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6,7-二氯-3-羟基-2-喹喔啉羧酸酯对新生大鼠脊髓兴奋性氨基酸受体的拮抗作用概况

Antagonist profile of 6,7-dichloro-3-hydroxy-2-quinoxalinecarboxylate at excitatory amino acid receptors in the neonatal rat spinal cord.

作者信息

Birch P J, Grossman C J, Hayes A G

机构信息

Department of Neuropharmacology, Glaxo Group Research Ltd., Ware, Herts., U.K.

出版信息

Eur J Pharmacol. 1989 Apr 12;163(1):127-31. doi: 10.1016/0014-2999(89)90405-6.

Abstract

In the neonatal rat spinal cord, 6,7-dichloro-3-hydroxy-2- quinoxalinecarboxylate antagonised responses mediated at both N-methyl-D-aspartate (NMDA) and non-NMDA receptors. The antagonism of responses to NMDA was unsurmountable and mediated via an antagonist action at the allosterically-linked strychnine-insensitive glycine site. At non-NMDA receptors, 6,7-dichloro-3-hydroxy-2-quinoxalinecarboxylate appeared to act as a competitive antagonist at low concentrations and a non-competitive antagonist at higher concentrations. In contrast to published data, this antagonist did not distinguish between the responses mediated by DL-alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionate (AMPA) and kainate.

摘要

在新生大鼠脊髓中,6,7-二氯-3-羟基-2-喹喔啉羧酸酯可拮抗由N-甲基-D-天冬氨酸(NMDA)受体和非NMDA受体介导的反应。对NMDA反应的拮抗作用是不可克服的,且是通过对变构连接的士的宁不敏感的甘氨酸位点的拮抗作用介导的。在非NMDA受体处,6,7-二氯-3-羟基-2-喹喔啉羧酸酯在低浓度时似乎作为竞争性拮抗剂起作用,而在高浓度时作为非竞争性拮抗剂起作用。与已发表的数据相反,该拮抗剂不能区分由DL-α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)和海人藻酸介导的反应。

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