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Updated: May 16, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Neuroactive flavonoids: new ligands for the Benzodiazepine receptors
J H Medina1, H Viola, C Wolfman
1Instituto de Biologia Celular y Neurociencias, Facultad de Medicina, UBA, Parguay, Buenos Aires Argentina.
Abstract:
Flavonoids isolated from plants used as tranquilizers in folkloric medicine have a selective affinity, for central benzodiazepine receptors (BDZ-Rs) and some of them possess a pharmacological profile compatible with a partial agonist action. Synthetic derivatives of the common flavone nucleus, give rise to high affinity ligands when electronegative groups are introduced in carbons 6 and/or 3'. Representative compounds such as 6,3'-dinitroflavone and, 6-bromo-3'-nitroflavone exhibit a high affinity for the BDZ-Rs (Ki = 1.5 to 30 nM) and have anxiolytic effects not associated with myorelaxant, sedative or amnesic actions. These compounds or similar ones, could lead to improved therapeutic drugs in the treatment of anxiety.
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