by atropine, while others (induction of striatal DA-receptor hypersensitivity) were enhanced. It is concluded that the interaction between dopaminergic and cholinergic systems in the striatum is highly complex, and that a neuroleptic possessing both potent DA-receptor blocking and muscarinic anticholinergic activity, while being less likely to cause parkinsonism in patients, would be more likely to induce tardive dyskinesias.
在常用于表征抗精神病化合物的各种测试中，比较了单独使用氟哌啶醇及其与阿托品联合使用的效果，以及单独使用氯氮平及其与毒扁豆碱联合使用的效果。结果发现，氯氮平与毒扁豆碱联合使用时，并未呈现出经典抗精神病药物的活性特征；氟哌啶醇与阿托品联合使用时也未呈现出氯氮平的活性特征。事实上，阿托品可拮抗氟哌啶醇的某些作用（僵住症），而另一些作用（纹状体多巴胺受体超敏反应的诱导）则增强。得出的结论是，纹状体中多巴胺能系统与胆碱能系统之间的相互作用非常复杂，并且一种兼具强效多巴胺受体阻断和毒蕈碱抗胆碱能活性的抗精神病药物，虽然在患者中引起帕金森症的可能性较小，但更有可能诱发迟发性运动障碍。
