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

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...

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Detalles Bibliográficos
Autores principales: Morris, Olivia, Gregory, J., Kadirvel, M., Henderson, Fiona, Blykers, A., McMahon, Adam, Taylor, Mark, Allsop, David, Allan, Stuart, Grigg, J., Boutin, Herve, Prenant, Christian
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Pergamon Press 2016
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5034901/
https://www.ncbi.nlm.nih.gov/pubmed/27518217
http://dx.doi.org/10.1016/j.apradiso.2016.07.023
Descripción
Sumario: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.

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