A new class of agonists and antagonist of N-methyl-D-aspartic acid receptors: Derivatives of imidozole-4,5- and pyrazole-3,4-dicarboxylic acids

L. B. Piotrovskii, P. V. Lishko, A. P. Maksimyuk, I. Y. Aleksandrova, O. A. Kryshtal

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Abstract

Studies of imidazole-4,5- and pyrazole-3,4-dicarboxylic acid derivatives revealed a number of new agonists and antagonists of N-methyl-D-aspartic acid (NMDA) receptors. Studies were based on whole-cell patch-clamp methods applied to rat hippocampus pyramidal cells. Increases in the lipophilicity of the environment of the nitrogen atom, keeping the distance between the terminal acid functions constant, led to a weakening of NMDA antagonism and increases in NMDA antagonism. Increases in the lipophilicity around the nitrogen atom could also lead to less selectivity in the interaction with NMDA receptors and the appearance of non-NMDA antagonist properties.

Original languageEnglish
Article numberBF02462614
Pages (from-to)553-558
Number of pages6
JournalNeuroscience and Behavioral Physiology
Volume30
Issue number5
DOIs
StatePublished - 2000

Keywords

  • Agonist
  • Antagonist
  • Lipophilicity
  • NMDA

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