Talvik M, Nordström A L, Nyberg S, Olsson H, Halldin C, Farde L
Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S-171 76 Stockholm, Sweden.
Am J Psychiatry. 2001 Jun;158(6):926-30. doi: 10.1176/appi.ajp.158.6.926.
The authors' goal was to test the hypothesis of extrastriatal D(2) receptor selectivity as the mechanism of action of clozapine.
Positron emission tomography (PET) was used to examine extrastriatal as well as striatal dopamine D(2) receptor occupancy in four patients treated with clozapine and three patients treated with haloperidol. The reference radioligand [(11)C]raclopride was used for determination of D(2) receptor occupancy in the striatum. The radioligand [(11)C]FLB 457 was chosen for determination of D(2) receptor occupancy in the thalamus, the temporal cortex, and the frontal cortex.
In patients treated with haloperidol the D(2) receptor occupancy was high in all examined brain regions. In clozapine-treated patients the D(2) receptor occupancy was relatively low in both the striatum and the extrastriatal regions.
The results from the present study give no support for the hypothesis of regional selectivity as the mechanism of action for clozapine.
作者的目标是检验纹状体以外的D(2)受体选择性作为氯氮平作用机制的假说。
采用正电子发射断层扫描（PET）检查4例接受氯氮平治疗的患者和3例接受氟哌啶醇治疗的患者纹状体以外及纹状体内多巴胺D(2)受体占有率。参考放射性配体[(11)C]雷氯必利用于测定纹状体内D(2)受体占有率。放射性配体[(11)C]FLB 457用于测定丘脑、颞叶皮质和额叶皮质内D(2)受体占有率。
接受氟哌啶醇治疗的患者，所有检查脑区的D(2)受体占有率均较高。接受氯氮平治疗的患者，纹状体和纹状体以外区域的D(2)受体占有率相对较低。
本研究结果不支持区域选择性作为氯氮平作用机制的假说。
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