6-bromoflavone, a high affinity ligand for the central benzodiazepine receptors is a member of a family of active flavonoids

Marder M.; Wasowski, C; Paladini A.C.; Viola, H.; Wolfman C.; Medina, J.H.; Waterman P.G.; Cassels, B.K.

Keywords: kinetics, acid, flavonoids, mouse, animals, maze, binding, learning, structure, mice, experiment, male, receptor, motor, agents, flavonoid, tissue, affinity, drug, molecular, article, variance, analysis, activity, benzodiazepine, controlled, animal, relation, labels, study, relationship, derivative, priority, of, flavone, bromination, intraperitoneal, administration, nonhuman, journal, tranquilizing, Anti-Anxiety, Flunitrazepam, gamma-Aminobutyric, Receptors,, GABA-A, Structure-Activity, Animalia

Abstract

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 structure/affinity relationship for those receptors in a series of natural and synthetic flavonoids is presented.

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Título de la Revista: BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
Volumen: 223
Número: 2
Editorial: ACADEMIC PRESS INC ELSEVIER SCIENCE
Fecha de publicación: 1996
Página de inicio: 384
Página final: 389
URL: http://www.scopus.com/inward/record.url?eid=2-s2.0-0004396593&partnerID=q2rCbXpz