Moroni F, Pellegrini-Giampietro D E, Alesiani M, Cherici G, Mori F, Galli A
Department of Preclinical and Clinical Pharmacology, Mario Aiazzi Mancini, University of Florence, Italy.
Eur J Pharmacol. 1989 Apr 12;163(1):123-6. doi: 10.1016/0014-2999(89)90404-4.
The responses evoked by stimulation of the N-methyl-D-aspartate receptors in the guinea-pig myenteric plexus were potentiated by micromolar concentrations of glycine and were non-competitively antagonized by kynurenate (IC50: 60 microM). The effects of kynurenate were competitively prevented by glycine. Furthermore, kynurenate displaced [3H]glycine from its binding sites on rat cortical membranes (IC50: 20 microM). Kynurenate and glycine, therefore, probably act at the same site, evoking opposite effects on the function of the ion channel complex of the N-methyl-D-aspartate receptor.
豚鼠肠肌丛中N-甲基-D-天冬氨酸受体受刺激所诱发的反应，在微摩尔浓度的甘氨酸作用下得到增强，且被犬尿烯酸非竞争性拮抗（半数抑制浓度：60微摩尔）。甘氨酸可竞争性地阻止犬尿烯酸的作用。此外，犬尿烯酸可将[3H]甘氨酸从其在大鼠皮层膜上的结合位点置换下来（半数抑制浓度：20微摩尔）。因此，犬尿烯酸和甘氨酸可能作用于同一部位，对N-甲基-D-天冬氨酸受体离子通道复合体的功能产生相反的影响。
