Full automated synthesis of 11C-β-CFT as a dopamine transporter imaging agent

To develop an automatic and efficient synthesis of 11C-β-CFT as a dopamine trans- porter imaging agent for clinical use, 11C-β-CFT was prepared from 11C-Triflate-CH3 by methylation with nor-β-CFT, and then purified by a C-18 Sep-Pak. Fully automated radio- synthesis of 11C-β-CFT was carried out. The corrected radiochemical yield of 11C-β-CFT was 70.2%±1.8% from 11CH3I or 11CH3Br, and the radiochemical purity was above 95%. PET imaging was performed on healthy volunteers and patients with Parkinson's Disease (PD). PET imaging showed high radioactivity uptake of 11C-β-CFT in the bilateral striatums symmetrically for the healthy volunteers, but lower radioactivity uptake in the bilateral striatums asymmetrically for the PD patients. This simple automated synthesis of 11C-β-CFT is efficient with high yields, helpful with the radiation protection of personnel, and satisfactory to clinical applications. (authors)