<p>This study employed a solid-phase synthesis method to modify melittin, obtaining the labeled precursor NOTA-melittin. The aluminum fluoride method was used for the automated radiosynthesis of [<sup>18</sup>F]AlF-NOTA-melittin via an AllinOne module, achieving a radiochemical yield (RCY) of over 30%, with a synthesis time of approximately 30&#xa0;min and a radiochemical purity surpassing 97%. Biodistribution studies in both normal mice and small animal PET experiments revealed that the drug exhibited significant uptake in the blood, with the liver showing the highest accumulation followed by the kidneys. This suggests that the primary site of drug metabolism is the liver, with subsequent metabolism occurring in the kidneys.</p>

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Simple automated radiosynthesis of [18F]AlF-NOTA-melittin and biodistribution in normal mice

  • Chuanyin Sun,
  • Guolin Wang,
  • Chengjun Yao,
  • Ahmad Alhaskawi,
  • Yanzhao Dong,
  • Xiangping Chen,
  • Xinhui Su,
  • Hui Lu,
  • Zhenfeng Liu

摘要

This study employed a solid-phase synthesis method to modify melittin, obtaining the labeled precursor NOTA-melittin. The aluminum fluoride method was used for the automated radiosynthesis of [18F]AlF-NOTA-melittin via an AllinOne module, achieving a radiochemical yield (RCY) of over 30%, with a synthesis time of approximately 30 min and a radiochemical purity surpassing 97%. Biodistribution studies in both normal mice and small animal PET experiments revealed that the drug exhibited significant uptake in the blood, with the liver showing the highest accumulation followed by the kidneys. This suggests that the primary site of drug metabolism is the liver, with subsequent metabolism occurring in the kidneys.