Details

Autor(en) / Beteiligte

• Hüll, Katharina
• Fernández-Dueñas, Víctor
• Schönberger, Matthias
• López-Cano, Marc
• Trauner, Dirk
• Ciruela, Francisco

Titel

Optical Control of Adenosine-Mediated Pain Modulation

Ist Teil von

• Bioconjugate chemistry, 2021-09, Vol.32 (9), p.1979-1983

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2021

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• 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.