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June 1, 2026ACS Central ScienceOpen Access

Second-Generation of Deuterium-Substituted Glutamate Uptake Enhancers Exhibit Superior Drug-Like Properties in Preclinical Evaluation

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Authors

MAMichał AbramJagiellonian UniversityMJMarcin JakubiecJagiellonian UniversityMSMałgorzata SzafarzJagiellonian University

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Implication

Randomized trial demonstrates improved drug-like properties in preclinical models, suggesting potential for epilepsy treatment.

Key Points

  • The aim is to evaluate the drug-like properties of deuterium-substituted glutamate uptake enhancers for epilepsy treatment.
  • Applied deuterium-hydrogen exchange to develop novel analogues of EAAT2 PAMs.
  • Evaluated pharmacokinetics and antiseizure activity in mice using various seizure models.
  • Conducted electrophysiological recordings in acute mouse hippocampal slices and oocytes expressing EAAT2.
  • d6-(R)-AS-7 showed prolonged elimination half-life and enhanced plasma/brain exposure.
  • Demonstrated sustained antiseizure efficacy in multiple seizure models with significant effects.
  • Markedly enhanced glutamate uptake in both COS-7 cells and primary astrocyte cultures.

Cite This Study

Abram et al. (2026) studied this question.

synapsesocial.com/papers/6a1d216202fbce9130637655https://doi.org/10.1021/acscentsci.6c00080
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