Piotrovskii L B, Lishko P V, Maksimyuk A P, Aleksandrova I Y, Kryshtal O A
Institute of Experimental Medicine, Russian Academy of Medical Sciences, St. Petersburg.
Neurosci Behav Physiol. 2000 Sep-Oct;30(5):553-8. doi: 10.1007/BF02462614.
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 of selectivity in the interaction with NMDA receptors and the appearance of non-NMDA antagonist properties.
对咪唑-4,5-二羧酸和吡唑-3,4-二羧酸衍生物的研究揭示了许多新型N-甲基-D-天冬氨酸（NMDA）受体激动剂和拮抗剂。研究基于应用于大鼠海马锥体细胞的全细胞膜片钳方法。在保持末端酸官能团之间距离不变的情况下，氮原子周围环境亲脂性的增加会导致NMDA拮抗作用减弱和NMDA拮抗作用增强。氮原子周围亲脂性的增加还可能导致与NMDA受体相互作用的选择性降低以及非NMDA拮抗剂特性的出现。
