title: Neuroactive flavonoids: new ligands for the Benzodiazepine receptors.
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.
authors.affiliation: Instituto de Biologia Celular y Neurociencias, Facultad de Medicina, UBA, Parguay, Buenos Aires Argentina.
authors.forename: J H
authors.initials: JH
authors.lastname: Medina
authors.forename: H
authors.initials: H
authors.lastname: Viola
authors.forename: C
authors.initials: C
authors.lastname: Wolfman
authors.forename: M
authors.initials: M
authors.lastname: Marder
authors.forename: C
authors.initials: C
authors.lastname: Wasowski
authors.forename: D
authors.initials: D
authors.lastname: Calvo
authors.forename: A C
authors.initials: AC
authors.lastname: Paladini