Bacopoulos N G
J Pharmacol Exp Ther. 1981 Dec;219(3):708-14.
The stereospecific binding sites of [3H]spiroperidol in frontal cortical regions of the rat brain have a higher affinity for serotonin than they do for dopamine, although the reverse relative affinity is observed in the caudate nucleus and in mesolimbic regions. The antipsychotic butyrophenones haloperidol and butaclamol compete with comparably high affinities for [3H]spiroperidol binding sites in all of the above brain regions. Both butyrophenones accelerated dopamine turnover in these three brain regions without altering serotonin turnover. A chronic treatment regimen with fluphenazine which induced tolerance to the metabolic effects of haloperidol in all three brain regions also induced tolerance to its behavioral effects. The number of binding sites of [3H]spiroperidol were increased in the caudate nucleus and mesolimbic regions but not in the frontal cortex of tolerant animals. These results are consistent with the hypothesis that [3H]spiroperidol interacts with a serotonergic site in the frontal cortex. However, the in vitro interaction of antipsychotic drugs with this receptor does not seem to be related to their acute or chronic effects on neurotransmitter function in the frontal cortex in vivo.
[3H]螺哌啶醇在大鼠脑额叶皮质区域的立体特异性结合位点对5-羟色胺的亲和力高于对多巴胺的亲和力，尽管在尾状核和中脑边缘区域观察到的相对亲和力情况相反。抗精神病药物氟哌啶醇和布他拉莫在上述所有脑区中，以相当高的亲和力与[3H]螺哌啶醇结合位点竞争。这两种丁酰苯类药物在这三个脑区均加速了多巴胺的周转，而未改变5-羟色胺的周转。用氟奋乃静进行的慢性治疗方案，在所有三个脑区中诱导了对氟哌啶醇代谢作用的耐受性，同时也诱导了对其行为效应的耐受性。在产生耐受性的动物的尾状核和中脑边缘区域，[3H]螺哌啶醇的结合位点数量增加，但在额叶皮质中未增加。这些结果与[3H]螺哌啶醇与额叶皮质中的5-羟色胺能位点相互作用的假说一致。然而，抗精神病药物与该受体的体外相互作用似乎与其在体内对额叶皮质神经递质功能的急性或慢性影响无关。
