Guarneri P, Guarneri R, Mocciaro C, Piccoli F
Neurochem Res. 1983 Dec;8(12):1537-45. doi: 10.1007/BF00964155.
The effect of uridine, a postulated anticonvulsant agent, on GABA receptors has been investigated. Uridine inhibits [3H]GABA binding to rat cerebellar buffer-washed membranes. Pretreatment of the membranes with Triton X-100 increases the effect of uridine on GABA-binding. The Scatchard analysis reveals that both high and low affinities of GABA for its receptors are affected by 1 mM uridine, while the apparent number of binding sites remains unchanged. The ability of uridine to interact competitively with GABA binding sites, also examined by the Lineweaver-Burk analysis, suggests a possible mechanism of action of this anticonvulsant agent, so including it among those compounds characterized by a GABAergic agonist activity.
人们已经研究了假定的抗惊厥剂尿苷对γ-氨基丁酸（GABA）受体的作用。尿苷可抑制[³H]GABA与大鼠小脑缓冲液洗涤膜的结合。用曲拉通X-100预处理膜可增强尿苷对GABA结合的作用。斯卡查德分析表明，1 mM尿苷会影响GABA与其受体的高亲和力和低亲和力，而结合位点的表观数量保持不变。通过线性回归分析也检测了尿苷与GABA结合位点竞争性相互作用的能力，这提示了这种抗惊厥剂可能的作用机制，因此将其纳入具有GABA能激动剂活性的化合物之列。
