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喹喔啉二酮:强效竞争性非NMDA谷氨酸受体拮抗剂。

Quinoxalinediones: potent competitive non-NMDA glutamate receptor antagonists.

作者信息

Honoré T, Davies S N, Drejer J, Fletcher E J, Jacobsen P, Lodge D, Nielsen F E

机构信息

Ferroson Research Division, Soeborg, Denmark.

出版信息

Science. 1988 Aug 5;241(4866):701-3. doi: 10.1126/science.2899909.

Abstract

The N-methyl-D-aspartate (NMDA)-subtype of glutamate receptors has been well described as a result of the early appearance of NMDA antagonists, but no potent antagonist for the "non-NMDA" glutamate receptors has been available. Quinoxalinediones have now been found to be potent and competitive antagonists at non-NMDA glutamate receptors. These compounds will be useful in the determination of the structure-activity relations of quisqualate and kainate receptors and the role of such receptors in synaptic transmission in the mammalian brain.

摘要

由于N-甲基-D-天冬氨酸(NMDA)受体拮抗剂的早期出现,谷氨酸受体的NMDA亚型已得到充分描述,但尚无针对“非NMDA”谷氨酸受体的有效拮抗剂。现已发现喹喔啉二酮是强效且具有竞争性的非NMDA谷氨酸受体拮抗剂。这些化合物将有助于确定quisqualate和kainate受体的构效关系以及此类受体在哺乳动物大脑突触传递中的作用。

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