title: Use of 2-[(18)F]fluoroethylazide for the Staudinger ligation - Preparation and characterisation of GABA(A) receptor binding 4-quinolones.
abstract: The labelling reagent 2-[(18)F]fluoroethylazide was used in a traceless Staudinger ligation. This reaction was employed to obtain the GABA(A) receptor binding 6-benzyl-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid (2-[(18)F]fluoroethyl) amide. The radiotracer was prepared with a non-decay corrected radiochemical yield of 7%, a radiochemical purity >95% and a specific radioactivity of 0.9 GBq/micromol. The compound showed low brain penetration in normal rats. A series of fluoroalkyl 4-quinolone analogues with nanomolar to sub-nanomolar affinity for the GABA(A) receptor has been prepared as well.
authors.affiliation: GE Healthcare, Medical Diagnostics, Amersham HP7 9LL, UK.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Gaeta
authors.forename: John
authors.initials: J
authors.lastname: Woodcraft
authors.forename: Stuart
authors.initials: S
authors.lastname: Plant
authors.forename: Julian
authors.initials: J
authors.lastname: Goggi
authors.forename: Paul
authors.initials: P
authors.lastname: Jones
authors.forename: Mark
authors.initials: M
authors.lastname: Battle
authors.forename: William
authors.initials: W
authors.lastname: Trigg
authors.forename: Sajinder K
authors.initials: SK
authors.lastname: Luthra
authors.forename: Matthias
authors.initials: M
authors.lastname: Glaser
mesh_terms: D042462:4-Quinolones / Q000737:chemistry*; D000818:Animals; D001386:Azides / Q000737:chemistry*; D001921:Brain / Q000000981:diagnostic imaging; D005462:Fluorine Radioisotopes / Q000737:chemistry; D011485:Protein Binding; D011859:Radiography; D019275:Radiopharmaceuticals / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011963:Receptors, GABA-A / Q000737:chemistry* / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D042462:4-Quinolones; D001386:Azides; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D011963:Receptors, GABA-A