Flavonoid modulation of ionic currents mediated by GABAA and GABAC receptors
The modulation of ionotropic γ-aminobutyric acid (GABA) receptors (GABA-gated Cl- channels) by a group of natural and synthetic flavonoids was studied in electrophysiological experiments. Quercetin, apigenin, morine, chrysin and flavone inhibited ionic currents mediated by α1β1γ2s GABAA and ρ1 GABAC...
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| Formato: | Capítulo de libro |
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Elsevier
2003
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| Acceso en línea: | Registro en Scopus DOI Handle Registro en la Biblioteca Digital |
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| LEADER | 15242caa a22014297a 4500 | ||
|---|---|---|---|
| 001 | PAPER-5055 | ||
| 003 | AR-BaUEN | ||
| 005 | 20230518203440.0 | ||
| 008 | 190411s2003 xx ||||fo|||| 00| 0 eng|d | ||
| 024 | 7 | |2 scopus |a 2-s2.0-0037436059 | |
| 024 | 7 | |2 cas |a acetylcholine, 51-84-3, 60-31-1, 66-23-9; alpha naphthoflavone, 604-59-1; apigenin, 520-36-5; benzodiazepine, 12794-10-4; chrysin, 12624-02-1, 480-40-0; flavone, 525-82-6; flumazenil, 78755-81-4; kainic acid, 487-79-6; morin, 480-16-0; quercetin, 117-39-5; serotonin, 50-67-9 | |
| 040 | |a Scopus |b spa |c AR-BaUEN |d AR-BaUEN | ||
| 030 | |a EJPHA | ||
| 100 | 1 | |a Goutman, J.D. | |
| 245 | 1 | 0 | |a Flavonoid modulation of ionic currents mediated by GABAA and GABAC receptors |
| 260 | |b Elsevier |c 2003 | ||
| 270 | 1 | 0 | |m Calvo, D.J.; Inst. Invest. Ing. Genet. Biol. M., Vuelta de Obligado 2490, Capital Federal (1428), Buenos Aires, Argentina; email: dcalvo@dna.uba.ar |
| 506 | |2 openaire |e Política editorial | ||
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| 520 | 3 | |a The modulation of ionotropic γ-aminobutyric acid (GABA) receptors (GABA-gated Cl- channels) by a group of natural and synthetic flavonoids was studied in electrophysiological experiments. Quercetin, apigenin, morine, chrysin and flavone inhibited ionic currents mediated by α1β1γ2s GABAA and ρ1 GABAC receptors expressed in Xenopus laevis oocytes in the micromolar range. α1β1γ2s GABAA and ρ1 GABAC receptors differ largely in their sensitivity to benzodiazepines, but they were similarly modulated by different flavonoids. Quercetin produced comparable actions on currents mediated by α4β2 neuronal nicotinic acetylcholine, serotonin 5-HT3A and glutamate AMPA/kainate receptors. Sedative and anxiolytic flavonoids, like chrysin or apigenin, failed to potentiate but antagonized α1β1γ2s GABAA receptors. Effects of apigenin and quercetin on α1β1γ2s GABAA receptors were insensitive to the benzodiazepine antagonist flumazenil. Results indicate that mechanism/s underlying the modulation of ionotropic GABA receptors by some flavonoids differs from that described for classic benzodiazepine modulation. © 2003 Elsevier Science B.V. All rights reserved. |l eng | |
| 536 | |a Detalles de la financiación: Inter-American Development Bank | ||
| 536 | |a Detalles de la financiación: Fondo para la Investigación Científica y Tecnológica, PICT99 5-6800 | ||
| 536 | |a Detalles de la financiación: Consejo Nacional de Investigaciones Científicas y Técnicas, PIP 780/98 | ||
| 536 | |a Detalles de la financiación: We would like to thank people that generously provided us with plasmids carrying the different receptor subunits, Dr. Paul Whiting and Dr. Peter Seeburg for α 1 β 1 γ 2s GABA A ; Dr. Ricardo Miledi and Dr. Ataúlfo Martinez-Torres for ρ 1 GABA C and Dr. Stephen Heinemann, Dr. Jim Boulter and Dr. David Johnson for nicotinic α 4 β 2 and 5-HT 3A . We also thank Dr. Mariana del Vas and Dr. Marcelo Rubinstein for reading the manuscript. This work was supported by grants from CONICET (PIP 780/98) and FONCyT (PICT99 5-6800, BID 1201). | ||
| 593 | |a Inst. Invest. Ing. Genet. Biol. M., Vuelta de Obligado 2490, Capital Federal (1428), Buenos Aires, Argentina | ||
| 593 | |a Depto. Fisiol., Biol. Molec. y Cel., Fac. de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Buenos Aires, Argentina | ||
| 593 | |a Departamento de Neurociencias, Fac. de Med. y Odontología, Universidad del País Vasco, Leioa, Spain | ||
| 690 | 1 | 0 | |a BENZODIAZEPINE |
| 690 | 1 | 0 | |a FLAVONOID |
| 690 | 1 | 0 | |a GABA (Γ-AMINOBUTYRIC ACID) |
| 690 | 1 | 0 | |a GABAA RECEPTOR |
| 690 | 1 | 0 | |a GABAC RECEPTOR |
| 690 | 1 | 0 | |a 4 AMINOBUTYRIC ACID A RECEPTOR |
| 690 | 1 | 0 | |a 4 AMINOBUTYRIC ACID C RECEPTOR |
| 690 | 1 | 0 | |a ACETYLCHOLINE |
| 690 | 1 | 0 | |a ALPHA NAPHTHOFLAVONE |
| 690 | 1 | 0 | |a AMPA RECEPTOR |
| 690 | 1 | 0 | |a ANXIOLYTIC AGENT |
| 690 | 1 | 0 | |a APIGENIN |
| 690 | 1 | 0 | |a BENZODIAZEPINE |
| 690 | 1 | 0 | |a BRAIN RECEPTOR |
| 690 | 1 | 0 | |a CHLORIDE CHANNEL |
| 690 | 1 | 0 | |a CHRYSIN |
| 690 | 1 | 0 | |a FLAVONE |
| 690 | 1 | 0 | |a FLAVONOID |
| 690 | 1 | 0 | |a FLUMAZENIL |
| 690 | 1 | 0 | |a GLUTAMATE RECEPTOR |
| 690 | 1 | 0 | |a IONOTROPIC RECEPTOR |
| 690 | 1 | 0 | |a KAINIC ACID |
| 690 | 1 | 0 | |a KAINIC ACID RECEPTOR |
| 690 | 1 | 0 | |a MORIN |
| 690 | 1 | 0 | |a NICOTINIC RECEPTOR |
| 690 | 1 | 0 | |a QUERCETIN |
| 690 | 1 | 0 | |a RECEPTOR SUBUNIT |
| 690 | 1 | 0 | |a SEDATIVE AGENT |
| 690 | 1 | 0 | |a SEROTONIN |
| 690 | 1 | 0 | |a SEROTONIN 3 RECEPTOR |
| 690 | 1 | 0 | |a ARTICLE |
| 690 | 1 | 0 | |a DRUG ANTAGONISM |
| 690 | 1 | 0 | |a DRUG EFFECT |
| 690 | 1 | 0 | |a DRUG MECHANISM |
| 690 | 1 | 0 | |a ELECTROPHYSIOLOGY |
| 690 | 1 | 0 | |a ION CURRENT |
| 690 | 1 | 0 | |a PRIORITY JOURNAL |
| 690 | 1 | 0 | |a PROTEIN EXPRESSION |
| 690 | 1 | 0 | |a RECEPTOR SENSITIVITY |
| 690 | 1 | 0 | |a XENOPUS LAEVIS |
| 653 | 0 | 0 | |a ro 15 1788, Hoffmann La Roche, United States |
| 700 | 1 | |a Waxemberg, M.D. | |
| 700 | 1 | |a Doñate-Oliver, F. | |
| 700 | 1 | |a Pomata, P.E. | |
| 700 | 1 | |a Calvo, D.J. | |
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