Comparison of 2β-Carbomethoxy-3β-(4-[18F]Fluorophenyl)Tropane and N-(3-[18F]Fluoropropyl)-2β-Carbomethoxy-3β-(4-Fluorophenyl)Nortropane, Tracers for Imaging Dopamine Transporter in Rat

Marjamäki, Päivi; Haaparanta, Merja; Forsbäck, Sarita; Fagerholm, Veronica; Eskola, Olli; Grönroos, Tove J.; Koivula, Teija; Solin, Olof

doi:10.1007/s11307-009-0278-0

Cited by 3 publications

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“…These parallel studies provide a good demonstration of the strengths and weaknesses of different methods in radiopharmacological studies. Overall, the distribution of 18 F activity in rats after [ 18 F]CFT injection was in good agreement with our earlier preliminary studies [5,8] and with studies using [ 3 H]CFT [19,35]. …”

Section: Discussionsupporting

confidence: 91%

“…A report on the ability of [ 18 F]CFT to reflect nigral dopaminergic cell loss in a rat model of Parkinson's disease [7] as well as a study comparing the brain accumulation, metabolism, and kinetics of [ 18 F]CFT and [ 18 F]CFT-FP [8] have shown that [ 18 F]CFT can be used to image DAT in rats. The suitability of [ 18 F]CFT as a radioligand for in vivo studies of DAT in humans has been evaluated [9], and [ 18 F]CFT has been used in human studies of Parkinson's disease [10-15], schizophrenia [16,17], and detached personality [18].…”

Section: Introductionmentioning

confidence: 99%

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[18F]CFT synthesis and binding to monoamine transporters in rat

et al. 2012

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BackgroundWe present the electrophilic synthesis of [18F]2β-carbomethoxy-3β-(4-fluoro)tropane [[18F]CFT] and the pharmacological specificity and selectivity of [18F]CFT for monoamine transporters in the brain and peripheral organs of rats. The human radiation dose is extrapolated from the animal data.Methods[18F]CFT was synthesized by electrophilic fluorination of a stannylated precursor by using post-target-produced [18F]F2 as a fluorinating agent. The ex vivo 18F-activity biodistribution of [18F]CFT in the brain of rats was studied by autoradiography. The binding of [18F]CFT to the monoamine transporters was studied using in vivo blocking experiments with dopamine transporter [DAT], norepinephrine transporter [NET], or serotonin transporter [SERT] inhibitors. In vivo animal positron emission tomography was used as a comparative method to determine tracer kinetics. Human radiation dose was assessed using OLINDA software.ResultsThe radiochemical yield of [18F]CFT from the initial [18F]F-, decay corrected to the end of bombardment, was 3.2 ± 1.0%. The specific activity [SA] was 14.5 ± 3.4 GBq/μmol, decay corrected to the end of synthesis. Radiochemical purity exceeded 99%. DAT-specific binding was found in the striatum, locus coeruleus, and pancreas. NET-specific binding was found in the locus coeruleus. SERT-specific binding was not found in any of the studied organs. Effective dose equivalent [EDE] estimated for the standard human model was 12.8 μSv/MBq. Effective dose [ED] was 9.17 μSv/MBq.ConclusionsPost-target-produced high-SA [18F]F2 was used to incorporate18F directly into the phenyl ring of [18F]CFT. The final product had high radiochemical and chemical purities and a high SA for DAT and NET studies in vivo. In periphery, [18F]CFT showed a specific uptake in the pancreas. EDE and ED corresponded well with other18F-radioligands.

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Section: Discussionsupporting

confidence: 91%