复杂的药理性质重组alpha-amino-3-hydroxy-5-methyl-4-isoxazole丙酸受体亚型。
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斯坦E,考克斯JA Seeburg PH值,Verdoorn助教
复杂的药理性质重组alpha-amino-3-hydroxy-5-methyl-4-isoxazole丙酸受体亚型。
摩尔杂志。1992年11月,42 (5):864 - 71。
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1279377 (在PubMed]
- 文摘
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两个谷氨酸受体亚型的药理性质,GluR-A / B和GluR-B / D,检查在RNA-injected非洲爪蟾蜍卵母细胞使用二电极电压钳位。量效关系表明L-glutamate的效能,kainate,丙酸和alpha-amino-3-hydroxy-5-methyl-4-isoxazole (AMPA)这两种受体亚型之间略有不同,但兴奋剂的等级次序效力没有。GluR-A / B的EC50值3.31 microM AMPA受体,6.16 microM谷氨酸,和57.5 microM kainate,而GluR-B / D受体的EC50值5.01 microM microM 32.3和64.6 microM AMPA, L-glutamate和kainate分别。6-cyano-7-nitroquinoxaline-2的效能,3-dione (CNQX)和2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo (f)喹喔啉(NBQX)被席尔德量化分析。NBQX的力量阻止电流由GluR-A / B受体改变取决于受体激动剂用于激活受体(pA2值如下:kainate块,7.23 + / - 0.01;L-glutamate, 6.78 + / - 0.02;AMPA, 6.95 + / - 0.02)。在细胞受体激动剂之间的差异不太明显表达GluR-B / D受体(回目价值观:kainate, 7.28 + / - 0.01;L-glutamate, 7.30 + / - 0.02;AMPA, 7.35 + / - 0.01)。 In each case, the slope of the Schild regression was not different from unity, consistent with competitive antagonism of these receptors by NBQX. CNQX also blocked GluR-A/B and GluR-B/D receptors competitively but was less potent than NBQX and did not differentiate between agonists or subunit combination. These data suggest that L-glutamate, kainate, and AMPA bind to different receptor substructures on recombinant AMPA receptors and that NBQX but not CNQX binds to these sites with different affinities. Moreover, because the properties of these binding sites vary between GluR-A/B and GluR-B/D receptors, our findings provide a basis for mutational analysis aimed at identifying receptor domains involved in agonist and antagonist binding.