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石杉碱甲对大鼠大脑皮层NMDA受体的调节作用

Modulation of NMDA receptor by huperzine A in rat cerebral cortex.

作者信息

Wang X D, Zhang J M, Yang H H, Hu G Y

机构信息

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.

出版信息

Zhongguo Yao Li Xue Bao. 1999 Jan;20(1):31-5.

PMID:10437121
Abstract

AIM

To investigate the effects of huperzine A (Hup A) on NMDA receptors in rat cerebral cortex.

METHODS

  1. The effect of hup A on NMDA-induced current was studied in acutely dissociated rat hippocampal pyramidal neurons using whole-cell recording. 2) The effect of Hup A on NMDA receptor binding was assessed using [3H] dizocilpine (Diz) binding assay in synaptic membrane preparation of rat cerebral cortex.

RESULTS

  1. Hup A reversibly inhibited NMDA-induced current in a concentration-dependent manner with IC50 of 45.4 mumol.L-1. 2) Hup A inhibited the specific binding of [3H]MK-801 to extensively washed synaptic membrane of rat cerebral cortex in a concentration-dependent manner with IC50 of 0.5 (0.1-1.9) mumol.L-1 (n = 4). 3) L-Glutamate 10 mumol.L-1 markedly increased [3H] MK-801 binding. In the presence of L-glutamate, Hup A 0.001-0.1 mumol.L-1 caused a further increase of the binding, whereas Hup A 1-300 mumol.L-1 inhibited the binding in a concentration-dependent manner with IC50 of 12.3 (5.8-26.3) mumol.L-1 (n = 5).

CONCLUSION

Hup A acted as an antagonist of NMDA receptor in cerebral cortex in addition to its inhibitory effect on acetylcholinesterase.

摘要

目的

研究石杉碱甲（Hup A）对大鼠大脑皮质N-甲基-D-天冬氨酸（NMDA）受体的作用。

方法

1）采用全细胞膜片钳记录技术，研究Hup A对急性分离的大鼠海马锥体神经元中NMDA诱导电流的影响。2）采用[3H]二氮卓西平（Diz）结合试验，在大鼠大脑皮质突触膜制备物中评估Hup A对NMDA受体结合的影响。

结果

1）Hup A以浓度依赖性方式可逆性抑制NMDA诱导电流，半数抑制浓度（IC50）为45.4μmol·L-1。2）Hup A以浓度依赖性方式抑制[3H]MK-801与大鼠大脑皮质广泛洗涤的突触膜的特异性结合，IC50为0.5（0.1-1.9）μmol·L-1（n = 4）。3）10μmol·L-1的L-谷氨酸显著增加[3H]MK-801结合。在L-谷氨酸存在下，0.001-0.1μmol·L-1的Hup A导致结合进一步增加，而1-300μmol·L-1的Hup A以浓度依赖性方式抑制结合，IC50为12.3（5.8-26.3）μmol·L-1（n = 5）。

结论

Hup A除对乙酰胆碱酯酶有抑制作用外，还可作为大脑皮质NMDA受体的拮抗剂。

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