IRIS – Institutional Research Information System
IRIS è il sistema di gestione della ricerca dell’Università degli Studi di Milano-Bicocca.Il repository BOA è il modulo del sistema dedicato alla raccolta e alla disseminazione della produzione scientifica di Ateneo. Le pubblicazioni sono ricercabili per parola chiave attraverso il box nella barra orizzontale in alto oppure, mediante il pulsante Sfoglia, per "Afferenza", "Autore", "Titolo", "Tipologia" o "Settore scientifico-disciplinare".
IRIS contiene inoltre alcuni moduli dedicati alla registrazione dei progetti e dei contratti, e alla reportistica avanzata per le attività di valutazione della ricerca
EnglishThe 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.
Turolla, E.A., Matarrese, M., Belloli, S., Moresco, R.M., Simonelli, P., Todde, S., et al. (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. JOURNAL OF MEDICINAL CHEMISTRY, 48(22), 7018-7023 [10.1021/jm050171k].
| Citazione: | Turolla, E.A., Matarrese, M., Belloli, S., Moresco, R.M., Simonelli, P., Todde, S., et al. (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. JOURNAL OF MEDICINAL CHEMISTRY, 48(22), 7018-7023 [10.1021/jm050171k]. | |
| Tipo: | Articolo in rivista - Articolo scientifico | |
| Carattere della pubblicazione: | Scientifica | |
| 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 | |
| Autori: | Turolla, EA; Matarrese, M; Belloli, S; Moresco, RM; Simonelli, P; Todde, S; Fazio, F; Magni, F; Kienle, MG; Leopoldo, M; Berardi, F; Colabufo, NA; Lacivita, E; Perrone, R | |
| Autori: | ||
| Data di pubblicazione: | 2005 | |
| Lingua: | English | |
| Rivista: | JOURNAL OF MEDICINAL CHEMISTRY | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1021/jm050171k | |
| Appare nelle tipologie: | 01 - Articolo su rivista |
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