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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todo:paper_00142999_v461_n2-3_p79_Goutman2023-10-03T14:12:06Z Flavonoid modulation of ionic currents mediated by GABAA and GABAC receptors Goutman, J.D. Waxemberg, M.D. Doñate-Oliver, F. Pomata, P.E. Calvo, D.J. Benzodiazepine Flavonoid GABA (γ-aminobutyric acid) GABAA receptor GABAC receptor 4 aminobutyric acid A receptor 4 aminobutyric acid C receptor acetylcholine alpha naphthoflavone AMPA receptor anxiolytic agent apigenin benzodiazepine brain receptor chloride channel chrysin flavone flavonoid flumazenil glutamate receptor ionotropic receptor kainic acid kainic acid receptor morin nicotinic receptor quercetin receptor subunit sedative agent serotonin serotonin 3 receptor article drug antagonism drug effect drug mechanism electrophysiology ion current priority journal protein expression receptor sensitivity Xenopus laevis 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. Fil:Goutman, J.D. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Pomata, P.E. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Calvo, D.J. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_00142999_v461_n2-3_p79_Goutman |
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Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
Benzodiazepine Flavonoid GABA (γ-aminobutyric acid) GABAA receptor GABAC receptor 4 aminobutyric acid A receptor 4 aminobutyric acid C receptor acetylcholine alpha naphthoflavone AMPA receptor anxiolytic agent apigenin benzodiazepine brain receptor chloride channel chrysin flavone flavonoid flumazenil glutamate receptor ionotropic receptor kainic acid kainic acid receptor morin nicotinic receptor quercetin receptor subunit sedative agent serotonin serotonin 3 receptor article drug antagonism drug effect drug mechanism electrophysiology ion current priority journal protein expression receptor sensitivity Xenopus laevis |
| spellingShingle |
Benzodiazepine Flavonoid GABA (γ-aminobutyric acid) GABAA receptor GABAC receptor 4 aminobutyric acid A receptor 4 aminobutyric acid C receptor acetylcholine alpha naphthoflavone AMPA receptor anxiolytic agent apigenin benzodiazepine brain receptor chloride channel chrysin flavone flavonoid flumazenil glutamate receptor ionotropic receptor kainic acid kainic acid receptor morin nicotinic receptor quercetin receptor subunit sedative agent serotonin serotonin 3 receptor article drug antagonism drug effect drug mechanism electrophysiology ion current priority journal protein expression receptor sensitivity Xenopus laevis Goutman, J.D. Waxemberg, M.D. Doñate-Oliver, F. Pomata, P.E. Calvo, D.J. Flavonoid modulation of ionic currents mediated by GABAA and GABAC receptors |
| topic_facet |
Benzodiazepine Flavonoid GABA (γ-aminobutyric acid) GABAA receptor GABAC receptor 4 aminobutyric acid A receptor 4 aminobutyric acid C receptor acetylcholine alpha naphthoflavone AMPA receptor anxiolytic agent apigenin benzodiazepine brain receptor chloride channel chrysin flavone flavonoid flumazenil glutamate receptor ionotropic receptor kainic acid kainic acid receptor morin nicotinic receptor quercetin receptor subunit sedative agent serotonin serotonin 3 receptor article drug antagonism drug effect drug mechanism electrophysiology ion current priority journal protein expression receptor sensitivity Xenopus laevis |
| description |
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. |
| format |
JOUR |
| author |
Goutman, J.D. Waxemberg, M.D. Doñate-Oliver, F. Pomata, P.E. Calvo, D.J. |
| author_facet |
Goutman, J.D. Waxemberg, M.D. Doñate-Oliver, F. Pomata, P.E. Calvo, D.J. |
| author_sort |
Goutman, J.D. |
| title |
Flavonoid modulation of ionic currents mediated by GABAA and GABAC receptors |
| title_short |
Flavonoid modulation of ionic currents mediated by GABAA and GABAC receptors |
| title_full |
Flavonoid modulation of ionic currents mediated by GABAA and GABAC receptors |
| title_fullStr |
Flavonoid modulation of ionic currents mediated by GABAA and GABAC receptors |
| title_full_unstemmed |
Flavonoid modulation of ionic currents mediated by GABAA and GABAC receptors |
| title_sort |
flavonoid modulation of ionic currents mediated by gabaa and gabac receptors |
| url |
http://hdl.handle.net/20.500.12110/paper_00142999_v461_n2-3_p79_Goutman |
| work_keys_str_mv |
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