2,3-Benzodiazepine AMPA antagonists

István Tarnawa, E. Vízi

Research output: Contribution to journalArticle

47 Citations (Scopus)

Abstract

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
Volume13
Issue number1-2
Publication statusPublished - Oct 1998

Fingerprint

alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
Benzodiazepines
aniracetam
GYKI 53655
Allosteric Site
Central Nervous System Diseases
Glutamate Receptors
Neurodegenerative Diseases
Biological Availability
Epilepsy
Theoretical Models
Pharmacology
Research

Keywords

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

ASJC Scopus subject areas

  • Neuroscience(all)
  • Neuropsychology and Physiological Psychology

Cite this

2,3-Benzodiazepine AMPA antagonists. / Tarnawa, István; Vízi, E.

In: Restorative Neurology and Neuroscience, Vol. 13, No. 1-2, 10.1998, p. 41-57.

Research output: Contribution to journalArticle

Tarnawa, István ; Vízi, E. / 2,3-Benzodiazepine AMPA antagonists. In: Restorative Neurology and Neuroscience. 1998 ; Vol. 13, No. 1-2. pp. 41-57.
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