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<p>It has been previously established that Sigma1R chaperone agonists enhance, while antagonists weaken the pharmacological effects of allosteric modulators of the GABA<sub>A</sub> receptor. The present study evaluated the anticonvulsant effect of the Sigma1R ligand fabomotizole at doses of 5, 10, and 20 mg/kg i.p. and a combination of the same doses of fabomotizole with diazepam administered at a dose of 1 mg/kg i.p., recording the doses of pentylenetetrazole that caused clonic twitching, generalized clonic seizures, and generalized tonic seizures when administered intravenously to ICR mice. It was found that fabomotizole at doses of 10 and 20 mg/kg exhibited anticonvulsant properties. The anticonvulsant effect of diazepam was enhanced in combination with it. The anticonvulsant effect of fabomotizole at a dose of 20 mg/kg was shown to be attenuated by prior administration of the Sigma1R chaperone antagonist BD-1047 at a dose of 20 mg/kg.</p>

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Anticonvulsant Properties of Fabomotizole When Administered Separately and in Conjunction with Diazepam

  • 期刊论文

  • 发表日期：

    2025年10月1日

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  • S. V. Shangin,
  • Yu. V. Vakhitova,
  • S. A. Litvinova,
  • M. V. Voronin,
  • S. B. Seredenin

摘要

It has been previously established that Sigma1R chaperone agonists enhance, while antagonists weaken the pharmacological effects of allosteric modulators of the GABAA receptor. The present study evaluated the anticonvulsant effect of the Sigma1R ligand fabomotizole at doses of 5, 10, and 20 mg/kg i.p. and a combination of the same doses of fabomotizole with diazepam administered at a dose of 1 mg/kg i.p., recording the doses of pentylenetetrazole that caused clonic twitching, generalized clonic seizures, and generalized tonic seizures when administered intravenously to ICR mice. It was found that fabomotizole at doses of 10 and 20 mg/kg exhibited anticonvulsant properties. The anticonvulsant effect of diazepam was enhanced in combination with it. The anticonvulsant effect of fabomotizole at a dose of 20 mg/kg was shown to be attenuated by prior administration of the Sigma1R chaperone antagonist BD-1047 at a dose of 20 mg/kg.