5-AMINOMETHYLQUINOXALINE-2,3-DIONES, PART-III - ARYLAMIDE DERIVATIVESAS HIGHLY POTENT AND SELECTIVE GLYCINE-SITE NMDA RECEPTOR ANTAGONISTS

A series of quinoxaline-2,3-diones with very high affinity to the glyc ine site of the NMDA receptor has been discovered. In contrast to the 7-nitro derivatives, the most potent 7-bromo substituted compounds wer e highly selective for the glycine site. Although none of the describe d compounds were active in the electroshock model in mice, la displaye d significant protection in the quinolinic acid-induced excitotoxicity model in vivo. (C) 1998 Elsevier Science Ltd. All rights reserved.