Neuroactive flavonoids: new ligands for the Benzodiazepine receptors

• Published in: Phytomedicine (Stuttgart) Vol. 5; no. 3; pp. 235 - 243
• Main Authors: Medina, J.H., Viola, H., Wolfman, C., Marder, M., Wasowski, C., Calvo, D., Paladini, A.C.
• Format: Journal Article
• Language: English
• Published: Germany Elsevier GmbH 01.05.1998
• Subjects: anxiolysis; benzodiazepine receptors; flavonoids; partial agonist; partial agonist; benzodiazepine receptors; anxiolysis; flavonoids
• ISSN: 0944-7113; 1618-095X
• DOI: 10.1016/S0944-7113(98)80034-2

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.