A series of PET imaging studies were conducted with two fluorine-18-labeled
tropane analoges, [F-18](+)-FTT and [F-18](+)-FCT. Both compounds possesse
d a high affinity and selectivity for the dopamine transporter and had a hi
gher accumulation in the basal ganglia, a brain region having a high densit
y of the dopamine transporter (DAT) than the cerebellum, a reference region
devoid of dopaminergic terminals. [F-18](+)-FCT had a higher brain uptake
and more suitable basal ganglia:cerebellum (BG:Cb) ratio than [F-18](+)-FTT
. [F-18](+)-FCT also displayed reversible binding kinetics in vivo, indicat
ing that the measurement of DAT density in vivo with PET will be relatively
insensitive to changes in cerebral blood flow that can occur as a conseque
nce of disease or prolonged cocaine abuse. The uptake of [F-18](+)-FCT was
also displaced by an intravenous injection of cocaine (1.0 mg/kg), which is
consistent with the labeling of the DAT in vivo by this radiotracer. These
data suggest that [F-18](+)-FCT may be a suitable radiotracer for studying
DAT function in vivo with PET. Synapse 37:109-117, 2000. (C) 2000 Wiley-Li
ss, Inc.