Synthesis and characterization of [18F]MCl-322 as a potential PET radiotracer for imaging the dopamine transporter

The fluoroethyl ester-containing phenyltropane derivative MCL-322 was shown to display high affinity to the dopamine transporter (DAT) (Ki = 2.3 nM). The binding affinities (Ki values) for the serotonin transporter and norepinephrine transporter were determined to be 5.1 nM and 280 nM, respectively [1]. The high binding affinities and selectivities of MCL-322 make the corresponding 18F-labelled compound an attractive PET radioligand for imaging DAT in brain tissue. Here, we report on the radiosynthesis of [18F]MCL-322 and its radiopharmacological characterization involving biodistribution, autoradiography and small animal PET studies.