Sedvall G, Nybäck H, Farde L, Persson A
Department of Psychiatry and Psychology, Karolinska Institutet, Stockholm, Sweden.
J Neural Transm Suppl. 1987;24:43-8.
Recent developments in positron emission tomography and ligand binding techniques have allowed the visualization of regional metabolism and neuroreceptor distributions in the living human brain. For dopamine-D 2 and benzodiazepine receptors it has also been possible to determine neuroreceptor characteristics such as Bmax and Kd by performing in vivo saturation analysis of ligand binding to the receptors. Using 11-C raclopride and 11-C-Ro 15-1788 as ligands for dopamine-D 2 and benzodiazepine receptors respectively we have determined Bmax and Kd-values in healthy volunteers and patients with various types of neuropsychiatric disorders. These ligands were also used in order to determine the degree of receptor occupancy in psychiatric patients treated with different types of drugs interfering with these neuroreceptors. We have administered 11-C-deoxy-glucose, 11-C-raclopride and 11-C-Ro 15-1788 to patients with Alzheimer's disease in order to examine possible alterations of glucose utilization and neuroreceptor distribution and quantities in these patients. The preliminary results indicate that this approach may be useful for the analysis of degenerative alterations of neuron populations and neuroreceptor systems in Alzheimer's disease.
正电子发射断层扫描和配体结合技术的最新进展,已使活体人脑区域代谢和神经受体分布的可视化成为可能。对于多巴胺-D2和苯二氮䓬受体,通过对配体与受体的结合进行体内饱和分析,也能够确定诸如最大结合容量(Bmax)和平衡解离常数(Kd)等神经受体特征。分别使用11-C-雷氯必利和11-C-罗15-1788作为多巴胺-D2和苯二氮䓬受体的配体,我们已经测定了健康志愿者以及患有各种类型神经精神疾病患者的Bmax和Kd值。这些配体还被用于确定接受不同类型干扰这些神经受体药物治疗的精神疾病患者的受体占有率。我们已给阿尔茨海默病患者施用11-C-脱氧葡萄糖、11-C-雷氯必利和11-C-罗15-1788,以检查这些患者葡萄糖利用以及神经受体分布和数量的可能变化。初步结果表明,这种方法可能有助于分析阿尔茨海默病中神经元群体和神经受体系统的退行性改变。