新型喹喔啉二酮对培养的小鼠皮层神经元中使君子氨酸反应表现出强效拮抗作用。
New quinoxalinediones show potent antagonism of quisqualate responses in cultured mouse cortical neurons.
作者信息
Drejer J, Honoré T
机构信息
Ferrosan Research Division, Department of Biochemistry, Soeborg, Denmark.
出版信息
Neurosci Lett. 1988 Apr 22;87(1-2):104-8. doi: 10.1016/0304-3940(88)90153-x.
Two new quinoxalines, DNQX (6,7-dinitro-quinoxaline-2,3-dion = FG 9041) and CNQX (6-nitro-7-cyano-quinoxaline-2,3-dion = FG 9065), were tested as antagonists of excitatory amino acid responses in cultured neurons and brain slices. DNQX and CNQX showed potent competitive antagonism of quisqualate and kainate induced [3H]GABA release from cultured mouse cortical neurons with weaker effects on NMDA responses (Schild values for DNQX were 6.2, 5.9 and 5.4, respectively). Also in a model of excitatory amino acid induced 22Na efflux from striatal slices DNQX blocked responses to quisqualate and kainate more effectively than responses to NMDA.
两种新的喹喔啉类化合物，DNQX（6,7-二硝基喹喔啉-2,3-二酮 = FG 9041）和CNQX（6-硝基-7-氰基喹喔啉-2,3-二酮 = FG 9065），作为兴奋性氨基酸反应的拮抗剂在培养的神经元和脑片中进行了测试。DNQX和CNQX对quisqualate和海人藻酸诱导的来自培养的小鼠皮层神经元的[3H]GABA释放表现出强效竞争性拮抗作用，对NMDA反应的作用较弱（DNQX的Schild值分别为6.2、5.9和5.4）。同样，在兴奋性氨基酸诱导纹状体切片中22Na外流的模型中，DNQX对quisqualate和海人藻酸反应的阻断作用比对NMDA反应更有效。
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