巴比妥酸
致电离效应
NMDA受体
红藻氨酸
红藻氨酸受体
天冬氨酸
化学
受体
2-氨基-5-磷酸新戊酯
变构调节
甘氨酸
谷氨酸受体
药理学
生物化学
生物
AMPA受体
氨基酸
兴奋性氨基酸拮抗剂
作者
M Bertolino,Stefano Vicini,E. Costa
标识
DOI:10.1016/0028-3908(89)90078-6
摘要
The action of kynurenic acid on currents elicited by the activation of amino acid receptors was investigated in primary cultures of cortical neurons prepared from neonatal rats. Kynurenic acid was tested on currents elicited by both N-methyl-d-aspartic acid (NMDA) and kainate, using patch-clamp recording techniques in “outside-out” and “whole-cell” configurations. The inhibition by kynurenic acid was compared with that elicited by amino-phosphono-valeric acid (APV). Whole-cell currents, elicited by increasing doses of NMDA, were antagonized competitively by APV and non-competitively by kynurenic acid (ID50 70 μM); in contrast, kynurenic acid inhibited competitively the whole-cell currents elicited by kainic acid (id50) 500 μM). The non-competitive inhibition by kynurenic acid of the whole cell currents elicited by NMDA was antagonized competitively by glycine, a specific positive allosteric modulator of NMDA receptors; on the other hand glycine failed to change the inhibition by APV of the NMDA-elicited responses. Thus, kynurenic acid inhibits NMDA receptors allosterically (non-competitively) and kainic acid receptors isosterically (competitively).
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