Snead O C, Liu C C
Biochem Pharmacol. 1984 Aug 15;33(16):2587-90. doi: 10.1016/0006-2952(84)90629-4.
The binding of gamma-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 population of binding sites, a high-affinity site with a KD1 of 580 nM and a B max1 of 1.8 pmoles/mg protein and a low-affinity site with a KD2 of 2.3 microM and a B max2 of 11.3 pmoles/mg protein. [3H]GHB binding was not inhibited by gamma-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.
在大鼠和人类大脑突触体膜中对γ-羟基[2,3-³H]丁酸（GHB）的结合特性进行了研究。结果表明，结合具有饱和性、pH依赖性，且与蛋白质浓度呈线性关系。在大鼠和人类大脑中，[³H]GHB结合位点存在明显的区域分布，海马体中结合位点密度最高，小脑最低。竞争和饱和实验揭示了两种不同类型的结合位点，一种高亲和力位点，KD1为580 nM，B max1为1.8 pmoles/mg蛋白质；另一种低亲和力位点，KD2为2.3 μM，B max2为11.3 pmoles/mg蛋白质。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[³H]GHB结合。这些数据表明，GHB可能在大脑中作为一种神经递质或神经调节剂发挥作用，且独立于GABA。
