Radiolabeling of 11C-sertraline by fast and easy loop method with [11C]CH3OTf

Abstract

Cis-(1S,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tertrahydro-N-methyl-1-naphthalenamine (sertraline) hydrochloride from among selective serotonin reuptake inhibitors (SSRIs) is a treatment of major depression. For the differential diagnosis by metabolizing serotonin in a patient with neurological disorders, the radiolabeled 11C-sertraline was developed for non-invasive positron emission tomography in living brain and use the evaluation of new drug for SSRIs. We release the results of a fast and easy radiolabeling method applied a one-step loop method with [11C]CH3OTf for routine clinical applications of 11C-sertraline. 1 mg of a precursor for 11C-sertraline in 0.1 mL DMF and 5 μL of 1N NaOH, were injected into the loop of semi-prep high-performance liquid chromatography (HPLC). [11C]CH3OTf was passed through the loop at room temperature (RT). The 11C-sertraline was separated by the semi-preparative HPLC. 11C-sertraline was eluted at 28.0 min was collected and evaluated by analytical HPLC and mass spectrometer. The total radiolabeling efficiency of 11C-sertraline was 30.7±8.7%. The specific activity was 64.8±51.4 GBq/μmol. The radiochemical and chemical purities were higher than 99%. The mass spectrum of the product showed m/z peaks at 307.1 (M+1), indicating the mass of sertraline. By the one-step loop method with [11C]CH3OTf, 11C-sertraline could be quickly and easily prepared for clinical application. J Radiopharm Mol Probes 3(1):32-37, 2017