RELATIVE AFFINITIES OF DOPAMINERGIC DRUGS AT DOPAMINE D-2 AND D-3 RECEPTORS

被引：34

作者：

LEVANT, B ^{[1
]}

GRIGORIADIS, DE ^{[1
]}

DESOUZA, EB ^{[1
]}

机构：

[1] DUPONT MERCK PHARMACEUT CO,WILMINGTON,DE 19880

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1995年 / 278卷 / 03期

关键词：

DOPAMINE D-2 RECEPTOR; DOPAMINE D-3 RECEPTOR; I-125] IODOSULPIRIDE; RECEPTOR AUTORADIOGRAPHY; STRIATUM; CEREBELLUM; (RAT);

D O I：

10.1016/0014-2999(95)00160-M

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Quantitative autoradiography was used to evaluate the pharmacological profile of dopamine D-2-like receptors labeled by [I-125]iodosulpiride. Caudate/putamen, a brain region associated primarily with dopamine D-2 receptor mRNA, was used as a prototypical D-2 tissue; cerebellar lobule X (D-3 mRNA associated), as a D-3 tissue. 7-OH-DPAT ((+/-)-2-dipropylamino-7-hydroxy-1,2,3,4-tetrahydronaphthalene) exhibited selectivity for cerebellar receptors (24-fold), followed by quinpirole (6-fold). Haloperidol and domperidone were 4- and 18-fold more potent at striatal receptors, respectively. These data are in close agreement with that derived from dopamine D-2 and D-3 receptor-expressing cell lines.

引用

页码：243 / 247

页数：5

共 16 条

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