Synthesis and in vitro characterization of trans-and cis-[18 F]-4-methylbenzyl 4-[(pyrimidin-2-ylamino) methyl]-3-fluoropiperidine-1-carboxylates as new potential PET …

R Koudih, G Gilbert, M Dhilly, A Abbas, L Barré…

Index: Koudih, Radouane; Gilbert, Gwenaelle; Dhilly, Martine; Abbas, Ahmed; Barre, Louisa; Debruyne, Daniele; Sobrio, Franck European Journal of Medicinal Chemistry, 2012 , vol. 53, p. 408 - 415

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Citation Number: 6

Abstract

Diastereoisomeric compounds [18F] cis-and [18F] 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 logD7. 4 values ...

~63%

Synthesis and SAR of substituted tetrahydrocarbazole derivat...

[Di Fabio, Romano; Giovannini, Riccardo; Bertani, Barbara; Borriello, Manuela; Bozzoli, Andrea; Donati, Daniele; Falchi, Alessandro; Ghirlanda, Damiano; Leslie, Colin P.; Pecunioso, Angelo; Rumboldt, Giovanna; Spada, Simone Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 6 p. 1749 - 1752]