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<p>The anticonvulsant activity of the new NMDA-receptor ligand 6,7-dihydro-5<i>H</i>-pyrrolo[1,2-<i>a</i>]imidazole-2,3-dicarboxylic acid and one of its possible prodrugs, the <i>bis</i>-methylamide, was explored in the models of NMDA-induced and pentylenetetrazole (corazole)-induced seizures. The effects of these compounds on ion currents in isolated midbrain neurons of <i>Danio rerio</i> were investigated using a whole-cell patch-clamp method. Experiments on isolated neurons showed that the acid acted as an NMDA receptor antagonist. 6,7-Dihydro-5<i>H</i>-pyrrolo[1,2-<i>a</i>]imidazole-2,3-dicarboxylic acid and its <i>bis</i>-methylamide exhibited pronounced anticonvulsant activity against NMDA-induced seizures and were inactive in the pentylenetetrazole seizure model in mice. The effective dose of the <i>bis</i>-methylamide in the model of NMDA-induced seizures was 4.5 times lower than that of the acid.</p>

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Anticonvulsant Activity of 6,7-Dihydro-5H-Pyrrolo[1,2-a]Imidazole-2,3-Dicarboxylic Acid and Its bis-Methylamide

  • 期刊论文

  • 发表日期：

    2025年1月1日

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  • M. A. Brusina,
  • A. M. Potapkin,
  • L. G. Kubarskaya,
  • E. V. Litasova,
  • L. B. Piotrovsky

摘要

The anticonvulsant activity of the new NMDA-receptor ligand 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole-2,3-dicarboxylic acid and one of its possible prodrugs, the bis-methylamide, was explored in the models of NMDA-induced and pentylenetetrazole (corazole)-induced seizures. The effects of these compounds on ion currents in isolated midbrain neurons of Danio rerio were investigated using a whole-cell patch-clamp method. Experiments on isolated neurons showed that the acid acted as an NMDA receptor antagonist. 6,7-Dihydro-5H-pyrrolo[1,2-a]imidazole-2,3-dicarboxylic acid and its bis-methylamide exhibited pronounced anticonvulsant activity against NMDA-induced seizures and were inactive in the pentylenetetrazole seizure model in mice. The effective dose of the bis-methylamide in the model of NMDA-induced seizures was 4.5 times lower than that of the acid.