dc.creator | Viola, Haydee Ana Maria | |
dc.creator | Wolfman, C. | |
dc.creator | Marder, Nora Mariel | |
dc.creator | Goutman, Juan Diego | |
dc.creator | Bianchin, M | |
dc.creator | Wasowski, Cristina Lucia N. | |
dc.creator | Calvo, Daniel Juan | |
dc.creator | Izquierdo, I. | |
dc.creator | Paladini, Alejandro C. | |
dc.creator | Medina, Jorge Horacio | |
dc.date.accessioned | 2021-07-08T15:55:01Z | |
dc.date.accessioned | 2022-10-15T11:45:13Z | |
dc.date.available | 2021-07-08T15:55:01Z | |
dc.date.available | 2022-10-15T11:45:13Z | |
dc.date.created | 2021-07-08T15:55:01Z | |
dc.date.issued | 2000-12 | |
dc.identifier | Viola, Haydee Ana Maria; Wolfman, C.; Marder, Nora Mariel; Goutman, Juan Diego; Bianchin, M; et al.; 6-Chloro-3'-nitroflavone is a potent ligand for the benzodiazepine binding site of the GABA(A) receptor devoid of intrinsic activity; Pergamon-Elsevier Science Ltd; Pharmacology Biochemistry and Behavior; 65; 2; 12-2000; 313-320 | |
dc.identifier | 0091-3057 | |
dc.identifier | http://hdl.handle.net/11336/135735 | |
dc.identifier | CONICET Digital | |
dc.identifier | CONICET | |
dc.identifier.uri | https://repositorioslatinoamericanos.uchile.cl/handle/2250/4382345 | |
dc.description.abstract | 6-Chloro-3'-nitroflavone integrates a list of nearly 70 flavone derivatives synthesized in our laboratories. The effects of 6-chloro-3'- nitroflavone on the benzodiazepine binding sites (BDZ-BSs) of the GABA(A) receptor were examined in vitro and in vivo. 6-Chloro-3'-nitroflavone inhibited the [3H]flunitrazepam ([3H]FNZ) binding to rat cerebral cortex membranes with a K(i) of 6.68 nM and the addition of GABA to extensively washed membranes did not modify its affinity for the BDZ-BSs (GABA-shift = 1. 16 ± 0.12). The binding assays performed in rat striatal and cerebellar brain membranes showed that this compound has similar affinity to different populations of BDZ-BSs. Electrophysiological experiments revealed that 6- chloro-3'-nitroflavone did not affect GABA(A)-receptors (GABA(A)-Rs) responses recorded in Xenopus oocytes expressing α1β2γ(2s) subunits, but blocked the potentiation exerted by diazepam (DZ) on GABA-activated chloride currents. In vivo experiments showed that 6-chloro-3'-nitroflavone did not possess anxiolytic, anticonvulsant, sedative, myorelaxant actions in mice or amnestic effects in rats; however, 6-chloro-3'-nitroflavone antagonized diazepam-induced antianxiety action, anticonvulsion, short-term, and long- term amnesia and motor incoordination. These biochemical, electrophysiological, and pharmacological results suggest that 6-chloro-3'- nitroflavone behaves as an antagonist of the BDZ-BSs. | |
dc.language | eng | |
dc.publisher | Pergamon-Elsevier Science Ltd | |
dc.relation | info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0091305799001999 | |
dc.relation | info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/s0091-3057(99)00199-9 | |
dc.rights | https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ | |
dc.rights | info:eu-repo/semantics/restrictedAccess | |
dc.subject | ANTAGONIST | |
dc.subject | BENZODIAZEPINE BINDING SITE OF THE GABA(A) RECEPTOR | |
dc.subject | FLAVONOIDS | |
dc.title | 6-Chloro-3'-nitroflavone is a potent ligand for the benzodiazepine binding site of the GABA(A) receptor devoid of intrinsic activity | |
dc.type | info:eu-repo/semantics/article | |
dc.type | info:ar-repo/semantics/artículo | |
dc.type | info:eu-repo/semantics/publishedVersion | |