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6-Methylapigenin and hesperidin: new valeriana flavonoids with activity on the CNS
This paper is the first report of the presence of 2S(-)-hesperidin in valeriana and describes that it has sedative and sleep-enhancing properties, and 6-methylapigenin (MA) was found to have anxiolytic properties and was able to potentiate the sleep- enhancing properties of hesperidIn (HN).
Central nervous system depressant action of flavonoid glycosides.
It is demonstrated in this work that these behavioural actions, as measured in the hole board, thiopental induced sleeping time and locomotor activity tests, are unlikely to involve a direct action on gamma-aminobutyric acid type A (GABA(A))) receptors.
Flavonoids and the Central Nervous System: from Forgotten Factors to Potent Anxiolytic Compounds
Semisynthetic derivatives of flavone obtained by introducing halogens, nitro groups or both in its molecule give rise to high affinity ligands for the benzodiazepine receptor, active in‐vivo; 6,3′‐dinitroflavone, for example, is an anxiolytic drug 30 times more potent than diazepam.
Sedative and sleep-enhancing properties of linarin, a flavonoid-isolated from Valeriana officinalis
The identification in V. officinalis of the flavone glycoside linarin (LN) and the discovery that it has, like HN, sedative and sleep-enhancing properties that are potentiated by simultaneous administration of valerenic acid (VA).
Isolation and identification of 6-methylapigenin, a competitive ligand for the brain GABA(A) receptors, from Valeriana wallichii.
Using the guidance by a competitive assay for the benzodiazepine binding site in the GABA(A) receptor, active compounds were isolated from the rhizomes and roots of Valeriana wallichii DC. The UV,
GABA(A)-receptor ligands of flavonoid structure.
The new research developments that have established the CNS-activity of some natural flavonoids are described and a survey of the occurrence of ligands for the benzodiazepine binding site in the flavonoid field is attempted.
Synergistic interaction between hesperidin, a natural flavonoid, and diazepam.
It is demonstrated that 6-Methylapigenin is able to potentiate the sleep-enhancing effect of hesperidin and this property is shared with various GABA(A) receptor ligands, among them the agonist diazepam, which was used to study the potentiation as measured in the hole board test.
Overview—Flavonoids: A New Family of Benzodiazepine Receptor Ligands
Flavonoid derivatives, such as 6,3′-dinitroflavone were found to have a very potent anxiolytic effect not associated with myorelaxant, amnestic or sedative actions, and could represent an improved therapeutic tool in the treatment of anxiety.
6-Bromoflavone, a high affinity ligand for the central benzodiazepine receptors is a member of a family of active flavonoids.
6-Bromoflavone, obtained by bromination of flavanone, binds to central benzodiazepine receptors with a Ki=70 nM and has a clear anxiolytic activity in mice, at 0.5 mg/kg i.p. A survey of the
Flavonoids as GABAA receptor ligands: the whole story?
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 GABAtype A selective agents further.