Synthesis and preclinical evaluation of carbon-11 labelled N-((5-(4-fluoro-2-[C-11]methoxyphenyl) pyridin-3-yl) methyl) cyclopentanamine as a PET tracer for NR2B subunit-containing NMDA receptors

J.A.M. Christiaans, P.J. Klein, A. Metaxas, E.J.M. Kooijman, R.C. Schuit, J.E. Leysen, A.A. Lammertsma, B.N.M. van Berckel, A.D. Windhorst

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Abstract

Introduction: The N-methyl-D-Aspartate (NMDA) receptor plays an important role in learning and memory. Overactivation is thought to play an important role in neurodegenerative disorders such as Alzheimer's disease. Currently, it is not possible to assess N-methyl-D-aspartate receptor (NMDAr) bio-availability in vivo. The purpose of this study was to develop a positron emission tomography (PET) ligand for the NR2B binding site of the NMDA receptor. Methods: N-((5-(4-fluoro-2-methoxyphenyl)pyridin-3-yl)methyl)cyclopentanamine was radiolabelled with carbon-11 in the phenyl moiety. Biodistribution and blocking studies were carried out in anaesthetized mice and in non-anaesthetized rats. Results: N-((5-(4-fluoro-2-[
Original languageEnglish
Pages (from-to)670-680
JournalNuclear medicine and biology
Volume41
Issue number8
DOIs
Publication statusPublished - 2014

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