IQUIFIB 02644
INSTITUTO DE QUIMICA Y FISICOQUIMICA BIOLOGICAS "PROF. ALEJANDRO C. PALADINI"
Unidad Ejecutora - UE
artículos
Título:
Flavonoids as GABAA receptor ligands: the whole story?
Autor/es:
CRISTINA WASOWSKI; MARIEL MARDER
Revista:
Journal of Experimental Pharmacology
Editorial:
Dove press
Referencias:
Año: 2012 vol. 4 p. 9 - 24
ISSN:
1179-1454
Resumen:
Abstract: Benzodiazepines 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, and ethanol and barbiturate potentiation and
tolerance. They exert their therapeutic effects via binding to the benzodiazepine binding site
of gamma-aminobutyric acid (GABA) type A receptors, and allosterically modulating the
chloride flux through the ion channel complex. First isolated from plants used as tranquilizers
in folkloric medicine, some natural flavonoids have been shown to possess selective affinity
for the benzodiazepine binding site with a broad spectrum of central nervous system effects.
Since the initial search for alternative benzodiazepine ligands amongst the flavonoids, a list
of successful synthetic derivatives has been generated with enhanced activities. This review
provides an update on research developments that have established the activity of natural and
synthetic flavonoids on GABA type A receptors. Flavonoids are prominent drugs in the treatment
of mental disorders, and can also be used as tools to study modulatory sites at GABA type
A receptors and to develop GABA type A selective agents further.Benzodiazepines 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, and ethanol and barbiturate potentiation and
tolerance. They exert their therapeutic effects via binding to the benzodiazepine binding site
of gamma-aminobutyric acid (GABA) type A receptors, and allosterically modulating the
chloride flux through the ion channel complex. First isolated from plants used as tranquilizers
in folkloric medicine, some natural flavonoids have been shown to possess selective affinity
for the benzodiazepine binding site with a broad spectrum of central nervous system effects.
Since the initial search for alternative benzodiazepine ligands amongst the flavonoids, a list
of successful synthetic derivatives has been generated with enhanced activities. This review
provides an update on research developments that have established the activity of natural and
synthetic flavonoids on GABA type A receptors. Flavonoids are prominent drugs in the treatment
of mental disorders, and can also be used as tools to study modulatory sites at GABA type
A receptors and to develop GABA type A selective agents further.
