AI Article Synopsis

  • This study looked at a new PET scanning agent called [F]LBT-999 to see how it spreads and works in the brain, especially focusing on dopamine transporters, which are important for brain function.
  • Eight healthy people received [F]LBT-999 and then had their brains scanned to check how well it worked without causing any side effects.
  • The results showed that [F]LBT-999 was good at showing areas in the brain with high dopamine activity, especially in parts called the caudate and putamen, making it a helpful tool for doctors to look at how dopamine functions in the brain.

Article Abstract

Background: The aim of this study was to evaluate in healthy human brain the distribution, uptake, and kinetics of [F]LBT-999, a PET ligand targeting the dopamine transporter, to assess its ability to explore dopaminergic innervation, using a shorter protocol, more convenient for patients than currently with [I]ioflupane.

Methods: After intravenous injection of [F]LBT-999, 8 healthy subjects (53-80y) underwent a dynamic PET-scan. Venous samples were concomitantly obtained for metabolites analysis. Time activity curves (TACs) were generated for several ROIs (caudate, putamen, occipital cortex, substantia nigra and cerebellum). Cerebellum was used as reference region to calculate binding potentials (BPND).

Results: No adverse events or detectable pharmacological effects were reported. [F]LBT-999 PET revealed a good cerebral distribution, with an intense and symmetric uptake in both putamen and caudate (BPND of 6.75±1.17 and 6.30±1.17, respectively), without other brain abnormal tracer accumulation. Regional TACs showed a plateau from the maximal uptake, 20min pi, to the end of the acquisition for both caudate and putamen, whereas uptake in substantia nigra decreased progressively. A faster clearance and lowest BPND values were observed in both cortex and cerebellum. Ratios to the cerebellum exhibit value of about 3 in substantia nigra, close to 10 for both caudate and putamen, and remained around the value of 1 in cortex. The parent fraction of [F]LBT-999 in plasma was 80%, 60% and 45% at 15, 30 and 45 min pi, respectively.

Conclusions: These findings support the usefulness of [F]LBT-999 for a quantitative clinical evaluation of presynaptic dopaminergic innervation.

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http://dx.doi.org/10.23736/S1824-4785.19.03175-3DOI Listing

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