Measurement of DA-3 dopaminergic receptor and its application in studing pharmacologic mechanism of some drugs

Yimin Jiang; Jinchang Wu

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Measurement of DA-3 dopaminergic receptor and its application in studing pharmacologic mechanism of some drugs

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- Measurement of DA-3 dopaminergic receptor and its application in studing pharmacologic mechanism of some drugs
- Nuclear Techniques Vol. 12, Issue 1, (1989)
- 作者机构：
  
  苏州医学院附属第一医院
- 作者简介：
- 基金信息：
- DOI：
  CLC：
- Received：22 May 1987，
  
  Published：1989-01
- 稿件说明：
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Yimin Jiang, Jinchang Wu. Measurement of DA-3 dopaminergic receptor and its application in studing pharmacologic mechanism of some drugs[J]. Nuclear techniques, 1989, 12(1): 58-62.
DOI：

Yimin Jiang, Jinchang Wu. Measurement of DA-3 dopaminergic receptor and its application in studing pharmacologic mechanism of some drugs[J]. Nuclear techniques, 1989, 12(1): 58-62. DOI：

摘要

本文报道用多巴胺（DA）激动剂

H-DA为放射配体作受体饱和结合实验，直接测定了Wistar大鼠纹状体DA-3亚型受体的

和

值；竞争性抑制实验测定了去水吗啡和经典抗精神病药的

和

值。结果表明：

H-DA结合部位具有受体的基本特性，并显示出对DA激动剂有较高的亲和力，对拮抗剂亲和力则较低；去水吗啡具有DA激动剂－拮抗剂的混合作用；经典抗精神病药的药理机制与DA-3亚型受体无关。

Abstract

The total concentration (

) and equilibrium dissociation constant (

) of DA-3 dopaminergic receptor in rat striatum were investigated by

H-dopamine binding assay

and the concentration of antagonist producing a half-maximal inhibition (

) and dissociation constant of the receptor-antagonist interaction (

) of apomorphine and some classical antipsychotic drugs were measured by competitive binding of labelled and unlabelled ligands. The results showed that: 1.

H-dopamine binding sites have some essential characteristics of receptor; 2. apomorphine behaves like a mixed agonist-antagonist; 3. the action of classical antipsychotic drugs is not related to DA-3 dopaminergic receptor.

关键词

Keywords

references

M. W. Hamblim and I. Creese , Life Sei . , 30 （ 1982 ）, 1587 .

周廷冲编著，受体生化药理学，人民卫生出版社， 1985 年。

R. Winek et al . , Biochem. Biophys. Res. Commun , 91 （ 1979 ）, 200 .

Г. В. Столяров и О. Ф., Маркова , Ж. Невр. Псих. , 82 （ 1982 ）, 8 : 1217 .

C. Tamminga et al . , Science , 200 （ 1978 ）, 567 .

I. Creese et al . ， Life Sci . , 23 （ 1978 ）, 495 .

金国章，中国药理学会编，药理学进展（1983—1985），人民卫生出版社， 1985 年。

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