Factors for the synthesis of 18F-MyoZone and myocardial tomography in normal swine / 中华核医学与分子影像杂志

ABSTRACT

Objective To study the factors affecting the synthesis of 18F-MyoZone,and to evaluate its potential as a myocardial perfusion imaging (MPI) agent in normal Chinese mini-swine.Methods 18F-MyoZone was prepared by substituting the leaving group toluenesulfonyloxy (OTs) from the precursor compound with 18F-fluoride (18F-F-).The conditions affecting the labeling yield were studied by varying the amount of K2CO3 and precursor compound,18F-fluorination reaction time and temperature.PET was performed at 5,30,60 and 120 min post-injection on normal Chinese mini-swine.Results The doses of K2CO3 and precursor,the reaction time and the reaction temperature could affect the labeling yield of 18F-MyoZone,especially K2CO3.The optimized synthetic condition was 1.0 mg K2CO3,2.0 mg mpp2-OTs,20 min reaction time at 90 ℃.The total radio-synthesis time in this condition was 60 min.The uncorrected radiochemical yield was (24.0±5.1) ％.The radiochemical purity was ＞98％.PET imaging showed that 18F-MyoZone had high initial uptake (SUV=8.17± 1.83 at 5 min post-injection) and good retention (SUV =5.78±0.99 at 120 min post-injection) in the heart.The clearance of 18F-MyoZone from liver was very fast.The heart/liver ratios were 3.32,5.31,6.09 and 5.76 at 5,30,60 and 120 min post-injection,respectively.From 5 to 120 min post-injection,the outline of heart was clear and intact.There was almost no interference from the adjacent organs.The quality of PET images was highly satisfactory.Conelusions 18 F-MyoZone has the potential to be a good myocardial perfusion agent.The amount of K2CO3 used could significantly affect the labeling yield of 18F-MyoZone.