Predicting the Antinociceptive
Efficacy of σ<sub>1</sub> Receptor Ligands by a Novel Receptor
Fluorescence Resonance
Energy Transfer (FRET) Based Biosensor
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Abstract
We
have developed a novel methodology for monitoring the σ<sub>1</sub> receptor activation switch in living cells. Our assay uncovered
the intrinsic nature of σ<sub>1</sub> 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
σ<sub>1</sub> receptor ligands