Nordström A L, Farde L, Halldin C
Department of Psychiatry and Psychology, Karolinska Hospital, Stockholm, Sweden.
Psychopharmacology (Berl). 1993;110(3):365-7. doi: 10.1007/BF02251294.
The clinical benefit of the atypical antipsychotic drug clozapine may be related to a combined effect on D2 and 5-HT2 receptors. To examine the basis for this hypothesis, positron emission tomography (PET) and the radioligand [11C]N-methylspiperone were used to determine cortical 5-HT2 receptor occupancy in three psychotic patients treated with 125 mg, 175mg and 200mg clozapine daily. The uptake of [11C]N-methylspiperone in the frontal cortex was very low compared to that in neuroleptic naive schizophrenic patients. 5-HT2 receptor occupancy calculated in the clozapine treated patients was 84%, 87% and 90%. The results show that clinical treatment with clozapine induces a high 5-HT2 receptor occupancy in psychotic patients at a low dose level.
非典型抗精神病药物氯氮平的临床疗效可能与对D2和5-HT2受体的联合作用有关。为检验这一假设的依据，采用正电子发射断层扫描（PET）和放射性配体[11C]N-甲基螺哌隆，测定了3例每日服用125mg、175mg和200mg氯氮平的精神病患者的皮质5-HT2受体占有率。与未用过抗精神病药物的精神分裂症患者相比，[11C]N-甲基螺哌隆在额叶皮质的摄取非常低。在接受氯氮平治疗的患者中计算出的5-HT2受体占有率分别为84%、87%和90%。结果表明，氯氮平临床治疗可使精神病患者在低剂量水平时5-HT2受体占有率较高。
