QUANTITATIVE-ANALYSIS OF D2 DOPAMINE RECEPTOR-BINDING IN THE LIVING HUMAN-BRAIN BY PET
QUANTITATIVE-ANALYSIS OF D2 DOPAMINE RECEPTOR-BINDING IN THE LIVING HUMAN-BRAIN BY PET
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DOI：
10.1126/science.2867601
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发表时间：
1986-01-17
期刊：
影响因子：
56.9
通讯作者：
SEDVALL, G
中科院分区：
文献类型：
--
作者：
FARDE, L;HALL, H;SEDVALL, G
用选择性、高亲和力的D2受体拮抗剂碳11标记的拉氯普利和正电子发射断层扫描对活体受试者壳核中的D2受体进行了表征。在四名健康男性身上的实验证明，[11C]雷氯必利与希尔系数接近1的表面上均一的位点群结合是饱和的。在正常壳核中，最大结合量为12~17皮摩尔/立方厘米，解离常数为3.4~4.7纳摩尔。尸检时，人体壳核的最大结合量为每立方米15皮摩尔。[11C]拉氯必利结合的研究表明，临床有效剂量的不同的抗精神病药物导致85%到90%的D2多巴胺受体在精神分裂症患者的壳核中占据。
D2 dopamine receptors in the putamen of living human subjects were characterized by using the selective, high-affinity D2 dopamine receptor antagonist carbon-11-labeled raclopride and positron emission tomography. Experiments in four healthy men demonstrated saturability of [11C]raclopride binding to an apparently homogeneous population of sites with Hill coefficients close to unity. In the normal putamen, maximum binding ranged from 12 to 17 picomoles per cubic centimeter and dissociation constants from 3.4 to 4.7 nanomolar. Maximum binding for human putamen at autopsy was 15 picomoles per cubic centrimeter. Studies of [11C]raclopride binding indicate that clinically effective doses of chemically distinct neuroleptic drugs result in 85 to 90 percent occupancy of D2 dopamine receptors in the putamen of schizophrenic patients.