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.

Marjamaki P; Haaparanta M; Forsback S; Fagerholm V; Eskola O; Gronroos T; Koivula T; Solin O

首页> 外文期刊>Molecular imaging and biology: MIB : the official publication of the Academy of Molecular Imaging >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.

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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.

机译：比较2β-羰甲氧基-3β-（4-（18F）氟苯基）托烷和N-（3-（18F）氟丙基）-2β-羰甲氧基-3β-（4-氟苯基）降冰片烷，大鼠多巴胺转运蛋白成像示踪剂。

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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.

机译：目的：这项研究比较2beta-carbomethoxy-3beta-（4-[（（18）F]氟苯基）托烷（[（18）F] beta-CFT）和N-（3-[（18）F]氟丙基）-2beta -碳甲氧基-3β-（4-氟苯基）正烷（[（18）F]β-CFT-FP）作为放射性示踪剂，用于在大鼠中对多巴胺转运蛋白（DAT）进行成像。程序：在用DAT，5-羟色胺转运蛋白（SERT）和去甲肾上腺素转运蛋白（NET）的特异性拮抗剂预处理的大鼠中和离体大鼠中，对离体示踪剂的生物分布，特异性和选择性进行了离体研究。使用HRRT扫描仪进行正电子发射断层扫描（PET）研究。用薄层色谱分析放射性标记的代谢物。结果：[（18）F] beta CFT显示缓慢的动力学与120分钟最大纹状体/小脑摄取比为9.2。 [（18）F]β-CFT-FP显示快速动力学，在5分钟时的最大比率为3.1。两个跟踪器都绑定到DAT。 [（18）F] beta-CFT也绑定到NET。 [（18）F] beta-CFT比[（18）F] beta-CFT-FP更耐代谢。结论：[（18）F]β-CFT-FP的结构修饰显着改变了其生物学特性。 [（18）F] beta-CFT是适合临床前和人类PET研究的示踪剂，但[（18）F] beta-CFT-FP不太适合作为PET示踪剂。

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《Molecular imaging and biology: MIB : the official publication of the Academy of Molecular Imaging》 |2010年第3期|共9页
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Marjamaki P; Haaparanta M; Forsback S; Fagerholm V; Eskola O; Gronroos T; Koivula T; Solin O;
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1. 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. [J] . Marjamaki P, Haaparanta M, Forsback S, Molecular imaging and biology: MIB : the official publication of the Academy of Molecular Imaging . 2010,第3期

机译：比较2β-羰甲氧基-3β-（4-（18F）氟苯基）托烷和N-（3-（18F）氟丙基）-2β-羰甲氧基-3β-（4-氟苯基）降冰片烷，大鼠多巴胺转运蛋白成像示踪剂。
2. 2Beta-carbomethoxy-3beta-(4- and 2-(18F)fluoromethylphenyl)tropanes: specific probes for in vivo quantification of central dopamine transporter sites. [J] . Stout D, Petric A, Satyamurthy N, Nuclear Medicine and Biology . 1999,第8期

机译：2Beta-carbomethoxy-3beta-（4-和2-（18F）氟甲基苯基）托烷：用于体内定量中央多巴胺转运蛋白位点的特异性探针。
3. Importance of valine at position 152 for the substrate transport and 2beta-carbomethoxy-3beta-(4-fluorophenyl)tropane binding of dopamine transporter. [J] . Lee SH, Chang MY, Lee KH, Molecular pharmacology. . 2000,第5期

机译：缬氨酸在位置152上对底物转运和多巴胺转运蛋白的2β-羰甲氧基-3β-（4-氟苯基）托烷结合的重要性。
4. Synthesis radiosynthesis and in vivo evaluation of 123I-4-(2-(bis(4-fluorophenyl)methoxy)ethyl)-1-(4-iodobenzyl)piperidine as a selective tracer for imaging the dopamine transporter [O] . S. De Bruyne, T. L. Boos, L. wyffels, -1

机译：123i -4-（2-（二氟苯基）乙基）-1-（4-碘苄基）哌啶作为对多巴胺转运蛋白成像的选择性示踪剂的合成可放热合成和体内评价
5. Pilot Preclinical and Clinical Evaluation of (4S)-4-(3-[18F]Fluoropropyl)-L-Glutamate (18F-FSPG) for PET/CT Imaging of Intracranial Malignancies. [O] . Erik S Mittra, Norman Koglin, Camila Mosci, 2016

机译：用于颅内恶性肿瘤的pET / CT成像的（4s）-4-（3- [18 F]氟代丙基）-L-谷氨酸（18F-FspG）的临床前和临床评价。

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.

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