2,3-Benzodiazepine AMPA antagonists

István Tarnawa, E. Sylvester Vizi

Research output: Contribution to journalReview article

47 Citations (Scopus)


The 2,3-benzodiazepine GYKI 52466 (1-(4-aminophenyl)-4-methyl-7,8- methylenedioxy-5H-2,3-benzodiazepine) and its analogues represent a family of selective AMPA antagonists. They modulate AMPA channel functions through an allosteric site on the receptor, which is probably different from the ones involved in the actions of cyclothiazide and aniracetam. These compounds are frequently used as research tools to elucidate glutamate receptor-mediated functions. The most effective members of the family inhibit AMPA-induced currents in the submicromolar range. In addition, they are active at low systemic doses in various in vivo experimental models and also possess a good oral bioavailability. In vitro and in vivo pharmacological results with 2,3- benzodiazepine AMPA antagonists indicate their potential therapeutical value in treating a great variety of central nervous system diseases, of which epilepsy and neurodegenerative disorders are regarded as the most important.

Original languageEnglish
Pages (from-to)41-57
Number of pages17
JournalRestorative neurology and neuroscience
Issue number1-2
Publication statusPublished - Oct 1 1998


  • Epilepsy
  • GYKI 52466
  • Neurodegenerative disorders
  • Neuroprotection
  • Pain disorders
  • Spasticity

ASJC Scopus subject areas

  • Neurology
  • Developmental Neuroscience
  • Clinical Neurology

Fingerprint Dive into the research topics of '2,3-Benzodiazepine AMPA antagonists'. Together they form a unique fingerprint.

  • Cite this