title: 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.
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.
authors: Wolfson Molecular Imaging Centre, CRUK/EPSRC Imaging Centre of Cambridge & Manchester, The University of Manchester, UK. Electronic address: olivia.morris-2@postgrad.manchester.ac.uk.
authors: Olivia
authors: O
authors: Morris
authors: Wolfson Molecular Imaging Centre, CRUK/EPSRC Imaging Centre of Cambridge & Manchester, The University of Manchester, UK.
authors: J
authors: J
authors: Gregory
authors: Wolfson Molecular Imaging Centre, CRUK/EPSRC Imaging Centre of Cambridge & Manchester, The University of Manchester, UK.
authors: M
authors: M
authors: Kadirvel
authors: Wolfson Molecular Imaging Centre, CRUK/EPSRC Imaging Centre of Cambridge & Manchester, The University of Manchester, UK.
authors: Fiona
authors: F
authors: Henderson
authors: In-Vivo Cellular and Molecular Imaging Lab, Vrije Universiteit Brussel, Belgium.
authors: A
authors: A
authors: Blykers
authors: Wolfson Molecular Imaging Centre, CRUK/EPSRC Imaging Centre of Cambridge & Manchester, The University of Manchester, UK.
authors: Adam
authors: A
authors: McMahon
authors: Division of Biomedical and Life Sciences, The University of Lancaster, UK.
authors: Mark
authors: M
authors: Taylor
authors: Division of Biomedical and Life Sciences, The University of Lancaster, UK.
authors: David
authors: D
authors: Allsop
authors: The University of Manchester, UK.
authors: Stuart
authors: S
authors: Allan
authors: GE Healthcare, Life Sciences, Imaging R&D, The Grove Centre, Amersham, Bucks, UK.
authors: J
authors: J
authors: Grigg
authors: Wolfson Molecular Imaging Centre, CRUK/EPSRC Imaging Centre of Cambridge & Manchester, The University of Manchester, UK.
authors: Herve
authors: H
authors: Boutin
authors: Wolfson Molecular Imaging Centre, CRUK/EPSRC Imaging Centre of Cambridge & Manchester, The University of Manchester, UK.
authors: Christian
authors: C
authors: Prenant
mesh_terms: D016229:Amyloid beta-Peptides / Q000737:chemistry* / Q000378:metabolism*; D000818:Animals; D005462:Fluorine Radioisotopes / Q000737:chemistry* / Q000493:pharmacokinetics*; D007553:Isotope Labeling / Q000379:methods; D008657:Metabolic Clearance Rate; D009928:Organ Specificity; D049268:Positron-Emission Tomography / Q000379:methods*; D011485:Protein Binding; D011725:Pyridines / Q000737:chemistry / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D012371:Robotics / Q000379:methods; D014018:Tissue Distribution
chemical_list: D016229:Amyloid beta-Peptides; D005462:Fluorine Radioisotopes; D011725:Pyridines; D019275:Radiopharmaceuticals; C051439:pyridinecarboxaldehyde; C000615276:Fluorine-18
keywords: Aβ peptide; Chemical ligation; Oxime bond; PET; [(18)F]F prosthetic group