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乙醇在培养的小脑颗粒细胞中,以低微摩尔浓度范围内对ifenprodil具有亲和力,特异性抑制N-甲基-D-天冬氨酸(NMDA)受体。

Ethanol specifically inhibits NMDA receptors with affinity for ifenprodil in the low micromolar range in cultured cerebellar granule cells.

作者信息

Engblom A C, Courtney M J, Kukkonen J P, Akerman K E

机构信息

Department of Biochemistry and Pharmacy, Abo Akademi University, Finland.

出版信息

J Neurochem. 1997 Nov;69(5):2162-8. doi: 10.1046/j.1471-4159.1997.69052162.x.

Abstract

The effect of ethanol on the intracellular Ca2+ concentration response to NMDA in rat cerebellar granule cells grown in low or high KCl concentrations has been studied using image analysis. The cells grown in low KCl displayed high sensitivity for glycine. The subtype-selective antagonist ifenprodil inhibited the response with high (in the low micromolar range) and low (in the high micromolar range) potency. Ethanol affected the high-potency component in these cultures. In cells grown in high KCl the glycine sensitivity was lower, and a low potency for ifenprodil (high micromolar) dominated. These cells were not significantly sensitive to ethanol. The results indicate that the component displaying potency for ifenprodil in the low micromolar range with properties of the NR2B subunit is the target for ethanol action on the NMDA receptor.

摘要

利用图像分析技术,研究了乙醇对在低或高氯化钾浓度下培养的大鼠小脑颗粒细胞中细胞内钙离子浓度对N-甲基-D-天冬氨酸(NMDA)反应的影响。在低氯化钾浓度下培养的细胞对甘氨酸表现出高敏感性。亚型选择性拮抗剂艾芬地尔以高(低微摩尔范围)和低(高微摩尔范围)效力抑制反应。乙醇影响这些培养物中的高效力成分。在高氯化钾浓度下培养的细胞中,甘氨酸敏感性较低,艾芬地尔的低效力(高微摩尔)占主导。这些细胞对乙醇不敏感。结果表明,在低微摩尔范围内对艾芬地尔具有效力且具有NR2B亚基特性的成分是乙醇作用于NMDA受体的靶点。

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