A novel fluorescent GSH-adduct binds to the NMDA receptor.
A novel fluorescent GSH-adduct binds to the NMDA receptor.
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一种新型荧光 GSH 加合物与 NMDA 受体结合。
DOI：
10.1016/s0165-0270(99)00092-8
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发表时间：
1999
影响因子：
3
通讯作者：
Langmuir,ME
中科院分区：
文献类型：
--
作者：
Shaw,CA;Pasqualotto,BA;Curry,K;Kim,SU;LeCompte,KA;Langmuir,ME
在尝试开发各种荧光探针来标记谷胱甘肽 (GSH) 受体时，我们偶然合成了一种结合并拮抗 NMDA 受体的探针。探针 1 是一种 GSH 加合物，在大鼠突触膜中以比 NMDA 或半胱氨酸更高的亲和力取代竞争性 NMDA 拮抗剂 [3H]-CGP 39653。在记录大鼠皮质“楔形”制剂的实验时，探针 1 可逆地阻断 NMDA 和半胱氨酸诱导的去极化。在混合星形胶质细胞-神经元组织培养制剂中，探针 1 标记细胞体和突起的部分。目前的数据表明探针 1 与 NMDA 受体结合并拮抗通道功能。
In an attempt to develop various fluorescent probes to label glutathione (GSH) receptors, we have serendipitously synthesized a probe that binds to and antagonizes the NMDA receptor. Probe 1, a GSH adduct, displaces the competitive NMDA antagonist [3H]-CGP 39653 with a higher affinity than NMDA or cysteine in rat synaptic membranes. In recording experiments from a rat cortical ‘wedge’ preparation, Probe 1 reversibly blocks both NMDA- and cysteine-induced depolarization. In mixed astrocyte-neuron tissue culture preparations, Probe 1 labels parts of both cell bodies as well as processes. The present data suggest that Probe 1 binds to the NMDA receptor and antagonizes channel function.