(3-Methoxy-naphthalen)-2-yl-(1-benzyl-piperidin)-4-yl-acetate (SB-235753) was labelled with 11C (t(1/2) = 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.
Synthesis and in vivo evaluation of 3-[C-11]methyl-(3-methoxy-naphthalen)-2-yl-(1-benzyl-piperidin)-4-yl-ace tate (SB-235753), as a putative dopamine D-4 receptors antagonist for PET / M. Matarrese, D. Soloviev, R. Moresco, S. Todde, P. Simonelli, D. Colombo, F. Magni, A. Carpinelli, F. Fazio, M. Kienle. - In: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS. - ISSN 0362-4803. - 43:4(2000), pp. 359-374.
|Titolo:||Synthesis and in vivo evaluation of 3-[C-11]methyl-(3-methoxy-naphthalen)-2-yl-(1-benzyl-piperidin)-4-yl-ace tate (SB-235753), as a putative dopamine D-4 receptors antagonist for PET|
|Settore Scientifico Disciplinare:||Settore BIO/10 - Biochimica|
|Data di pubblicazione:||2000|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1002/(SICI)1099-1344(20000330)43:4<359::AID-JLCR323>3.3.CO;2-M|
|Appare nelle tipologie:||01 - Articolo su periodico|