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http://hdl.handle.net/2445/194890
Title: | Optical control of adenosine-mediated pain modulation |
Author: | Hüll, Katharina Fernández Dueñas, Víctor Schönberger, Matthias López-Cano, Marc Trauner, Dirk Ciruela Alférez, Francisco |
Keywords: | Adenosina Tractament del dolor Fisiologia Adenosine Pain treatment Physiology |
Issue Date: | 1-Dec-2021 |
Publisher: | American Chemical Society |
Abstract: | 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 peripheralmediated 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. |
Note: | Reproducció del document publicat a: https://doi.org/10.1021/acs.bioconjchem.1c00387 |
It is part of: | Bioconjugate Chemistry, 2021, vol. 32, num. 9, p. 1-5 |
URI: | http://hdl.handle.net/2445/194890 |
Related resource: | https://doi.org/10.1021/acs.bioconjchem.1c00387 |
ISSN: | 1043-1802 |
Appears in Collections: | Articles publicats en revistes (Patologia i Terapèutica Experimental) Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL)) |
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