Fully automated synthesis and coupling of [18F]FBEM to glutathione using the iPHASE FlexLab module
Identifieur interne : 002F32 ( Istex/Curation ); précédent : 002F31; suivant : 002F33Fully automated synthesis and coupling of [18F]FBEM to glutathione using the iPHASE FlexLab module
Auteurs : Uwe Ackermann [Australie] ; Lucie Plougastel [France] ; Christian Wichmann [Australie] ; Yit Wooi Goh [Australie] ; Shinn Dee Yeoh [Australie] ; Stan S. Poniger [Australie] ; Henri J. Tochon-Danguy [Australie] ; Andrew M. Scott [Australie]Source :
- Journal of Labelled Compounds and Radiopharmaceuticals [ 0362-4803 ] ; 2014-02.
Abstract
Site‐specific radiolabelling of peptides or antibodies using [18F]FBEM is often preferred over non‐site‐specific radiolabelling with [18F]SFB because it does not affect the affinity of the antibody to its target. Unfortunately, the synthesis of [18F]FBEM and its conjugation to thiol containing macromolecules requires some manual intervention, which leads to radiation exposure of the radiochemist. In this publication, we report on the complete automation of [18F]FBEM production and its subsequent conjugation to glutathione using a slightly modified iPHASE FlexLab module. [18F]FBEM was produced in 1.185 ± 0.168 GBq (15–20%; n = 10; 0.75 ± 0.106 GBq non‐decay corrected) with a specific activity of 57 ± 10 GBq/µmol. Radiochemical purity was 97 ± 1% and the synthesis time including HPLC purification and reformulation was 70 min. After evaporation to dryness, [18F]FBEM was conjugated to glutathione in PBS buffer pH 7.4 in quantitative yields. This fully automated method does not require any manual intervention and therefore reduces the radiation exposure to the operator.
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DOI: 10.1002/jlcr.3175
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xml:lang="fr">Australie</country><wicri:regionArea>The University of Melbourne, Parkville, Melbourne</wicri:regionArea></affiliation></author><author><name sortKey="Goh, Yit Wooi" sort="Goh, Yit Wooi" uniqKey="Goh Y" first="Yit Wooi" last="Goh">Yit Wooi Goh</name><affiliation wicri:level="1"><mods:affiliation>Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, Melbourne</wicri:regionArea></affiliation><affiliation wicri:level="1"><mods:affiliation>The University of Melbourne, Parkville, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>The University of Melbourne, Parkville, Melbourne</wicri:regionArea></affiliation></author><author><name sortKey="Yeoh, Shinn Dee" sort="Yeoh, Shinn Dee" uniqKey="Yeoh S" first="Shinn Dee" last="Yeoh">Shinn Dee Yeoh</name><affiliation wicri:level="1"><mods:affiliation>Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, Melbourne</wicri:regionArea></affiliation><affiliation wicri:level="1"><mods:affiliation>The University of Melbourne, Parkville, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>The University of Melbourne, Parkville, Melbourne</wicri:regionArea></affiliation></author><author><name sortKey="Poniger, Stan S" sort="Poniger, Stan S" uniqKey="Poniger S" first="Stan S." last="Poniger">Stan S. Poniger</name><affiliation wicri:level="1"><mods:affiliation>iPHASE Technologies, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>iPHASE Technologies, Melbourne</wicri:regionArea></affiliation></author><author><name sortKey="Tochon Anguy, Henri J" sort="Tochon Anguy, Henri J" uniqKey="Tochon Anguy H" first="Henri J." last="Tochon-Danguy">Henri J. Tochon-Danguy</name><affiliation wicri:level="1"><mods:affiliation>Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, Melbourne</wicri:regionArea></affiliation><affiliation wicri:level="1"><mods:affiliation>The University of Melbourne, Parkville, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>The University of Melbourne, Parkville, Melbourne</wicri:regionArea></affiliation><affiliation wicri:level="1"><mods:affiliation>Ludwig Institute for Cancer Research, Melbourne Branch, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Ludwig Institute for Cancer Research, Melbourne Branch, Melbourne</wicri:regionArea></affiliation><affiliation wicri:level="1"><mods:affiliation>iPHASE Technologies, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>iPHASE Technologies, Melbourne</wicri:regionArea></affiliation></author><author><name sortKey="Scott, Andrew M" sort="Scott, Andrew M" uniqKey="Scott A" first="Andrew M." last="Scott">Andrew M. Scott</name><affiliation wicri:level="1"><mods:affiliation>Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, Melbourne</wicri:regionArea></affiliation><affiliation wicri:level="1"><mods:affiliation>The University of Melbourne, Parkville, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>The University of Melbourne, Parkville, Melbourne</wicri:regionArea></affiliation><affiliation wicri:level="1"><mods:affiliation>Ludwig Institute for Cancer Research, Melbourne Branch, Melbourne, Australia</mods:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Ludwig Institute for Cancer Research, Melbourne Branch, Melbourne</wicri:regionArea></affiliation></author></analytic><monogr></monogr><series><title level="j" type="main">Journal of Labelled Compounds and Radiopharmaceuticals</title><title level="j" type="alt">JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS</title><idno type="ISSN">0362-4803</idno><idno type="eISSN">1099-1344</idno><imprint><biblScope unit="vol">57</biblScope><biblScope unit="issue">2</biblScope><biblScope unit="page" from="115">115</biblScope><biblScope unit="page" to="120">120</biblScope><biblScope unit="page-count">6</biblScope><date type="published" when="2014-02">2014-02</date></imprint><idno type="ISSN">0362-4803</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0362-4803</idno></seriesStmt></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract">Site‐specific radiolabelling of peptides or antibodies using [18F]FBEM is often preferred over non‐site‐specific radiolabelling with [18F]SFB because it does not affect the affinity of the antibody to its target. Unfortunately, the synthesis of [18F]FBEM and its conjugation to thiol containing macromolecules requires some manual intervention, which leads to radiation exposure of the radiochemist. In this publication, we report on the complete automation of [18F]FBEM production and its subsequent conjugation to glutathione using a slightly modified iPHASE FlexLab module. [18F]FBEM was produced in 1.185 ± 0.168 GBq (15–20%; n = 10; 0.75 ± 0.106 GBq non‐decay corrected) with a specific activity of 57 ± 10 GBq/µmol. Radiochemical purity was 97 ± 1% and the synthesis time including HPLC purification and reformulation was 70 min. After evaporation to dryness, [18F]FBEM was conjugated to glutathione in PBS buffer pH 7.4 in quantitative yields. This fully automated method does not require any manual intervention and therefore reduces the radiation exposure to the operator.</div></front></TEI></record>Pour manipuler ce document sous Unix (Dilib)
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