Background: Parkinson's disease is a neurodegenerative disorder that is characterized by a degeneration of the dopaminergic system. Dopamine transporter (DAT) positron emission tomography (PET) imaging has emerged as a powerful and non-invasive method to quantify dopaminergic function in the living brain. The PET radioligand, [F]FE-PE2I, a cocaine chemical derivative, has shown promising properties for in vivo PET imaging of DAT, including high affinity and selectivity for DAT, excellent brain permeability, and favorable metabolism. The aim of the current study was to scale up the production of [F]FE-PE2I to fulfil the increasing clinical demand for this tracer.
Results: Thus, a fully automated and GMP-compliant production procedure has been developed using a commercially available radiosynthesis module GE TRACERLab FX2 N. [F]FE-PE2I was produced with a radiochemical yield of 39 ± 8% (n = 4, relative [F]F delivered to the module). The synthesis time was 70 min, and the molar activity was 925.3 ± 763 GBq/µmol (250 ± 20 Ci/µmol). The produced [F]FE-PE2I was stable over 6 h at room temperature.
Conclusion: The protocol reliably provides a sterile and pyrogen-free GMP-compliant product.
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| http://dx.doi.org/10.1186/s41181-024-00269-9 | DOI Listing |
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