Development & Automation of a novel [18F]F prosthetic group, 2-[18F]-fluoro-3-pyridinecarboxaldehyde, and its application to an amino(oxy)-functionalised Aβ peptide

Olivia Morris, J. Gregory, M. Kadirvel, Fiona Henderson, A. Blykers, Adam McMahon, Mark Taylor, David Allsop, Stuart Allan, J. Grigg, Herve Boutin, Christian Prenant

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Abstract

2-[18F]-Fluoro-3-pyridinecarboxaldehyde ([18F]FPCA) is a novel, water-soluble prosthetic group. It’s radiochemistry has been developed and fully-automated for application in chemoselective radiolabelling of amino(oxy)-derivatised RI-OR2-TAT peptide, (Aoa-k)-RI-OR2-TAT, using a GE TRACERlab FX-FN. RI-OR2-TAT is a brain-penetrant, retro-inverso peptide that binds to amyloid species associated with Alzheimer’s Disease. Radiolabelled (Aoa-k)-RI-OR2-TAT was reproducibly synthesised and the product of the reaction with FPCA has been fully characterised. In-vivo biodistribution of [18F]RI-OR2-TAT has been measured in Wistar rats.
Original languageEnglish
Pages (from-to)120–127
Number of pages8
JournalApplied Radiation and Isotopes
Volume116
Early online date27 Jul 2016
DOIs
Publication statusPublished - 1 Oct 2016

Keywords

  • [F-18]F prosthetic group
  • PET
  • A beta peptide
  • Chemical ligation
  • Oxime bond

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