Gamma-hydroxybutyric acid binding sites in rat and human brain synaptosomal membranes.
Gamma-hydroxybutyric acid binding sites in rat and human brain synaptosomal membranes.
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大鼠和人脑突触体膜中的γ-羟基丁酸结合位点。
DOI：
10.1016/0006-2952(84)90629-4
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发表时间：
1984
影响因子：
5.8
通讯作者：
Liu,CC
中科院分区：
文献类型：
--
作者：
Snead3rd,OC;Liu,CC
研究了γ-羟基[2,3- 3h]丁酸（GHB）在大鼠和人脑突触体膜上的结合。结合是饱和的，pH依赖性的，并与蛋白质浓度成线性关系。[3H]GHB结合位点在大鼠和人脑中具有明显的区域分布，海马的结合位点密度最高，小脑的结合位点密度最低。竞争和饱和实验显示了两个不同的结合位点群体，一个高亲和力位点与akd1为580 nM， abmax1为1.8 pmol /mg蛋白，一个低亲和力位点与akd2为2.3 μM， abmax2为11.3 pmol /mg蛋白。[3H] γ-氨基丁酸（GABA）、GABA受体激动剂、阿片拮抗剂或抗惊厥药物均不抑制GHB的结合。这些数据表明，GHB可能作为一种独立于GABA的神经递质或神经调节剂在大脑中发挥作用。
The binding of γ-hydroxy[2,3-3H]butyric acid (GHB) was characterized in rat and human brain synaptosomal membranes. Binding was shown to be saturable, pH dependent, and linear with protein concentration. There was a distinct regional distribution of binding sites in both rat and human brain, with the hippocampus being the richest and the cerebellum the poorest, in density of [3H]GHB binding sites. Competition and saturation experiments revealed two different populations of binding sites, a high-affinity site with aKD1of 580 nM and aBmax1of 1.8 pmoles/mg protein and a low-affinity site with aKD2of 2.3 μM and aBmax2of 11.3 pmoles/mg protein. [3H]GHB binding was not inhibited by γ-aminobutyric acid (GABA), GABA receptor agonists, opiate antagonists or anticonvulsant drugs. These data suggest that GHB may play a role as a neurotransmitter or neuromodulator in brain independent of GABA.