Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl) phenyl-spaced. alpha.-amino acids as competitive N-methyl-D-aspartic acid …

…, G Johnson, DF Ortwine, JT Drummond…

Index: Bigge, Christopher F.; Johnson, Graham; Ortwine, Daniel F.; Drummond, James T.; Retz, Daniel M.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 8 p. 1371 - 1384

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Citation Number: 55

Abstract

A series of N-substituted a-amino acids containing terminal phosphonic acid groups has been synthesized as potential N-methybaspartate (NMDA) receptor antagonists. NMDA receptor affinity was determined by displacement of a known ligand ([3H] CPP) from crude rat brain synaptic membranes; an antagonist action was demonstrated by the inhibition of glutamate-induced accumulation of [% a2+] in cultured rat cortical neurons. Receptor ...