Objective: To explore the method and quality control of 11C radiolabeled l-SPD (l-Stepholidine) and biodistribution of 11C-l-SPD in vivo.
Methods: (1) 11CO2 was produced by CTI RDS III cyclotron, converted 11CO2 to 11C–CH3I by CH3I die-block, and then converted it to 11C-Triflate–CH4, imported 11C-Triflate–CH4 to l-SPD which was dissolved in Dimethyl sulfoxide [(CH3)2SO], reacted at common temperature and then obtained the product. (2) Take the sample of organs in different times 5, 15, 30, 60, 90min after injecting 11C-l-SPD by vail in mice and measure the radioactive counts per minute (cpm), then the percent injection dose of wet tissue per gram (%ID/g) was calculated.
Results: (1) The synthesis time of 11C-l-SPD was 15 to 20min with chemical purity>90%, and PH values 6.5±0.3, radiochemical purity>95% in 2h. All quality criteria of 11C-l-SPD met the requirements of the positron radio-pharmaceuticals. (2) 11C-l-SPD was of the characteristic that metabolism was through the liver, and kidney was the main excretory organ, which was 1.323±0.153%ID/g at 5min and was decreasing gradually, which was 1.484±0.350ID/g in liver at 5min.
Conclusion: (1) 11C-l-SPD can be used to further study the animal or human. (2) 11C-l-SPD could quickly discharge and decrease to the low level from background of issues in vivo.