Piperazine-2, 3-dicarboxylic acid derivatives as dual antagonists of NMDA and GluK1-containing kainate receptors

…, R Eaves, R Morley, MB Mayo-Martin…

文献索引：Irvine, Mark W.; Costa, Blaise M.; Dlaboga, Daniel; Culley, Georgia R.; Hulse, Richard; Scholefield, Caroline L.; Atlason, Palmi; Fang, Guangyu; Eaves, Richard; Morley, Richard; Mayo-Martin, Maria B.; Amici, Mascia; Bortolotto, Zuner A.; Donaldson, Lucy; Collingridge, Graham L.; Molnar, Elek; Monaghan, Daniel T.; Jane, David E. Journal of Medicinal Chemistry, 2012 , vol. 55, # 1 p. 327 - 341

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被引用次数: 9

摘要

Competitive N-methyl-d-aspartate receptor (NMDAR) antagonists bind to the GluN2 subunit, of which there are four types (GluN2A-D). We report that some N1-substituted derivatives of cis-piperazine-2, 3-dicarboxylic acid display improved relative affinity for GluN2C and GluN2D versus GluN2A and GluN2B. These derivatives also display subtype selectivity among the more distantly related kainate receptor family. Compounds 18i and (−)-4 were ...