M. Matarrese, D. Soloviev, R. Moresco
Mar 30, 2000
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
(3-Methoxy-naphthalen)2-yl-(1-benzyl-piperidin)4-yl-acetate (SB-235753) was labelled with 11C (t1/2=20·4 min) as a putative radioligand for the non-invasive assessment of Dopamine D4 receptors in vivo with positron emission tomography (PET). The precursor for the radiosynthesis 3-hydroxynaphthyl-2-[N-benzyl)-piperidyl]-acetate hydrochloride was prepared by a four-step synthesis starting from ethyl-4-pyridyl acetate. The radiolabelling consisted of methylation with [11C]methyltriflate in dimethylformamide in the presence of potassium hydroxide. [11C]SB-235753, was synthesised in 30 min with a radiochemical yield of 10±5% (EOS, non-decay corrected) with 99% radiochemical purity and specific radioactivity of 10±3 Ci/μmol. Biodistribution studies in rats with [11C]SB-235753 showed the uniform distribution of the tracer within different areas of the murine brain. At 30 min after injection 99% of the radioligand in plasma and 100% in cerebellum was metabolised. These findings suggest that [11C]SB-235753 can not be a suitable tracer for dopamine D4 receptor studies with PET. Copyright © 2000 John Wiley & Sons, Ltd.