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

Abstract Recently we developed [ 18 F] 4-(2-fluoroethoxy)-2 H -chromen-2-one as a novel 18 F 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 [ 18 F] 4-(2-fluoroethoxy)-2 H -chromen-2-one could be used as a potential hit for myocardial perfusion imaging.