Enantiomeric Propanolamines as selective N-Methyl-d-aspartate 2B Receptor Antagonists†

…, M Geballe, E Gruszecka-Kowalik…

文献索引：Tahirovic, Yesim A.; Geballe, Matthew; Gruszecka-Kowalik, Ewa; Myers, Scott J.; Lyuboslavsky, Polina; Le, Phuong; French, Adam; Irier, Hasan; Choi, Woo-Baeg; Easterling, Keith; Yuan, Hongjie; Wilson, Lawrence J.; Kotloski, Robert; McNamara, James O.; Dingledine, Raymond; Liotta, Dennis C.; Traynelis, Stephen F.; Snyder, James P. Journal of Medicinal Chemistry, 2008 , vol. 51, # 18 p. 5506 - 5521

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被引用次数: 15

摘要

Enantiomeric propanolamines have been identified as a new class of NR2B-selective NMDA receptor antagonists. The most effective agents are biaryl structures, synthesized in six steps with overall yields ranging from 11− 64%. The compounds are potent and selective inhibitors of NR2B-containing recombinant NMDA receptors with IC50 values between 30− 100 nM. Potency is strongly controlled by substitution on both rings and the centrally ...