Collins J F, Dixon A J, Badman G, De Sarro G, Chapman A G, Hart G P, Meldrum B S
Neurosci Lett. 1984 Oct 26;51(3):371-6. doi: 10.1016/0304-3940(84)90405-1.
beta-Kainic acid, and the glycine and amino-methylphosphonate derivatives of alpha- and beta-kainic acid, have been injected intracerebroventricularly in DBA/2 mice, that show sound-induced seizure responses. An anticonvulsant effect is observed with marked protection against the tonic and clonic phases of the seizure response. ED50 values against clonus are (in mumol): beta-kainic acid, 0.09; beta-kainylglycine, 0.11; alpha-kainylglycine, 0.28; alpha-kainylaminomethylphosphonate, 0.31; beta-kainylaminomethylphosphonate, greater than 1.5. In addition a direct convulsant effect occurs after the alpha-kainyl derivatives.
已将β-海人酸以及α-和β-海人酸的甘氨酸和氨基甲基膦酸酯衍生物脑室内注射到表现出声音诱发惊厥反应的DBA/2小鼠体内。观察到抗惊厥作用，对惊厥反应的强直期和阵挛期有明显保护作用。抗阵挛的半数有效剂量（以微摩尔计）为：β-海人酸，0.09；β-海人酰甘氨酸，0.11；α-海人酰甘氨酸，0.28；α-海人酰氨基甲基膦酸，0.31；β-海人酰氨基甲基膦酸，大于1.5。此外，α-海人酰衍生物注射后会产生直接惊厥作用。
