DIFFERENTIAL BENZODIAZEPINE PHARMACOLOGY OF MAMMALIAN RECOMBINANT GABA-A RECEPTORS

被引：84

作者：

VONBLANKENFELD, G

YMER, S

PRITCHETT, DB

SONTHEIMER, H

EWERT, M

SEEBURG, PH

KETTENMANN, H

机构：

[1] UNIV HEIDELBERG,DEPT NEUROBIOL,NEUENHEIMER FELD 345,W-6900 HEIDELBERG,GERMANY

[2] UNIV HEIDELBERG,ZMBH,W-6900 HEIDELBERG,GERMANY

来源：

NEUROSCIENCE LETTERS | 1990年 / 115卷 / 2-3期

关键词：

Benzodiazepine; cDNA; Cell transfection; GABA[!sub]A[!/sub] receptor; Inverse agonist; Patch clamp;

D O I：

10.1016/0304-3940(90)90467-N

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

We compared γ-aminobutyric acid (GABA)-activated currents and their modulation by benzodiazepines in cultured human cells transfected with complementary desoxyribonucleic acid (cDNA) encoding different GABAA receptor subunits. Flunitrazepam, a benzodiazepine agonist which potentiates GABA responses in both neurons and astrocytes was only effective in receptors containing the γ2 subunit (α1β1γ2 and α5β1γ2). The β-carboline methyl-4-ethyl-6,7-dimethoxy-β-carboline-3-carboxylate (DMCM) decreased GABA-activated currents in receptors composed of α1β1γ1 and α1β1γ2 subunits but increased GABA-activated currents in receptors containing the α5 subunit (α5β1γ1 and α5β1γ2). These results strongly suggest that flunitrazepam and DMCM do not act on isosteric sites and that differences in the responsiveness of GABAA receptors to these compounds are based on different subunit compositions of GABAA receptors. © 1990.

引用

页码：269 / 273

页数：5

共 14 条

[1] EFFECT OF BENZODIAZEPINES AND PENTOBARBITAL ON THE GABA-INDUCED DEPOLARIZATION IN CULTURED ASTROCYTES [J].