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Radiofluorinated N-Octanoyl Dopamine ([18F]F-NOD) as a tool to study tissue distribution and elimination of NOD in vitro and in vivo

To mitigate pretransplantation injury in organs of potential donors, N-octanoyl dopamine (NOD) treatment might be considered as it does not affect hemodynamic parameters in braindead (BD) donors. To better assess optimal NOD concentrations for donor treatment, we report on the fast and facile radiof...

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Main Authors: Pretze, Marc (Author) , Pallavi, Prama (Author) , Klotz, Sarah (Author) , Binzen, Uta (Author) , Greffrath, Wolfgang (Author) , Treede, Rolf-Detlef (Author) , Yard, Benito A. (Author) , Wängler, Carmen (Author) , Wängler, Björn (Author)
Format: Article (Journal)
Language:English
Published: October 12, 2016
In: Journal of medicinal chemistry
Year: 2016, Volume: 59, Issue: 21, Pages: 9855-9865
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.6b01191
Online Access:Verlag, Volltext: https://doi.org/10.1021/acs.jmedchem.6b01191
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Author Notes:Marc Pretze, Prama Pallavi, Mareike Roscher, Sarah Klotz, Julio Caballero, Uta Binzen, Wolfgang Greffrath, Rolf-Detlef Treede, Martin C. Harmsen, Mathias Hafner, Benito Yard, Carmen Wängler, and Björn Wängler
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Summary:To mitigate pretransplantation injury in organs of potential donors, N-octanoyl dopamine (NOD) treatment might be considered as it does not affect hemodynamic parameters in braindead (BD) donors. To better assess optimal NOD concentrations for donor treatment, we report on the fast and facile radiofluorination of the NOD-derivative [18F]F-NOD [18F]5 for in vivo assessment of NOD’s elimination kinetics by means of PET imaging. [18F]5 was synthesized in reproducibly high radiochemical yields and purity (>98%) as well as high specific activities (>20 GBq/μmol). Stability tests showed no decomposition of [18F]5 over a period of 120 min in rat plasma. In vitro, low cell association was found for [18F]5, indicating no active transport mechanism into cells. In vivo, [18F]5 exhibited a fast blood clearance and a predominant hepatobiliary elimination. As these data suggest that also NOD might be cleared fast, further pharmacokinetic evaluation is warranted.
Item Description:Gesehen am 18.06.2019
Physical Description:Online Resource
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.6b01191

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