Predicting the Antinociceptive Efficacy of σ₁ Receptor Ligands by a Novel Receptor Fluorescence Resonance Energy Transfer (FRET) Based Biosensor

Abstract

We have developed a novel methodology for monitoring the σ₁ receptor activation switch in living cells. Our assay uncovered the intrinsic nature of σ₁ receptor ligands by recording the ligand-mediated conformational changes of this chaperone protein. The change triggered by each ligand correlated well with its ability to attenuate formalin induced nociception in an animal model of pain. This tool may assist in predicting the antinociceptive efficacy of σ₁ receptor ligands