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Synthesis and biological evaluation of a novel 18F-labeled radiotracer for PET imaging of the adenosine A2A receptor

Permanent lenke
https://hdl.handle.net/10037/21639
DOI
https://doi.org/10.3390/ijms22031182
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article.pdf (3.941Mb)
Publisert versjon (PDF)
Dato
2021-01-25
Type
Journal article
Tidsskriftartikkel
Peer reviewed

Forfatter
Lai, Thu Hang; Toussaint, Magali; Teodoro, Rodrigo; Dukić-Stefanović, Sladjana; Kranz, Mathias; Deuther-Conrad, Winnie; Moldovan, Rareş-Petru; Brust, Peter
Sammendrag
The adenosine A2A receptor (A2AR) has emerged as a potential non-dopaminergic target for the treatment of Parkinson’s disease and, thus, the non-invasive imaging with positron emission tomography (PET) is of utmost importance to monitor the receptor expression and occupancy during an A2AR-tailored therapy. Aiming at the development of a PET radiotracer, we herein report the design of a series of novel fluorinated analogs (TOZ1-TOZ7) based on the structure of the A2AR antagonist tozadenant, and the preclinical evaluation of [18F]TOZ1. Autoradiography proved A2AR-specific in vitro binding of [18F]TOZ1 to striatum of mouse and pig brain. Investigations of the metabolic stability in mice revealed parent fractions of more than 76% and 92% of total activity in plasma and brain samples, respectively. Dynamic PET/magnetic resonance imaging (MRI) studies in mice revealed a brain uptake but no A2AR-specific in vivo binding.
Forlag
MDPI
Sitering
Lai, Toussaint, Teodoro, Dukić-Stefanović, Kranz, Deuther-Conrad, Moldovan, Brust. Synthesis and biological evaluation of a novel 18F-labeled radiotracer for PET imaging of the adenosine A2A receptor. International Journal of Molecular Sciences. 2021;22>1182(3):1-18
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  • Artikler, rapporter og annet (klinisk medisin) [1974]
Copyright 2021 The Author(s)

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