INVESTIGADORES
VIOLA Haydee Ana Maria
artículos
Título:
6-methyl-3'-bromoflavone, a high-affinity ligand for the benzodiazepine binding site of the GABA(A) receptor with some antagonistic properties
Autor/es:
VIOLA, HAYDEE; MARDER, MARIEL; NUÑEZ, JULIAN; IZQUIERDO, LUCIANA; WASOWSKI, CRISTINA; WOLFMAN, CLAUDIA; ARDENGHI, PATRICIA; BARROS, DANIELA; MEDINA, JORGE H.; PALADINI, ALEJANDRO C.
Revista:
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
Editorial:
ACADEMIC PRESS INC ELSEVIER SCIENCE
Referencias:
Año: 1999 vol. 262 p. 643 - 646
ISSN:
0006-291X
Resumen:
6-Methyl-3´-bromoflavone inhibited [3H]flunitrazepam binding to the benzodiazepine binding site of the GABA(A) receptor (BDZ-bs) with Ki values between 10 and 50 nM in different brain regions. The GABA ratio of 1.03 for [3H]flunitrazepam binding to cerebral cortex, 0.76 for cerebellum, 0.7 for hippocampus, 0.7 for striatum, and 0.8 for spinal cord indicated an antagonistic or weak inverse agonistic profile of 6-methyl-3´-bromoflavone on BDZ-bs. Unlike classical benzodiazepines, it had no anticonvulsant, anxiolytic, myorelaxant, sedative, amnestic or motor incoordination effects. However, it antagonized the muscle relaxant, the sedative effect, and the changes in locomotor activity induced by diazepam. Taken together, these findings suggest that 6-methyl-3´-bromoflavone has an antagonistic profile on the BDZ-bs.
