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

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  • Olivia Morris
  • J. Gregory
  • M. Kadirvel
  • Fiona Henderson
  • A. Blykers
  • Adam McMahon
  • Mark Neville Taylor
  • David Allsop
  • Stuart Allan
  • J. Grigg
  • Herve Boutin
  • Christian Prenant
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<mark>Journal publication date</mark>10/2016
<mark>Journal</mark>Applied Radiation and Isotopes
Volume116
Number of pages8
Pages (from-to)120-127
Publication statusPublished
Early online date27/07/16
Original languageEnglish

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.