Improved in vivo PET imaging of the adenosine A_2A receptor in the brain using [¹⁸F]FLUDA, a deuterated radiotracer with high metabolic stability.

ABSTRACT:

Purpose

The adenosine A_2A receptor has emerged as a therapeutic target for multiple diseases, and thus the non-invasive imaging of the expression or occupancy of the A_2A receptor has potential to contribute to diagnosis and drug development. We aimed at the development of a metabolically stable A_2A receptor radiotracer and report herein the preclinical evaluation of [¹⁸F]FLUDA, a deuterated isotopologue of [¹⁸F]FESCH.

Methods

[¹⁸F]FLUDA was synthesized by a two-step one-pot approach and evaluated in vitro by autoradiographic studies as well as in vivo by metabolism and dynamic PET/MRI studies in mice and piglets under baseline and blocking conditions. A single-dose toxicity study was performed in rats.

Resu

SUBMITTER: Lai TH 

PROVIDER: S-EPMC8263428 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature