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

作者：Morris Olivia^*; Gregory J; Kadirvel M; Henderson Fiona; Blykers A; McMahon Adam; Taylor Mark; Allsop David; Allan Stuart; Grigg J; Boutin Herve; Prenant Christian

来源：Applied Radiation and Isotopes, 2016, 116: 120-127.

DOI：10.1016/j.apradiso.2016.07.023

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

2-[F-18]-Fluoro-3-pyridinecarboxaldehyde ([F-18]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 [F-18]RI-OR2-TAT has been measured in Wistar rats.

• 出版日期2016-10