Development & automation of a novel [18F]F prosthetic group, 2-[18F]-fluoro-3-pyridinecarboxaldehyde, and its application to an amino(oxy)-functionalised Aβ peptide. (October 2016)

• Record Type: Journal Article
• Authors: Morris, Olivia; Gregory, J.; Kadirvel, M.; Henderson, Fiona; Blykers, A.; McMahon, Adam; Taylor, Mark; Allsop, David; Allan, Stuart; Grigg, J.; Boutin, Herve; Prenant, Christian
• Is Part Of: Applied radiation and isotopes. Volume 116(2016:Oct.)
• Page Start: 120
• Page End: 127
• Publication Date: 2016-10
• Subjects: [18F]F prosthetic group -- PET -- Aβ peptide -- Chemical ligation -- Oxime bond; Radiology -- Periodicals; Radiation -- Industrial applications -- Periodicals; Nuclear chemistry -- Periodicals; Internet resource; Periodical; 660.298
• DOI: 10.1016/j.apradiso.2016.07.023
• Languages: English
• ISSNs: 0969-8043

Abstract

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