Synthesis, evaluation and metabolic studies of radiotracers containing a 4-(4-[18 F]-fluorobenzyl) piperidin-1-yl moiety for the PET imaging of NR2B NMDA receptors

…, M Dhilly, A Abbas, O Tirel, A Buisson, J Henry…

文献索引：Labas, Romain; Gilbert, Gwenaelle; Nicole, Olivier; Dhilly, Martine; Abbas, Ahmed; Tirel, Olivier; Buisson, Alain; Henry, Joel; Barre, Louisa; Debruyne, Daniele; Sobrio, Franck European Journal of Medicinal Chemistry, 2011 , vol. 46, # 6 p. 2295 - 2309

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被引用次数: 14

摘要

In this study, novel specific PET radioligands containing the 4-(4-fluorobenzyl) piperidine moiety and selectively antagonistic for the NR2B subunit containing NMDA receptors were developed. Two antagonists, RGH-896 (1a) and 4-(4-fluorobenzyl) piperidinyl-1-methyl-2- benzimidazol-5-ol (2a), belonging to two different structural families, were radiolabeled by an aromatic nucleophilic radiofluorination followed by a reduction of the para-position ...