The Synthesis and Evaluation of ¹¹C-KW6002 as the PET Adenosine 2A Receptor Imaging Agent

PET with selective adenosine 2A receptor (A_2A) radiotracers can be used to study a neurodegenerative disorders in vivo and to diagnose of PD. The PET radiotracer ¹¹C-KW6002 for imaging A_2A was synthesized and evaluated, in normal and PD module rats. The results showed that the labeling yield was 56% （decay corrected yield, n=3） when ¹¹CH₃-Triflate reacted with nor-KW6002 under NaOH. The radiochemical purity of product was 99.5% with specific activity of 1.5×10¹⁴ Bq/g. The balance of radioactivity in striatum was observed in normal rats with microPET. A significant raised radioactivity on the striatum of lesion compared with the normal side. The radioactivity was found absence on the striatum of lesion with ¹¹C-CFT. ¹¹C-KW6002 is a potential PET radiotracer for imaging A_2A.