Preparation and preliminary biological evaluation of 11C-l-SPD

Abstract

Objective: To explore the method and quality control of [Formula: see text]C radiolabeled [Formula: see text]-SPD ([Formula: see text]-Stepholidine) and biodistribution of [Formula: see text]C-[Formula: see text]-SPD in vivo. Methods: (1) [Formula: see text]CO2 was produced by CTI RDS III cyclotron, converted [Formula: see text]CO2 to [Formula: see text]C–CH3I by CH3I die-block, and then converted it to [Formula: see text]C-Triflate–CH4, imported [Formula: see text]C-Triflate–CH4 to [Formula: see text]-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, 90[Formula: see text]min after injecting [Formula: see text]C-[Formula: see text]-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 [Formula: see text]C-[Formula: see text]-SPD was 15 to 20[Formula: see text]min with chemical [Formula: see text]%, and PH values [Formula: see text], radiochemical [Formula: see text]% in 2[Formula: see text]h. All quality criteria of [Formula: see text]C-[Formula: see text]-SPD met the requirements of the positron radio-pharmaceuticals. (2) [Formula: see text]C-[Formula: see text]-SPD was of the characteristic that metabolism was through the liver, and kidney was the main excretory organ, which was [Formula: see text]%ID/g at 5[Formula: see text]min and was decreasing gradually, which was [Formula: see text][Formula: see text]ID/g in liver at 5[Formula: see text]min. Conclusion: (1) [Formula: see text]C-[Formula: see text]-SPD can be used to further study the animal or human. (2) [Formula: see text]C-[Formula: see text]-SPD could quickly discharge and decrease to the low level from background of issues in vivo.