Synthesis and in vivo evaluation of [18F]ORG 13063, a potential pet radioligand for the 5‐HT1A receptor

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Abstract
[18F]Org 13063 or 4‐[18F]fluoro‐N‐{2‐[4‐(6‐trifluoromethyl‐2‐pyridinyl)‐1‐piperazinyl]ethyl}benzamide was synthesized by nucleophilic aromatic substitution on the nitro precursor in a microwave oven (5 min, 700 W). Overall radiochemical yield was 20 % (EOB), chemical and radiochemical purity were respectively higher than 95 and 99 %. Specific activity was always higher than 18.5 GBq/μmol (500 mCi/μmol). Biodistribution studies in rabbits were performed leading to 0.77 % ID in the brain at 5 min p.i. Radioactivity concentration of brain was significantly higher than that of blood. However, no significant differences in % ID/g tissue of the different isolated brain regions (hippocampus, hypothalamus, striatum, cortex and cerebellum) could be demonstrated.