Radiosynthesis and preclinical evaluation of [18F] 4-(2-fluoroethoxy)-2H-chromen-2-one as a novel myocardial perfusion imaging agent

Abstract

Abstract Recently we developed [18F] 4-(2-fluoroethoxy)-2H-chromen-2-one as a novel 18F myocardial perfusion imaging radiotracer. It was synthesized in good radiochemical yield (>90%). The total time from radiosynthesis to its purification was less than 40 min, with excellent radiochemical purity (≥99%). It showed good stability over a period of 5 h at room temperature. The partition coefficient (log P) of radiotracer was found to be 2.70, suggesting the lipophilic nature of radiotracer. Ex vivo biodistribution study of radiotracer in normal Wistar rats for 30 min post-injection, demonstrated a good heart uptake (>1.3% ID/g) and favorable pharmacokinetics. Additionally, the radiotracer showed significant excretion (>11% ID) by liver, which is indicative of its rapid clearance. Further, in vivo biodistribution study of radiotracer in New Zealand White rabbit provided the clear PET/CT images of cardiomyocytes and myocardial perfusion. All these experimental findings suggest that [18F] 4-(2-fluoroethoxy)-2H-chromen-2-one could be used as a potential hit for myocardial perfusion imaging.