在精神分裂症患者中使用氟哌啶醇或新型抗精神病药物对纹状体以外和纹状体的D(2)多巴胺受体进行阻断。
Extrastriatal and striatal D(2) dopamine receptor blockade with haloperidol or new antipsychotic drugs in patients with schizophrenia.
作者信息
Xiberas X, Martinot J L, Mallet L, Artiges E, Loc'H C, Mazière B, Paillère-Martinot M L
机构信息
INSERM U 334, Service Hospitalier Frédéric Joliot. A. Chenevier Hôpital, Créteil, France.
出版信息
Br J Psychiatry. 2001 Dec;179:503-8. doi: 10.1192/bjp.179.6.503.
BACKGROUND
Both traditional and atypical antipsychotics have been hypothesised to be effective in schizophrenia through limbic and cortical D(2) dopamine receptor blockade.
AIMS
To investigate this hypothesis with the D(2)/D(3)-selective positron emission tomography (PET) probe [(76)Br]-FLB457.
METHOD
PET scans were performed on 6 controls and 18 patients with schizophrenia treated with haloperidol or with risperidone, clozapine, amisulpride or olanzapine.
RESULTS
The D(2) dopamine receptor blockade was high in the temporal cortex with both haloperidol and atypical antipsychotics. The atypicals, however, induced a significantly lower D(2) binding index than haloperidol in the thalamus and in the striatum.
CONCLUSIONS
Results suggest that cortical D(2) dopamine receptors are a common target of traditional and atypical antipsychotics for therapeutic action. Higher in vivo binding to the D(2) receptors in the cortex than in the basal ganglia is suggested as an indicator of favourable profile for a putative antipsychotic compound.
背景
传统抗精神病药物和非典型抗精神病药物均被假定通过阻断边缘系统和皮质的D(2)多巴胺受体而对精神分裂症有效。
目的
使用D(2)/D(3)选择性正电子发射断层扫描（PET）探针[(76)Br]-FLB457对这一假说进行研究。
方法
对6名对照者以及18名接受氟哌啶醇或利培酮、氯氮平、氨磺必利或奥氮平治疗的精神分裂症患者进行PET扫描。
结果
氟哌啶醇和非典型抗精神病药物在颞叶皮质均有较高的D(2)多巴胺受体阻断作用。然而，非典型抗精神病药物在丘脑和纹状体诱导产生的D(2)结合指数显著低于氟哌啶醇。
结论
结果表明，皮质D(2)多巴胺受体是传统抗精神病药物和非典型抗精神病药物治疗作用的共同靶点。皮质中D(2)受体的体内结合高于基底神经节，这被认为是一种假定抗精神病化合物具有良好特性的指标。
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