Article

Neurochemical Research

, Volume 22, Issue 4, pp 419-425

Overview—Flavonoids: A New Family of Benzodiazepine Receptor Ligands

  • Jorge H. MedinaAffiliated withInstituto de Biologia Celular y Neurociencias, Facultad de Medicina, UBA
  • , Haydee ViolaAffiliated withInstituto de Biologia Celular y Neurociencias, Facultad de Medicina, UBA
  • , Claudia WolfmanAffiliated withInstituto de Biologia Celular y Neurociencias, Facultad de Medicina, UBA
  • , Mariel MarderAffiliated withInstituto de Quimica y Fisicoquimica Biologicas, Facultad de Farmacia y Bioquimica, UBA
  • , Cristina WasowskiAffiliated withInstituto de Quimica y Fisicoquimica Biologicas, Facultad de Farmacia y Bioquimica, UBA
  • , Daniel CalvoAffiliated withInstituto de Biologia Celular y Neurociencias, Facultad de Medicina, UBA
  • , Alejandro C. PaladiniAffiliated withInstituto de Quimica y Fisicoquimica Biologicas, Facultad de Farmacia y Bioquimica, UBA

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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.

Flavonoids benzodiazepine receptors anxiolysis partial agonist