Borison R L
J Clin Psychiatry. 1985 Apr;46(4 Pt 2):25-8.
Data on the pharmacologic dissimilarities of antipsychotic drugs, and the clinical consequences of these differences, are reviewed briefly, with an emphasis on the interaction of these drugs with dopaminergic systems. Although differential anticholinergic activity has been proposed as an explanation for purported differences in the incidence of anticholinergic side effects of various neuroleptics, a more plausible explanation relates to site specificity. The so-called atypical neuroleptics show far less dopamine blocking potency in human striatum compared to haloperidol, with equal receptor blocking potency in the limbic system. The model of site-specificity will be of major importance in the development of future antipsychotics, with the goal of decreasing the incidence of side effects.
本文简要综述了抗精神病药物的药理学差异数据以及这些差异的临床后果，重点关注这些药物与多巴胺能系统的相互作用。尽管有人提出不同的抗胆碱能活性可解释各种抗精神病药物抗胆碱能副作用发生率的所谓差异，但更合理的解释与位点特异性有关。与氟哌啶醇相比，所谓的非典型抗精神病药物在人类纹状体中的多巴胺阻断效力要低得多，而在边缘系统中的受体阻断效力相同。位点特异性模型在未来抗精神病药物的研发中将具有重要意义，目标是降低副作用的发生率。
