Ogren S O, Ferré S, Schwarcz R, Fuxe K
Department of Neuroscience, Karolinska Institute, Stockholm, Sweden.
Neurosci Lett. 1997 Aug 22;232(1):21-4. doi: 10.1016/s0304-3940(97)00564-8.
Difference in striatal dopamine D2 receptors and in spontaneous and theophylline-induced motor activity in rats withdrawn (for 72 h) from prolonged treatment with haloperidol or clozapine were studied. Haloperidol but not clozapine pretreatment increased the binding of the dopamine D2 antagonist [3H]raclopride in striatal membrane preparations, due to an increased number of striatal dopamine D2 receptors (Bmax) without changes in affinity (Kd). Haloperidol induced a significant increase (in motility and locomotion) and clozapine a decrease (in locomotion) of the spontaneous motor activity. Haloperidol but not clozapine pretreatment was associated with a stronger theophylline-induced motor activation. These results suggest that prolonged treatment with typical but not with atypical antipsychotics are associated with adaptive changes at both dopamine and adenosine receptors.
研究了从长期使用氟哌啶醇或氯氮平治疗中撤药（72小时）的大鼠纹状体多巴胺D2受体以及自发和茶碱诱导的运动活动的差异。氟哌啶醇而非氯氮平预处理增加了纹状体膜制剂中多巴胺D2拮抗剂[3H]雷氯必利的结合，这是由于纹状体多巴胺D2受体数量增加（Bmax）而亲和力（Kd）无变化。氟哌啶醇使自发运动活动显著增加（运动性和活动能力方面），氯氮平则使其降低（活动能力方面）。氟哌啶醇而非氯氮平预处理与更强的茶碱诱导的运动激活相关。这些结果表明，典型抗精神病药物而非非典型抗精神病药物的长期治疗与多巴胺和腺苷受体的适应性变化有关。
