多巴胺转运体
放射性配体
壳核
多巴胺质膜转运蛋白
多巴胺能
多巴胺
黑质
人脑
化学
结合势
运输机
内科学
神经科学
内分泌学
医学
生物
受体
生物化学
基因
作者
Aki Laakso,Jörgen Bergman,Merja Haaparanta,Harry Vilkman,Olof Solin,Jarmo Hietala
出处
期刊:Synapse
[Wiley]
日期:1998-03-01
卷期号:28 (3): 244-250
被引量:65
标识
DOI:10.1002/(sici)1098-2396(199803)28:3<244::aid-syn7>3.0.co;2-a
摘要
We have characterized the usage of [18F]CFT (also known as [18F]WIN 35,428) as a radioligand for in vivo studies of human dopamine transporter by PET. CFT was labeled with 18F to a high specific activity, and dynamic PET scans were conducted in healthy volunteers at various time points up to 5 h from [18F]CFT injection. The regional distribution of [18F]CFT uptake correlated well with the known distribution of dopaminergic nerve terminals in the human brain and also with that of other dopamine transporter radioligands. Striatal binding peaked at 225 min after injection and declined thereafter, demonstrating the reversible nature of the binding to the dopamine transporter. Therefore, due to the relatively long half-life of 18F (109.8 min), PET scans with [18F]CFT could easily be conducted during the binding equilibrium, allowing estimation of Bmax/Kd values (i.e., binding potential). Binding potentials for putamen and caudate measured at equilibrium were 4.79 ± 0.11 and 4.50 ± 0.23, respectively. We were able to also visualize midbrain dopaminergic neurons (substantia nigra) with [18F]CFT in some subjects. In conclusion, the labeling of CFT with 18F allows PET scans to be conducted at binding equilibrium, and therefore a high signal-to-noise ratio and reliable quantification of binding potential can be achieved. With a high resolution 3D PET scanner, the quantification of extrastriatal dopamine transporters should become possible. Synapse 28:244–250, 1998. © 1998 Wiley-Liss, Inc.
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