Quantitative analysis of dopamine transporters in human brain using [11C]PE2I and positron emission tomography: evaluation of reference tissue models

Seki, Chie; Ito, Hiroshi; Ichimiya, Tetsuya; Arakawa, Ryosuke; Ikoma, Yoko; Shidahara, Miho; Maeda, Jun; Takano, Akihiro; Takahashi, Hidehiko; Kimura, Yuichi; Suzuki, Kazutoshi; Kanno, Iwao; Suhara, Tetsuya

doi:10.1007/s12149-010-0364-z

Cited by 23 publications

(33 citation statements)

References 36 publications

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“…In human PET studies, 11 C-PE2I showed a high specific-to-nonspecific ratio (15)(16)(17)(18). However, 2 problems have been reported in quantifying DAT with 11 C-PE2I.…”

Section: F-(e)-n-(3-iodoprop-2e-enyl)-2b-carbofluoroethoxy-3b-(4-methmentioning

confidence: 99%

“…In nonhuman primates, 18 F-FE-PE2I showed faster kinetics and less production of radiometabolites that could potentially permeate the blood-brain barrier than did 11 C-PE2I. The aims of this study were to examine the quantification of DAT using 18 F-FE-PE2I and to assess the effect of radiometabolites of 18 F-FE-PE2I on the quantification in healthy humans. Methods: A 90-min dynamic PET scan was obtained for 10 healthy men after intravenous injection of 18 F-FE-PE2I.…”

Section: F-(e)-n-(3-iodoprop-2e-enyl)-2b-carbofluoroethoxy-3b-(4-methmentioning

confidence: 99%

“…The aims of this study were to examine the quantification of DAT using 18 F-FE-PE2I and to assess the effect of radiometabolites of 18 F-FE-PE2I on the quantification in healthy humans. Methods: A 90-min dynamic PET scan was obtained for 10 healthy men after intravenous injection of 18 F-FE-PE2I. Kinetic compartment model analysis with a metabolite-corrected arterial input function was performed.…”

Section: F-(e)-n-(3-iodoprop-2e-enyl)-2b-carbofluoroethoxy-3b-(4-methmentioning

confidence: 99%

“…The simplified reference tissue model (SRTM) method with the cerebellum as a reference region was evaluated as a noninvasive method of quantification. Results: After the injection of 18 F-FE-PE2I, the whole-brain radioactivity showed a high peak (;3-5 standardized uptake value) and fast washout. The radioactive uptake of 18 F-FE-PE2I in the brain was according to the relative density of the DAT (striatum .…”

Section: F-(e)-n-(3-iodoprop-2e-enyl)-2b-carbofluoroethoxy-3b-(4-methmentioning

confidence: 99%

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Quantification of Dopamine Transporter in Human Brain Using PET with ¹⁸F-FE-PE2I

Sasaki¹,

Ito²,

Kimura³

et al. 2012

J Nucl Med

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nortropane ( 18 F-FE-PE2I) is a new PET radioligand with a high affinity and selectivity for the dopamine transporter (DAT). In nonhuman primates, 18 F-FE-PE2I showed faster kinetics and less production of radiometabolites that could potentially permeate the blood-brain barrier than did 11 C-PE2I. The aims of this study were to examine the quantification of DAT using 18 F-FE-PE2I and to assess the effect of radiometabolites of 18 F-FE-PE2I on the quantification in healthy humans. Methods: A 90-min dynamic PET scan was obtained for 10 healthy men after intravenous injection of 18 F-FE-PE2I. Kinetic compartment model analysis with a metabolite-corrected arterial input function was performed. The effect of radiometabolites on the quantification was evaluated by time-stability analyses. The simplified reference tissue model (SRTM) method with the cerebellum as a reference region was evaluated as a noninvasive method of quantification. Results: After the injection of 18 F-FE-PE2I, the whole-brain radioactivity showed a high peak (;3-5 standardized uptake value) and fast washout. The radioactive uptake of 18 F-FE-PE2I in the brain was according to the relative density of the DAT (striatum . midbrain . thalamus). The cerebellum showed the lowest uptake. Tissue time-activity curves were well described by the 2-tissue-compartment model (TCM), as compared with the 1-TCM, for all subjects in all regions. Time stability analysis showed stable estimation of total distribution volume with 60-min or longer scan durations, indicating the small effect of radiometabolites. Binding potentials in the striatum and midbrain were well estimated by the SRTM method, with modest intersubject variability. Although the SRTM method yielded a slight underestimation and overestimation in regions with high and low DAT densities, respectively, binding potentials by the SRTM method were well correlated to the estimates by the indirect kinetic method with 2-TCM. Conclusion: 18 F-FE-PE2I is a promising PET radioligand for quantifying DAT. The binding potentials could be reliably estimated in both the striatum and midbrain using both the indirect kinetic and SRTM methods with a scan duration of 60 min. Although radiometabolites of 18 F-FE-PE2I in plasma possibly introduced some effects on the radioactivity in the brain, the effects on estimated binding potential were likely to be small.

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“…In human PET studies, 11 C-PE2I showed a high specific-to-nonspecific ratio (15)(16)(17)(18). However, 2 problems have been reported in quantifying DAT with 11 C-PE2I.…”

Section: F-(e)-n-(3-iodoprop-2e-enyl)-2b-carbofluoroethoxy-3b-(4-methmentioning

confidence: 99%

Section: F-(e)-n-(3-iodoprop-2e-enyl)-2b-carbofluoroethoxy-3b-(4-methmentioning

confidence: 99%

Section: F-(e)-n-(3-iodoprop-2e-enyl)-2b-carbofluoroethoxy-3b-(4-methmentioning

confidence: 99%

Section: F-(e)-n-(3-iodoprop-2e-enyl)-2b-carbofluoroethoxy-3b-(4-methmentioning

confidence: 99%

See 2 more Smart Citations

Quantification of Dopamine Transporter in Human Brain Using PET with ¹⁸F-FE-PE2I

Sasaki¹,

Ito²,

Kimura³

et al. 2012

J Nucl Med

Self Cite

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“…With a 60-min imaging time, BPND of striatum were approximately 103% of that of a 90-min imaging time. 13 (12,14,15,(29)(30)(31). Considering that in vitro DAT DAT is also known to localize in the midbrain, which contains dopaminergic cell bodies.…”

Section: Imaging Time Dependency Of Striatal Bpndmentioning

confidence: 99%

PET imaging of dopamine transporters with [ 18 F]FE-PE2I: Effects of anti-Parkinsonian drugs

Bang

Jung

Song

et al. 2016

Nuclear Medicine and Biology

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An efficient one‐step radiosynthesis of [¹⁸F]FE‐PE2I, a PET radioligand for imaging of dopamine transporters

Степанов

Красикова

Raus

et al. 2012

Labelled Comp Radiopharmac

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The aim of this study was to develop a direct fluorination method for the preparation of [18F]‐(E)‐N‐(3‐iodoprop‐2‐enyl)‐2β‐carbofluoroethoxy‐3β‐(4′‐methyl‐phenyl)nortropane ([18F]FE‐PE2I (VI). The synthesis procedure relies on the conventional Kryptofix‐mediated nucleophilic 18F‐substitution of the tosylate group in the precursor, TsOE‐PE2I (V). Out of reaction conditions tested, the highest fluorination efficiency was obtained in dimethyl sulfoxide at 140°C. The reaction mixture was purified by semi‐preparative HPLC, followed‐up by a standard Sep‐Pak SPE procedure. On average, 1.0 GBq of [18F]FE‐PE2I was produced from 5‐min irradiation at 35 μA (dimethyl sulfoxide, 5 min/140°C). Decay‐uncorrected yield of the product after HPLC purification and formulation was in the order of 20%. Specific radioactivity of [18F]FE‐PE2I at 15 min after EOS was 3.3–5.1 Ci/µmol (n = 3); radiochemical purity was >98% (n = 4). This direct nucleophilic fluorination strategy is well suited for the automation of the entire synthesis of [18F]FE‐PE2I in a modern PET synthesizer for human PET application. In addition, the 18F‐incorporation rate into TsOE‐PE2I was evaluated using radio‐thin layer chromatography (TLC) and radio‐HPLC. The suggested HPLC method (ACE 5 C18‐HL column and acetonitrile/0.1 M NH4CO2 (80:20)) was found to be suitable for evaluation of ‘free’ 18F‐fluoride in the reaction mixture; in addition, this method allowed the detection of three radiolabelled by‐products that were not discernable with the TLC approach. Therefore, we conclude that the HPLC approach may serve as a good alternative to traditional radio‐TLC technique as it provides more detailed information about the fluorination process in the reaction kinetics or optimization studies. Copyright © 2012 John Wiley & Sons, Ltd.

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Quantitative analysis of dopamine transporters in human brain using [11C]PE2I and positron emission tomography: evaluation of reference tissue models

Cited by 23 publications

References 36 publications

Quantification of Dopamine Transporter in Human Brain Using PET with ¹⁸F-FE-PE2I

Quantification of Dopamine Transporter in Human Brain Using PET with ¹⁸F-FE-PE2I

PET imaging of dopamine transporters with [ 18 F]FE-PE2I: Effects of anti-Parkinsonian drugs

An efficient one‐step radiosynthesis of [¹⁸F]FE‐PE2I, a PET radioligand for imaging of dopamine transporters

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Quantitative analysis of dopamine transporters in human brain using [11C]PE2I and positron emission tomography: evaluation of reference tissue models

Cited by 23 publications

References 36 publications

Quantification of Dopamine Transporter in Human Brain Using PET with 18F-FE-PE2I

Quantification of Dopamine Transporter in Human Brain Using PET with 18F-FE-PE2I

PET imaging of dopamine transporters with [ 18 F]FE-PE2I: Effects of anti-Parkinsonian drugs

An efficient one‐step radiosynthesis of [18F]FE‐PE2I, a PET radioligand for imaging of dopamine transporters

Contact Info

Product

Resources

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Quantification of Dopamine Transporter in Human Brain Using PET with ¹⁸F-FE-PE2I

Quantification of Dopamine Transporter in Human Brain Using PET with ¹⁸F-FE-PE2I

An efficient one‐step radiosynthesis of [¹⁸F]FE‐PE2I, a PET radioligand for imaging of dopamine transporters