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犬尿喹啉酸和FG9041在兴奋性氨基酸受体上同时具有竞争性和非竞争性拮抗作用。

Kynurenate and FG9041 have both competitive and non-competitive antagonist actions at excitatory amino acid receptors.

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. 1988 Jul 7;151(2):313-5. doi: 10.1016/0014-2999(88)90814-x.

Abstract

The antagonist profile of kynurenate and FG9041 have been characterised in a modified preparation of the baby rat hemisected spinal cord. Both kynurenate and FG9041 were competitive antagonists of responses to kainate and AMPA, although neither antagonist was selective for kainate versus AMPA. In contrast, both antagonists produced an apparent unsurmountable antagonism of responses to NMDA, indicating a different mode of action at the NMDA receptor.

摘要

犬尿喹啉酸和FG9041的拮抗剂特性已在改良的新生大鼠脊髓半横切标本中得到表征。犬尿喹啉酸和FG9041都是对 kainate 和AMPA反应的竞争性拮抗剂,尽管这两种拮抗剂对kainate和AMPA都没有选择性。相比之下,这两种拮抗剂对NMDA反应均产生明显的不可克服的拮抗作用,表明它们在NMDA受体上的作用模式不同。

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