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GYKI-32 887 对多巴胺(D2)和血清素(5-HT1 和 5-HT2)受体的作用。

The effect of GYKI-32 887 on dopamine (D2) and serotonin (5-HT1 and 5-HT2) receptors.

作者信息

Berzétei I P, Bagdy E, Hardy M, Borsy J

出版信息

Pol J Pharmacol Pharm. 1985 May-Jun;37(3):237-42.

PMID:4070077
Abstract

Investigations were carried out with a dopamine agonist compound GYKI-32 887 to compare its binding capacity towards D2, 5-HT1 and 5-HT2 receptors. Synaptosomal membranes were prepared from corpus striatum, hippocampus and frontal cortex of rats. The tritiated ligands used were: 3H-spiperone for D2 and 5-HT2 receptors and 3H-5-HT for 5-HT1 receptors. Comparing the results obtained, IC50 and Ki values, one can conclude that GYKI-32 887 has higher affinity towards D2 receptors than serotonin ones and shows better selectivity than bromocriptine, the reference substance.

摘要

使用多巴胺激动剂化合物GYKI-32 887进行研究,以比较其对D2、5-HT1和5-HT2受体的结合能力。从大鼠的纹状体、海马体和额叶皮质制备突触体膜。使用的氚标记配体为:用于D2和5-HT2受体的3H-螺哌隆以及用于5-HT1受体的3H-5-羟色胺。比较所得结果(IC50和Ki值)可以得出结论,GYKI-32 887对D2受体的亲和力高于对5-羟色胺受体的亲和力,并且比参比物质溴隐亭表现出更好的选择性。

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