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2β- 羧甲氧基 -3β-(4-[18F] 氟苯基) 托烷与 N-(3-[18F] 氟丙基)-2β- 羧甲氧基 -3β-(4- 氟苯基) 去甲托烷，用于大鼠多巴胺转运体成像的示踪剂比较。

Comparison of 2beta-carbomethoxy-3beta-(4-[18F]fluorophenyl)tropane and N-(3-[18F]fluoropropyl)-2beta-carbomethoxy-3beta-(4-fluorophenyl)nortropane, tracers for imaging dopamine transporter in rat.

机构信息

MediCity/PET Preclinical Laboratory, Turku PET Centre, University of Turku, Tykistökatu 6A, FI-20520, Turku, Finland.

出版信息

Mol Imaging Biol. 2010 Jun;12(3):269-77. doi: 10.1007/s11307-009-0278-0. Epub 2009 Dec 1.

DOI:10.1007/s11307-009-0278-0
PMID:19949983
Abstract

PURPOSE

This study compares 2beta-carbomethoxy-3beta-(4-[(18)F]fluorophenyl)tropane ([(18)F]beta-CFT) and N-(3-[(18)F]fluoropropyl)-2beta-carbomethoxy-3beta-(4-fluorophenyl)nortropane ([(18)F]beta-CFT-FP) as radiotracers for imaging the dopamine transporter (DAT) in rat.

PROCEDURES

Biodistribution, specificity and selectivity of the radiotracers were studied ex vivo in rats pre-treated with specific antagonists for DAT, serotonin transporter (SERT) and noradrenalin transporter (NET) and in control rats. Positron emission tomography (PET) studies were performed using an HRRT scanner. Radiolabelled metabolites were analyzed with thin-layer chromatography.

RESULTS

[(18)F]beta-CFT showed slow kinetics with a maximum striatum/cerebellum uptake ratio of 9.2 at 120 min. [(18)F]beta-CFT-FP showed fast kinetics with a maximum ratio of 3.1 at 5 min. Both tracers bound to DAT. [(18)F]beta-CFT also bound to NET. [(18)F]beta-CFT was more resistant to metabolism than [(18)F]beta-CFT-FP.

CONCLUSIONS

Structural modifications of [(18)F]beta-CFT significantly changed its biological properties, as shown by [(18)F]beta-CFT-FP. [(18)F]beta-CFT is a suitable tracer for both preclinical and human PET studies, but [(18)F]beta-CFT-FP is less suitable as a PET tracer.

摘要

目的

本研究比较了 2β- carbomethoxy-3β-(4-[(18)F]fluorophenyl)tropane([(18)F]β-CFT)和 N-(3-[(18)F]fluoropropyl)-2β- carbomethoxy-3β-(4-fluorophenyl)nortropane([(18)F]β-CFT-FP)作为放射性示踪剂，用于成像大鼠中的多巴胺转运体(DAT)。

方法

在预先用 DAT、5-羟色胺转运体(SERT)和去甲肾上腺素转运体(NET)的特异性拮抗剂预处理的大鼠和对照大鼠中，进行放射性示踪剂的生物分布、特异性和选择性研究。使用 HRRT 扫描仪进行正电子发射断层扫描(PET)研究。用薄层层析法分析放射性标记的代谢物。

结果

[(18)F]β-CFT 显示出缓慢的动力学，在 120 分钟时，纹状体/小脑的最大摄取比为 9.2。[(18)F]β-CFT-FP 显示出快速的动力学，在 5 分钟时最大比值为 3.1。两种示踪剂均与 DAT 结合。[(18)F]β-CFT 还与 NET 结合。[(18)F]β-CFT 比[(18)F]β-CFT-FP 更能抵抗代谢。

结论

[(18)F]β-CFT 的结构修饰显著改变了其生物学特性，这一点从[(18)F]β-CFT-FP 中可以看出。[(18)F]β-CFT 是适合进行临床前和人类 PET 研究的示踪剂，但[(18)F]β-CFT-FP 作为 PET 示踪剂不太合适。

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