大鼠体内[18F]-N-(对硝基苄基)螺哌隆([18F]PNBS)的合成与评价

Synthesis and in vivo evaluation of [18F]-N-(p-nitrobenzyl)spiperone ([18F]PNBS) in rats.

作者信息

Mach R H, Nowak P A, Moroney D A, Morton T E, Jackson J R, Ehrenkaufer R L

机构信息

Cerebrovascular Research Center, University of Pennsylvania, Philadelphia 19104.

出版信息

Nucl Med Biol. 1993 Apr;20(3):269-78. doi: 10.1016/0969-8051(93)90048-y.

DOI:10.1016/0969-8051(93)90048-y

PMID:8485486

Abstract

[18F]-N-(p-nitrobenzyl)spiperone, [18F]PNBS, was prepared and its in vivo uptake in rat brain was measured. A temporal increase in striatum:cerebellum ratio and frontal cortex:cerebellum (FC:Cb) ratio was observed. Blocking studies suggested the formation of a radiolabeled metabolite, presumably [18F]spiperone, that is capable of crossing the blood-brain barrier and labeling cortical 5-HT2 receptors. This was confirmed using the ISRP method of metabolite analysis indicating [18F]PNBS is not a suitable tracer for studying D2 receptors in vivo with PET.

摘要

制备了[18F]-N-(对硝基苄基)螺哌隆([18F]PNBS)，并测定了其在大鼠脑内的体内摄取情况。观察到纹状体与小脑的比值以及额叶皮质与小脑(FC:Cb)的比值随时间增加。阻断研究表明形成了一种放射性标记代谢物，推测为[18F]螺哌隆，它能够穿过血脑屏障并标记皮质5-HT2受体。使用代谢物分析的ISRP方法证实了这一点，表明[18F]PNBS不是用PET在体内研究D2受体的合适示踪剂。