845271-52-5Relevant academic research and scientific papers
Synthesis and preliminary in vivo evaluation of 4-[18F]fluoro-N- {2-[4-(6-trifluoromethylpyridin-2-yl) piperazin-1-yl]ethyl}benzamide, a potential PET radioligand for the 5-HT1A receptor
Vandecapelle,Dumont,De Vos,Strijckmans,Leysen,Audenaert,Dierckx,Slegers
, p. 531 - 542 (2004)
4-Fluoro-N-{2-[4-(6-trifluoromethylpyridin-2-yl)piperazin-1-yl]ethyl} benzamide is a full 5-HT1A agonist with high affinity (pK i=9.3), selectivity and a clog P of 3.045. The corresponding PET radioligand 4-[18F]fluoro-N-{2-[4-(6-trifluoromethylpyridin-2-yl) piperazin-1-yl]ethyl}benzamide was synthesized by nucleophilic aromatic substitution on the nitro precursor. The fluorinating agent K[ 18F]F/Kryptofix 2.2.2 was both dried (9 min, 700 W) and incorporated in the precursor (5 min, 700 W) using a commercially available microwave oven. In a total synthesis time of 60 min, an overall radiochemical yield of 18% (SD=5, n=7, EOS) was obtained. Radiochemical purity was always higher than 99% and specific activity always higher than 81.4 GBq/μmol (2.2 Ci/μmol). Initial brain uptake in mice was 2.19% ID (5.47% ID/g, 2 min) but decreased rapidly (0.17% ID, 0.45% ID/g (60 min)). During the first 20 min p.i., radioactivity concentration of the brain was significantly higher than that of blood demonstrating good brain entry of the tracer. Copyright
Synthesis and in vivo evaluation of [18F]Org 13063, a potential PET radioligand for the 5-HT1A receptor
Vandecapelle, M.,Vos, F. De,Vermeirsch, H.,Strijckmans, K.,Leysen, D.,Audenaert, K.,Dierckx, R. A.,Siegers, G.
, p. S201 - S203 (2007/10/03)
[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 percent (EOB), chemical and radiochemical purity were respectively higher than 95 and 99 percent. Specific activity was always higher than 18.5 GBq/μmol (500 mCi/μmol). Biodistribution studies in rabbit were performed leading to 0.77 percent ID in the brain at 5 min p.i. Radioactivity concentration in brain was significantly higher than that of blood. However, no significant differences in percent ID/g tissue of the different isolated brain regions (hippocampus, hypothalamus, striatum, cortex and cerebellum) could be demonstrated.
