Optical Control of Adenosine-Mediated Pain Modulation.

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 peripheral-mediated pain sensitization, whereas an average adenosine-mediated antinociceptive effect will be facilitated by A_2AR and A_2BR.

SUBMITTER: Hull K 

PROVIDER: S-EPMC8634359 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature