A1 Vertaisarvioitu alkuperäisartikkeli tieteellisessä lehdessä
Radiosynthesis of the norepinephrine transporter tracer [F-18]NS12137 via copper-mediated F-18-labelling
Tekijät: Salla Lahdenpohja, Thomas Keller, Johan Rajander, Anna K. Kirjavainen
Kustantaja: WILEY
Julkaisuvuosi: 2019
Journal: Journal of Labelled Compounds and Radiopharmaceuticals
Tietokannassa oleva lehden nimi: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
Lehden akronyymi: J LABELLED COMPD RAD
Vuosikerta: 62
Numero: 6
Aloitussivu: 259
Lopetussivu: 264
Sivujen määrä: 6
ISSN: 0362-4803
eISSN: 1099-1344
DOI: https://doi.org/10.1002/jlcr.3717
Rinnakkaistallenteen osoite: https://research.utu.fi/converis/portal/detail/Publication/41204500
[F-18]NS12137 (exo-3-[(6-[F-18]fluoro-2-pyridyl)oxy]8-azabicyclo[3.2.1]octane) is a highly selective norepinephrine transporter (NET) tracer. NETs are responsible for the reuptake of norepinephrine and dopamine and are linked to several neurodegenerative and neuropsychiatric disorders. The aim of this study was to develop a copper-mediated F-18-fluorination method for the production of [F-18]NS12137 with straightforward synthesis conditions and high radiochemical yield and molar activity. [F-18]NS12137 was produced in two steps. Radiofluorination of [F-18]NS12137 was performed via a copper-mediated pathway starting with a stannane precursor and using [F-18]F- as the source of the fluorine-18 isotope. Deprotection was performed via acid hydrolysis. The radiofluorination reaction was nearly quantitative as was the deprotection based on HPLC analysis. The radiochemical yield of the synthesis was 15.1 +/- 0.5%. Molar activity of [F-18]NS12137 was up to 300 GBq/mu mol. The synthesis procedure is straightforward and can easily be automated and adapted for clinical production.
Ladattava julkaisu This is an electronic reprint of the original article. |  |
