Neurochemical Research

, Volume 22, Issue 4, pp 419–425

Overview—Flavonoids: A New Family of Benzodiazepine Receptor Ligands

Authors

  • Jorge H. Medina
    • Instituto de Biologia Celular y Neurociencias, Facultad de MedicinaUBA
  • Haydee Viola
    • Instituto de Biologia Celular y Neurociencias, Facultad de MedicinaUBA
  • Claudia Wolfman
    • Instituto de Biologia Celular y Neurociencias, Facultad de MedicinaUBA
  • Mariel Marder
    • Instituto de Quimica y Fisicoquimica Biologicas, Facultad de Farmacia y BioquimicaUBA
  • Cristina Wasowski
    • Instituto de Quimica y Fisicoquimica Biologicas, Facultad de Farmacia y BioquimicaUBA
  • Daniel Calvo
    • Instituto de Biologia Celular y Neurociencias, Facultad de MedicinaUBA
  • Alejandro C. Paladini
    • Instituto de Quimica y Fisicoquimica Biologicas, Facultad de Farmacia y BioquimicaUBA
Article

DOI: 10.1023/A:1027303609517

Cite this article as:
Medina, J.H., Viola, H., Wolfman, C. et al. Neurochem Res (1997) 22: 419. doi:10.1023/A:1027303609517

Abstract

Benzodiazepines (BDZs) are the most widely prescribed class of psychoactive drugs in current therapeutic use, despite the important unwanted side-effects that they produce such as sedation, myorelaxation, ataxia, amnesia, ethanol and barbiturate potentiation and tolerance. Searching for safer BDZ-receptor (BDZ-R) ligands we have recently demonstrated the existence of a new family of ligands which have a flavonoid structure. First isolated from plants used as tranquilizers in folkloric medicine, some natural flavonoids have shown to possess a selective and relatively mild affinity for BDZ-Rs and a pharmacological profile compatible with a partial agonistic action. In a logical extension of this discovery various synthetic derivatives of those compounds, such as 6,3′-dinitroflavone were found to have a very potent anxiolytic effect not associated with myorelaxant, amnestic or sedative actions. This dinitro compound, in particular, exhibits a high affinity for the BDZ-Rs (Ki = 12–30 nM). Due to their selective pharmacological profile and low intrinsic efficacy at the BDZ-Rs, flavonoid derivatives, such as those described, could represent an improved therapeutic tool in the treatment of anxiety. In addition, several flavone derivatives may provide important leads for the development of potent and selective BDZ-Rs ligands.

Flavonoidsbenzodiazepine receptorsanxiolysispartial agonist
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Copyright information

© Plenum Publishing Corporation 1997