The structural patterns of the potentiation and the blockade of inhibitory <i>cys</i>-loop receptors through the transmembrane domain
Anion-conducting cys-loop receptors activated by -aminobutyric acid (GABAАRs) and glycine (GlyRs) have inhibitory activity in the brain and spinal cord. GABAАRs and GlyRs are targets for various substances that potentiate or inhibit the receptor functions. Many of these substances are clinically sig...
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| Format: | Article |
| Language: | English |
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Research Center of Neurology
2022-12-01
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| Series: | Анналы клинической и экспериментальной неврологии |
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| Online Access: | https://annaly-nevrologii.com/journal/pathID/article/viewFile/838/pdf |
| _version_ | 1828062039881285632 |
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| author | Alexey V. Rossokhin |
| author_facet | Alexey V. Rossokhin |
| author_sort | Alexey V. Rossokhin |
| collection | DOAJ |
| description | Anion-conducting cys-loop receptors activated by -aminobutyric acid (GABAАRs) and glycine (GlyRs) have inhibitory activity in the brain and spinal cord. GABAАRs and GlyRs are targets for various substances that potentiate or inhibit the receptor functions. Many of these substances are clinically significant agents to treat neurological and psychiatric conditions.
The review covers both our results and literature data on electrophysiology, mutations, and biochemistry of non-competitive antagonists, general anesthetics, barbiturates, and fenamates modulating GABAАRs and GlyRs. We focused on our own molecular modeling to determine the sites and the characteristics of binding of these substances to the GABAАR and GlyR transmembrane domain. With the structural patterns of the binding, we have identified possible molecular mechanisms of action for these substances. |
| first_indexed | 2024-04-10T22:22:50Z |
| format | Article |
| id | doaj.art-2c37a8e0dd2b472d8339853927c68d23 |
| institution | Directory Open Access Journal |
| issn | 2075-5473 2409-2533 |
| language | English |
| last_indexed | 2024-04-10T22:22:50Z |
| publishDate | 2022-12-01 |
| publisher | Research Center of Neurology |
| record_format | Article |
| series | Анналы клинической и экспериментальной неврологии |
| spelling | doaj.art-2c37a8e0dd2b472d8339853927c68d232023-01-17T12:35:36ZengResearch Center of NeurologyАнналы клинической и экспериментальной неврологии2075-54732409-25332022-12-01164445310.54101/ACEN.2022.4.6619The structural patterns of the potentiation and the blockade of inhibitory <i>cys</i>-loop receptors through the transmembrane domainAlexey V. Rossokhin0https://orcid.org/0000-0001-7024-7461Research Center of NeurolgyAnion-conducting cys-loop receptors activated by -aminobutyric acid (GABAАRs) and glycine (GlyRs) have inhibitory activity in the brain and spinal cord. GABAАRs and GlyRs are targets for various substances that potentiate or inhibit the receptor functions. Many of these substances are clinically significant agents to treat neurological and psychiatric conditions. The review covers both our results and literature data on electrophysiology, mutations, and biochemistry of non-competitive antagonists, general anesthetics, barbiturates, and fenamates modulating GABAАRs and GlyRs. We focused on our own molecular modeling to determine the sites and the characteristics of binding of these substances to the GABAАR and GlyR transmembrane domain. With the structural patterns of the binding, we have identified possible molecular mechanisms of action for these substances.https://annaly-nevrologii.com/journal/pathID/article/viewFile/838/pdfgabaа receptorglycine receptorpositive allosteric modulatorsnon-competitive antagonistsmolecular modeling |
| spellingShingle | Alexey V. Rossokhin The structural patterns of the potentiation and the blockade of inhibitory <i>cys</i>-loop receptors through the transmembrane domain Анналы клинической и экспериментальной неврологии gabaа receptor glycine receptor positive allosteric modulators non-competitive antagonists molecular modeling |
| title | The structural patterns of the potentiation and the blockade of inhibitory <i>cys</i>-loop receptors through the transmembrane domain |
| title_full | The structural patterns of the potentiation and the blockade of inhibitory <i>cys</i>-loop receptors through the transmembrane domain |
| title_fullStr | The structural patterns of the potentiation and the blockade of inhibitory <i>cys</i>-loop receptors through the transmembrane domain |
| title_full_unstemmed | The structural patterns of the potentiation and the blockade of inhibitory <i>cys</i>-loop receptors through the transmembrane domain |
| title_short | The structural patterns of the potentiation and the blockade of inhibitory <i>cys</i>-loop receptors through the transmembrane domain |
| title_sort | structural patterns of the potentiation and the blockade of inhibitory i cys i loop receptors through the transmembrane domain |
| topic | gabaа receptor glycine receptor positive allosteric modulators non-competitive antagonists molecular modeling |
| url | https://annaly-nevrologii.com/journal/pathID/article/viewFile/838/pdf |
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