Optical Control of Adenosine-Mediated Pain Modulation
Adenosine receptors (ARs) play many important roles in physiology and have been recognized as potential targets for pain relief. Here, we introduce three photoswitchable adenosine derivatives that function as light-dependent agonists for ARs and confer optical control to these G protein-coupled receptors. One of our compounds, AzoAdenosine-3, was evaluated in the classical formalin model of pain. The molecule, active in the dark, was not metabolized by adenosine deaminase and effectively reduced pain perception in a light-dependent manner. These antinociceptive effects suggested a major role for A1R and A3R in peripheral-mediated pain sensitization, whereas an average adenosine-mediated antinociceptive effect will be facilitated by A2AR and A2BR. Our results demonstrate that a photoswitchable adenosine derivative can be used to map the contribution of ARs mediating analgesia in vivo.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:32 |
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| Enthalten in: |
Bioconjugate chemistry - 32(2021), 9 vom: 15. Sept., Seite 1979-1983 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Hüll, Katharina [VerfasserIn] |
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| Links: |
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| Themen: |
Adenosine |
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| Anmerkungen: |
Date Completed 16.12.2021 Date Revised 16.12.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1021/acs.bioconjchem.1c00387 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM329914189 |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Adenosine receptors (ARs) play many important roles in physiology and have been recognized as potential targets for pain relief. Here, we introduce three photoswitchable adenosine derivatives that function as light-dependent agonists for ARs and confer optical control to these G protein-coupled receptors. One of our compounds, AzoAdenosine-3, was evaluated in the classical formalin model of pain. The molecule, active in the dark, was not metabolized by adenosine deaminase and effectively reduced pain perception in a light-dependent manner. These antinociceptive effects suggested a major role for A1R and A3R in peripheral-mediated pain sensitization, whereas an average adenosine-mediated antinociceptive effect will be facilitated by A2AR and A2BR. Our results demonstrate that a photoswitchable adenosine derivative can be used to map the contribution of ARs mediating analgesia in vivo | ||
| 650 | 4 | |a Journal Article | |
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| 700 | 1 | |a Fernández-Dueñas, Víctor |e verfasserin |4 aut | |
| 700 | 1 | |a Schönberger, Matthias |e verfasserin |4 aut | |
| 700 | 1 | |a López-Cano, Marc |e verfasserin |4 aut | |
| 700 | 1 | |a Trauner, Dirk |e verfasserin |4 aut | |
| 700 | 1 | |a Ciruela, Francisco |e verfasserin |4 aut | |
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