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 radiotracer candidates for the NR2B subtype N-methyl-D-aspartate receptor

European Journal of Medicinal Chemistry
Radouane KoudihFranck Sobrio

Abstract

Diastereoisomeric compounds [(18)F]cis- and [(18)F]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.

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Citations

Apr 16, 2015·TheScientificWorldJournal·Takeshi FuchigamiSakura Yoshida
Sep 15, 2020·Expert Opinion on Therapeutic Patents·Hazem AhmedSimon M Ametamey
Mar 25, 2021·Organic Letters·Víctor García-VázquezJoseph P A Harrity
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Aug 21, 2013·The Journal of Organic Chemistry·Simon J ShawRajinder Singh
Mar 11, 2021·CNS & Neurological Disorders Drug Targets·Vinod UgaleAtul Shirkhedkar

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