Allosteric Modulation of αβδ GABAA Receptors
GABAA receptors mediate the majority of the fast inhibition in the mature brain and play an important role in the pathogenesis of many neurological and psychiatric disorders. The αβδ GABAA receptor localizes extra- or perisynaptically and mediates GABAergic tonic inhibition. Compared with synaptical...
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| Format: | Article |
| Language: | English |
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MDPI AG
2010-11-01
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| Series: | Pharmaceuticals |
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| Online Access: | http://www.mdpi.com/1424-8247/3/11/3461/ |
| _version_ | 1819117748937031680 |
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| author | Hua-Jun Feng |
| author_facet | Hua-Jun Feng |
| author_sort | Hua-Jun Feng |
| collection | DOAJ |
| description | GABAA receptors mediate the majority of the fast inhibition in the mature brain and play an important role in the pathogenesis of many neurological and psychiatric disorders. The αβδ GABAA receptor localizes extra- or perisynaptically and mediates GABAergic tonic inhibition. Compared with synaptically localized αβγ receptors, αβδ receptors are more sensitive to GABA, display relatively slower desensitization and exhibit lower efficacy to GABA agonism. Interestingly, αβδ receptors can be positively modulated by a variety of structurally different compounds, even at saturating GABA concentrations. This review focuses on allosteric modulation of recombinant αβδ receptor currents and αβδ receptor-mediated tonic currents by anesthetics and ethanol. The possible mechanisms for the positive modulation of αβδ receptors by these compounds will also be discussed. |
| first_indexed | 2024-12-22T05:37:55Z |
| format | Article |
| id | doaj.art-c12126845de44b09a352d3bc7ef78977 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-12-22T05:37:55Z |
| publishDate | 2010-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-c12126845de44b09a352d3bc7ef789772022-12-21T18:37:17ZengMDPI AGPharmaceuticals1424-82472010-11-013113461347710.3390/ph3113461Allosteric Modulation of αβδ GABAA ReceptorsHua-Jun FengGABAA receptors mediate the majority of the fast inhibition in the mature brain and play an important role in the pathogenesis of many neurological and psychiatric disorders. The αβδ GABAA receptor localizes extra- or perisynaptically and mediates GABAergic tonic inhibition. Compared with synaptically localized αβγ receptors, αβδ receptors are more sensitive to GABA, display relatively slower desensitization and exhibit lower efficacy to GABA agonism. Interestingly, αβδ receptors can be positively modulated by a variety of structurally different compounds, even at saturating GABA concentrations. This review focuses on allosteric modulation of recombinant αβδ receptor currents and αβδ receptor-mediated tonic currents by anesthetics and ethanol. The possible mechanisms for the positive modulation of αβδ receptors by these compounds will also be discussed.http://www.mdpi.com/1424-8247/3/11/3461/GABAA receptorsδ subunitmodulationkinetics |
| spellingShingle | Hua-Jun Feng Allosteric Modulation of αβδ GABAA Receptors Pharmaceuticals GABAA receptors δ subunit modulation kinetics |
| title | Allosteric Modulation of αβδ GABAA Receptors |
| title_full | Allosteric Modulation of αβδ GABAA Receptors |
| title_fullStr | Allosteric Modulation of αβδ GABAA Receptors |
| title_full_unstemmed | Allosteric Modulation of αβδ GABAA Receptors |
| title_short | Allosteric Modulation of αβδ GABAA Receptors |
| title_sort | allosteric modulation of αβδ gabaa receptors |
| topic | GABAA receptors δ subunit modulation kinetics |
| url | http://www.mdpi.com/1424-8247/3/11/3461/ |
| work_keys_str_mv | AT huajunfeng allostericmodulationofabdgabaareceptors |