… . Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D- …

PD Leeson, R Baker, RW Carling…

Index: Leeson, Paul D.; Baker, Raymond; Carling, Robert W.; Curtis, Neil R.; Moore, Kevin W.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 4 p. 1243 - 1252

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Citation Number: 155

Abstract

Derivatives of the nonselective excitatory amino acid antagonist kynurenic acid (4oxo-1, 4- dihydroq~ o~~ 2-~~~~ c acid, 1) have been synthesized and evaluated for in vitro antagonist activity at the excitatory amino acid receptors sensitive to N-methyl-Baspartic acid (NMDA), quisqualic acid (QUIS or AMPA), and kainic acid (KA). Introduction of substituents at the 5-, 7- , and 5, 7-positions resulted in analogues having selective NMDA antagonist action, as a ...