芳基胺类蜘蛛毒素可拮抗大鼠海马切片中NMDA受体介导的突触传递。

Arylamine spider toxins antagonize NMDA receptor-mediated synaptic transmission in rat hippocampal slices.

作者信息

Mueller A L, Albensi B C, Ganong A H, Reynolds L S, Jackson H

机构信息

Natural Product Sciences, Inc., Salt Lake City, Utah 84108.

出版信息

Synapse. 1991 Dec;9(4):244-50. doi: 10.1002/syn.890090403.

DOI:10.1002/syn.890090403

PMID:1662833

Abstract

The effects of arylamine spider toxins on synaptic transmission in rat hippocampal slices were investigated. Two different responses were monitored: the AMPA receptor-mediated population spike recorded in control buffer (selectively antagonized by DNQX) and the NMDA receptor-mediated EPSP recorded in nominally magnesium-free buffer containing 20 microM DNQX (selectively antagonized by AP5, AP7, and dizocilpine (MK-801)). The synthetic arylamine spider toxins JSTX-3, argiotoxin-636, and argiotoxin-659 were 26 to 73 times more potent at antagonizing the NMDA receptor-mediated EPSP (IC50 values ranging from 12 to 24 microM) than the AMPA receptor-mediated population spike (IC50 values ranging from 612 to 878 microM). These results indicate that arylamine spider toxins are selective antagonists of NMDA receptors in the mammalian CNS.

摘要

研究了芳胺类蜘蛛毒素对大鼠海马脑片突触传递的影响。监测了两种不同的反应：在对照缓冲液中记录的AMPA受体介导的群体峰电位（被DNQX选择性拮抗）和在含有20μM DNQX的无镁缓冲液中记录的NMDA受体介导的兴奋性突触后电位（被AP5、AP7和地卓西平（MK-801）选择性拮抗）。合成的芳胺类蜘蛛毒素JSTX-3、蛛毒素-636和蛛毒素-659拮抗NMDA受体介导的兴奋性突触后电位（IC50值为12至24μM）的效力比AMPA受体介导的群体峰电位（IC50值为612至878μM）高26至73倍。这些结果表明芳胺类蜘蛛毒素是哺乳动物中枢神经系统中NMDA受体的选择性拮抗剂。