Somoza E, Bazán E, Galindo A
Neuropsychobiology. 1982;8(6):297-303. doi: 10.1159/000117915.
The binding of leu-enkephalin to synaptosome-enriched fractions prepared from rat whole brain has been measured in the presence and absence of haloperidol, chlorpromazine and chlozapine. All three neuroleptics produced a dose-dependent inhibition of the binding with inhibition constants of 33.7, 89.6, and 34.2 microM for haloperidol, chlorpromazine, and clozapine, respectively, and resulted in parabolic Hill plots suggestive of multiprocess modes of action rather than simple competitive or noncompetitive interactions. Except for the case of haloperidol, the inhibition constants are comparable to brain tissue levels of neuroleptics after chronic administration. This suggests that neuroleptic treatment may block a significant fraction of endogenous leu-enkephalin from reaching its CNS receptors.
在有和没有氟哌啶醇、氯丙嗪和氯氮平的情况下，已对亮氨酸脑啡肽与从大鼠全脑制备的富含突触体的组分的结合进行了测量。所有这三种抗精神病药物均产生了剂量依赖性的结合抑制作用，氟哌啶醇、氯丙嗪和氯氮平的抑制常数分别为33.7、89.6和34.2微摩尔，并且产生了抛物线形的希尔图，提示其作用模式为多过程模式，而非简单的竞争性或非竞争性相互作用。除氟哌啶醇外，抑制常数与长期给药后抗精神病药物在脑组织中的水平相当。这表明抗精神病药物治疗可能会阻止相当一部分内源性亮氨酸脑啡肽到达其中枢神经系统受体。
