Neuroactive flavonoids: new ligands for the Benzodiazepine receptors.

J. H. MEDINA; H. VIOLA; C. WOLFMAN; M. MARDER; C. WASOWSKI; D. CALVO; A. C. PALADINI

PHYTOMEDICINE

Año: 1998 vol. 5 p. 235 - 243

0944-7113

Flavonoids isolated from plants used as tranquilizers in folkloric medicine have a selective affinity for central benzodiazepine receptors (BDZ-Rs) and some of them posses 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.