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11C-Labelling of N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamide derivatives and evaluation as potential radioligands for PET imaging of dopamine D3 receptors (Articolo in rivista)

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11C-Labelling of N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamide derivatives and evaluation as potential radioligands for PET imaging of dopamine D3 receptors (Articolo in rivista) (literal)

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Turolla E.A 1., Matarrese M. 1, Belloli S. 1, Moresco R.M. 1, Simonelli P. 1, Todde S. 1, Fazio F. 1, Magni F. 2, Galli Kienle M. 2, Leopoldo M. 3, Berardi F. 3, Colabufo N.A. 3, Lacivita E. 3, Perrone R. 3 (2005)
11C-Labelling of N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamide derivatives and evaluation as potential radioligands for PET imaging of dopamine D3 receptors
in Journal of medicinal chemistry
(literal)

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Turolla E.A 1., Matarrese M. 1, Belloli S. 1, Moresco R.M. 1, Simonelli P. 1, Todde S. 1, Fazio F. 1, Magni F. 2, Galli Kienle M. 2, Leopoldo M. 3, Berardi F. 3, Colabufo N.A. 3, Lacivita E. 3, Perrone R. 3 (literal)

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Radiosintesi di nuovi radiotraccianti marcati con Carbonio-11 per lo studio dei sistemi di neurotrasmissione coinvolti nelle patologie neurodegenerative e nella depressione. (literal)

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1. Institute of Molecular Bioimaging and Physiology-CNR, University of Milano-Bicocca, Institute San Raffaele, Milano, Italy 2. DIMESAB, University of Milano-Bicocca, Monza (MI), Italy 3. Dipartimento Farmaco-Chimico, Università degli Studi, Bari, Italy (literal)

Titolo

11C-Labelling of N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamide derivatives and evaluation as potential radioligands for PET imaging of dopamine D3 receptors (literal)

Abstract

The selective dopamine D(3) receptor ligands N-4-[4-[(2,3-dichlorophenyl)piperazin-1-yl]butyl]1-methoxy-2-naphthalencarboxamide (1) and N-4-[4-[(2,3-dichlorophenyl)piperazin-1-yl]butyl]-7-methoxy-2-benzofurancarboxamide (2) were labeled with (11)C (t(1/2) = 20.4 min) as potential radioligands for the noninvasive assessment of the dopamine D(3) neurotransmission system in vivo with positron emission tomography (PET). The radiosynthesis consisted in an O-methylation of the des-methyl precursors N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]-1-hydroxy-2-naphthalenecarboxamide (3) and N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]-7-hydroxy-2-benzofurancarboxamide (4) with [(11)C]methyl iodide using tBuOK/HMPA and KOH/DMSO, respectively. The radiotracers [(11)C]1 and [(11)C]2 were obtained in 35 min with over 99% radiochemical purity, 74 +/- 37 GBq/mumol of specific radioactivity, 13% and 26% radiochemical yield (EOB, decay-corrected). Distribution studies in rats demonstrated that the new tracers [(11)C]1 and [(11)C]2 cross the blood-brain barrier and localize in the brain. However, the kinetics of cerebral uptake did not reflect the regional expression of the D(3) receptors. Despite their in vitro pharmacological profile, [(11)C]1 and [(11)C]2 do not display an in vivo behavior suitable to image D(3) receptor expression using PET. (literal)

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