Use of 2-[18F]fluoroethylazide for the Staudinger ligation – Preparation and characterisation of GABAA receptor binding 4-quinolones |
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Authors: | Alessandra Gaeta John Woodcraft Stuart Plant Julian Goggi Paul Jones Mark Battle William Trigg Sajinder K Luthra Matthias Glaser |
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Institution: | 1. GE Healthcare, Medical Diagnostics, White Lion Road, Amersham HP7 9LL, UK;2. GE Healthcare, Medical Diagnostics, Hammersmith Hospital, London W12 0NN, UK |
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Abstract: | The labelling reagent 2-18F]fluoroethylazide was used in a traceless Staudinger ligation. This reaction was employed to obtain the GABAA receptor binding 6-benzyl-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid (2-18F]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/μmol. The compound showed low brain penetration in normal rats. A series of fluoroalkyl 4-quinolone analogues with nanomolar to sub-nanomolar affinity for the GABAA receptor has been prepared as well. |
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