Potent quinoxaline-spaced phosphono. alpha.-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation

…, LP Greenblatt, IL Jirkovsky, M Conklin…

Index: Baudy, Reinhardt B.; Greenblatt, Lynne P.; Jirkovsky, Ivo L.; Conklin, Mary; Russo, Ralph J.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 3 p. 331 - 342

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Citation Number: 58

Abstract

A series of a-amino-3-(phosphonoalkyl)-2-quinoxalinepropanoic acids was synthesized and evaluated for NMDA receptor affinity using a [3Hl CPP binding assay. Functional antagonism of the NMDA receptor complex was evaluated in vitro using a stimulated [3HlTCP binding assay and in vivo by employing an NMDA-induced seizure model. Some analogues also were evaluated in the I3H1-glycine binding assay. Several compounds of ...