GBR-13119 is a blood-brain barrier-permeable inhibitor of the presynaptic dopamine uptake system . GBR-13119 binds to dopamine uptake sites with high selectivity, without being affected by other neurotransmitter reuptake inhibitors. GBR-13119 exhibits a lipophilic systemic distribution profile with extremely low defluorination in rats, while it shows a differential characteristic of slow striatal washout in the brain of primates. GBR-13119 can serve as a PET tracer to achieve visualized imaging of the striatum in primates, and can reflect MPTP-induced dopaminergic neuron degeneration through reduced uptake. GBR-13119 can be widely applied to studies related to Parkinson's disease and dopaminergic neuron degeneration.
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