Opposing effects of different steroid sulfates on GABAA receptor-mediated chloride uptake

被引：15

作者：

El-Etr, M ^{[1
]}

Akwa, Y ^{[1
]}

Robel, P ^{[1
]}

Baulieu, EE ^{[1
]}

机构：

[1] INSERM U33, Lab Hormones, F-94276 Le Kremlin Bicetre, France

来源：

BRAIN RESEARCH | 1998年 / 790卷 / 1-2期

关键词：

GABA(A) receptor; sulfated steroids; 3 alpha-hydroxy-5 alpha-pregnan-20-one sulfate; pregnenolone sulfate; chloride ionophore; neurosteroid;

D O I：

10.1016/S0006-8993(98)00145-0

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Steroids with the 3 alpha-hydroxy-5 alpha- or 5 beta-reduced configurations of the A ring interact with the gamma-aminobutyric acid (GABA) type A receptor chloride channel complex and potentiate the stimulation of Cl- uptake by GABA agonists. Conversely, the sulfate esters of 3 beta-hydroxy-5-ene neurosteroids pregnenolone and dehydroepiandrosterone behave as inhibitory modulators. In the present work, steroid sulfates were tested for their ability to modulate muscimol-induced chloride ion uptake into cortical synaptoneurosomes. 3 alpha-Hydroxy-5 alpha-pregnan-20-one sulfate and several other 3 alpha-hydroxy-steroid sulfates potentiated, whereas 3 beta-hydroxy-steroid sulfates inhibited muscimol effect. It is concluded that GABA-agonistic or antagonistic properties of steroid sulfates depend on the alpha or beta orientation of the sulfate moiety linked to the A ring. (C) 1998 Elsevier Science B.V.

引用

页码：334 / 338

页数：5

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