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舒必利对大鼠纹状体突触[3H] - 螺哌隆结合抑制活性的研究进展

Development of inhibitory activity of sulpiride for synaptic [3H]-spiperone binding in the rat striatum.

作者信息

Oki K, Nomura Y

出版信息

Dev Neurosci. 1982;5(4):379-84. doi: 10.1159/000112697.

Abstract

To establish the functional development of striatal dopamine2 (DA2) receptors, the effects of NA+ and GTP on the potency of sulpiride in competing for specific [3H]-spiperone binding were investigated in the striatum of developing rats. The IC50 value of sulpiride for specific [3H]-spiperone binding was 31-fold decreased by 100 mM Na+ compared to that in 70-day-old control animals but not by 50 microM GTP. In the presence of Na+, the IC50 of sulpiride was low in fetuses at 18 days of gestation and high at 360 days of postnatal life. It is suggested that the Na+-dependent binding of sulpiride to DA2 receptors probably reaches functional maturity in fetuses at 18 days of gestation and that the Na+ dependence of the effect decreases during aging.

摘要

为了确定纹状体多巴胺2(DA2)受体的功能发育情况,研究了钠离子(Na+)和鸟苷三磷酸(GTP)对舒必利竞争特异性[3H] - 螺哌隆结合能力的影响,实验对象为发育中的大鼠纹状体。与70日龄的对照动物相比,100 mM Na+使舒必利特异性结合[3H] - 螺哌隆的半数抑制浓度(IC50)值降低了31倍,但50 microM GTP未产生此效果。在有Na+存在的情况下,舒必利的IC50在妊娠18天的胎儿中较低,而在出生后360天较高。这表明舒必利与DA2受体的Na+依赖性结合可能在妊娠18天的胎儿中达到功能成熟,并且随着年龄增长,这种效应的Na+依赖性降低。

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