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Published on: January 11, 2020
[18F]FE@SUPPY and [18F]FE@SUPPY:2--metabolic considerations
Daniela Haeusler1, Lukas Nics, Leonhard-Key Mien
1Department of Nuclear Medicine, Medical University of Vienna, A-1090 Vienna, Austria.
[(18)F]FE@SUPPY demonstrated greater metabolic stability in rats compared to [(18)F]FE@SUPPY:2. This finding suggests [(18)F]FE@SUPPY is a more suitable positron emission tomography tracer for adenosine A(3) receptor imaging in clinical investigations.
Area of Science:
- Nuclear medicine
- Radiochemistry
- Pharmacology
Background:
- [(18)F]FE@SUPPY and [(18)F]FE@SUPPY:2 are novel positron emission tomography (PET) tracers for the adenosine A(3) receptor.
- Characterizing their metabolic profiles is crucial for clinical application.
Purpose of the Study:
- To perform metabolic characterization of [(18)F]FE@SUPPY and [(18)F]FE@SUPPY:2.
- To assess their stability and potential for adenosine A(3) receptor imaging.
Main Methods:
- In vitro carboxylesterase (CES) assays were performed to determine kinetic parameters.
- In vivo experiments in rats involved tracer injection, followed by blood and brain sample collection at various time points.
- High-performance liquid chromatography (HPLC) was used for sample analysis.
Main Results:
- CES hydrolysis showed Michaelis-Menten kinetics with micromolar constants for both tracers.
- In blood, [(18)F]FE@SUPPY exhibited higher intact percentages at 15 and 30 minutes post-injection compared to [(18)F]FE@SUPPY:2.
- [(18)F]FE@SUPPY:2 formed an early hydrophilic metabolite in the brain, while [(18)F]FE@SUPPY remained largely unmetabolized for 30 minutes.
Conclusions:
- [(18)F]FE@SUPPY demonstrates superior metabolic stability in rats, a species with faster metabolism than humans.
- This suggests [(18)F]FE@SUPPY is a promising PET tracer for adenosine A(3) receptor imaging with a suitable profile for clinical investigations.
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