Optical Control of Adenosine-Mediated Pain Modulation

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

Research output: Contribution to journalArticlepeer-review


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.

Original languageEnglish (US)
Pages (from-to)1979-1983
Number of pages5
JournalBioconjugate Chemistry
Issue number9
StatePublished - Sep 15 2021

ASJC Scopus subject areas

  • Biotechnology
  • Bioengineering
  • Biomedical Engineering
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry


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