Department of Animal Physiology, Institute of Biology and Biochemistry, Maria Curie-Skłodowska University, Akademicka 19, PL 20-033 Lublin, Poland.
Pharmacol Rep. 2011;63(5):1231-4. doi: 10.1016/s1734-1140(11)70643-0.
The anticonvulsant effects of D-cycloserine, which is a partial agonist of the glycine/N-methyl-D-aspartate (NMDA) receptor, and L-701,324, which is a selective and potent antagonist that acts at the glycine site, were studied in electroshock-induced seizures in mice. Glycine, which is a natural full agonist that acts at the glycine site, enhanced the seizure threshold-increasing effect of D-cycloserine. L-701,324 produced a marked increase in the seizure threshold, which was significantly reversed by the administration of glycine. These results suggest that indirect glycine/NMDA antagonistic mechanisms may be responsible for the anticonvulsant action of D-cycloserine.
D-环丝氨酸是甘氨酸/N-甲基-D-天冬氨酸（NMDA）受体的部分激动剂，L-701,324 是一种选择性和有效的甘氨酸位点拮抗剂，它们在电休克诱导的小鼠癫痫发作中的抗惊厥作用进行了研究。甘氨酸是一种天然的完全激动剂，作用于甘氨酸位点，增强了 D-环丝氨酸的惊厥阈升高作用。L-701,324 显著增加了惊厥阈，甘氨酸的给药明显逆转了这一作用。这些结果表明，间接甘氨酸/NMDA 拮抗机制可能是 D-环丝氨酸抗惊厥作用的原因。
