INTRODUCTION: The regional brain distribution of (2R,3R)-5-[(18)F]fluoroethoxy-benzovesamicol ((-)-[(18)F]FEOBV), a radioligand for the vesicular acetylcholine transporter (VAChT), was examined in vivo in mice, rats and rhesus monkeys. METHODS: Regional brain distributions of (-)-[(18)F]FEOBV in mice were determined using ex vivo dissection. MicroPET imaging was used to determine the regional brain pharmacokinetics of the radioligand in rat and rhesus monkey brains. RESULTS: In all three species, clear heterogeneous regional brain distributions were obtained, with the rank order of brain tissues (striatum>thalamus>cortex>cerebellum) consistent with the distribution of cholinergic nerve terminals containing the VAChT. CONCLUSIONS: (-)-[(18)F]FEOBV remains a viable candidate for further development as an in vivo imaging agent for positron emission tomography (PET) studies of the VAChT in the human brain.
INTRODUCTION: The regional brain distribution of (2R,3R)-5-[(18)F]fluoroethoxy-benzovesamicol ((-)-[(18)F]FEOBV), a radioligand for the vesicular acetylcholine transporter (VAChT), was examined in vivo in mice, rats and rhesus monkeys. METHODS: Regional brain distributions of (-)-[(18)F]FEOBV in mice were determined using ex vivo dissection. MicroPET imaging was used to determine the regional brain pharmacokinetics of the radioligand in rat and rhesus monkey brains. RESULTS: In all three species, clear heterogeneous regional brain distributions were obtained, with the rank order of brain tissues (striatum>thalamus>cortex>cerebellum) consistent with the distribution of cholinergic nerve terminals containing the VAChT. CONCLUSIONS: (-)-[(18)F]FEOBV remains a viable candidate for further development as an in vivo imaging agent for positron emission tomography (PET) studies of the VAChT in the human brain.
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