Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue -, Pages 408-415Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.04.011
Keywords
Fluorine-18; PET; NR2B NMDA receptors; In vitro binding; Radiotracer; Radiolabelling
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Funding
- Ministere de l'Enseignement Superieur et de la Recherche
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Diastereoisomeric compounds [F-18]cis- and [F-18]trans-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoro-piperidine-1-carboxylates were successfully synthesized as new subtype-selective PET radiotracers for imaging the NR2B subunit containing NMDA receptors. Rat brain section autoradiographies demonstrated a high specific binding in NR2B/NMDA receptor rich regions for both radioligands. The measured logD(7.4) values as well as B-max/K-d ratios indicated that both radiotracers possess the adequate properties required for PET radiotracers. (C) 2012 Elsevier Masson SAS. All rights reserved.
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