Use of 2-[(18)F]fluoroethylazide for the Staudinger ligation - Preparation and characterisation of GABA(A) receptor binding 4-quinolones.
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.
Gaeta
Alessandra
A
GE Healthcare, Medical Diagnostics, Amersham HP7 9LL, UK.
Woodcraft
John
J
Plant
Stuart
S
Goggi
Julian
J
Jones
Paul
P
Battle
Mark
M
Trigg
William
W
Luthra
Sajinder K
SK
Glaser
Matthias
M
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
D042462:4-Quinolones; D001386:Azides; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D011963:Receptors, GABA-A