一种特异性甘氨酸拮抗剂6,7-二氯喹喔啉-2,3-二酮（DCQX）对N-甲基-D-天冬氨酸（NMDA）介导反应的消除作用。
Abolition of the NMDA-mediated responses by a specific glycine antagonist, 6,7-dichloroquinoxaline-2,3-dione (DCQX).
作者信息
Yoneda Y, Ogita K
机构信息
Department of Pharmacology, Setsunan University, Osaka, Japan.
出版信息
Biochem Biophys Res Commun. 1989 Oct 31;164(2):841-9. doi: 10.1016/0006-291x(89)91535-0.
Among various quinoxaline derivatives examined, only 6,7-dichloroquinoxaline-2,3-dione (DCQX) competitively displaced the strychnine-insensitive binding of [3H]glycine, without affecting the other binding sites on the N-methyl-D-aspartate (NMDA) receptor complex. This novel specific antagonist abolished the ability of L-glutamate to potentiate [3H]MK-801 binding activity in brain synaptic membranes treated with Triton X-100. Inclusion of glycine reversed this preventive action of DCQX on the potentiation induced by glutamate.
在所检测的各种喹喔啉衍生物中，只有6,7-二氯喹喔啉-2,3-二酮（DCQX）能竞争性取代[3H]甘氨酸与士的宁不敏感位点的结合，而不影响N-甲基-D-天冬氨酸（NMDA）受体复合物上的其他结合位点。这种新型特异性拮抗剂消除了L-谷氨酸增强经Triton X-100处理的脑突触膜中[3H]MK-801结合活性的能力。加入甘氨酸可逆转DCQX对谷氨酸诱导增强作用的这种抑制作用。
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