Sagratella S, Frank C, de Carolis A S
Laboratoire di Farmacologia, Instituto Superiore di Sanità, Roma, Italy.
Arch Int Pharmacodyn Ther. 1989 May-Jun;299:28-34.
The effects of the broad spectrum antagonist of the excitatory amino acid neurotransmission, the cis-2,3 piperidine-dicarboxylic acid (cis-2,3 PDA) were investigated on the epileptiform activity induced in vitro by different treatments on rat hippocampal slices. The drug reduced the bursting duration by 45% and the occurrence of the additional population spikes by 50% compared with controls using 1 microM kainic acid to induce epileptiform bursting. At the same concentrations (50-100 microM) cis-2,3 PDA did not significantly affect the magnesium free-induced epileptiform activity. At higher concentrations (200-400 microM), the drug was able to reduce by 25% the bursting duration and the occurrence of the additional population spikes using 1 mM penicillin to induce epileptiform bursting. Our data indicate that the broad spectrum antagonist of the excitatory amino acid transmission, cis-2,3 PDA, presents a low antiepileptic activity that could be related to an influence on "non N-methyl-d-aspartate" (NMDA) receptors.
研究了兴奋性氨基酸神经传递的广谱拮抗剂顺式 -2,3 - 哌啶二羧酸（cis -2,3 PDA）对不同处理诱导的大鼠海马脑片体外癫痫样活动的影响。与使用1微摩尔红藻氨酸诱导癫痫样爆发的对照组相比，该药物使爆发持续时间减少了45%，额外群体峰电位的发生率降低了50%。在相同浓度（50 - 100微摩尔）下，cis -2,3 PDA对无镁诱导的癫痫样活动没有显著影响。在较高浓度（200 - 400微摩尔）下，使用1毫摩尔青霉素诱导癫痫样爆发时，该药物能够使爆发持续时间和额外群体峰电位的发生率降低25%。我们的数据表明，兴奋性氨基酸传递的广谱拮抗剂cis -2,3 PDA具有较低的抗癫痫活性，这可能与对“非N - 甲基 - D - 天冬氨酸”（NMDA）受体的影响有关。
