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Cell·· 2 days agoPickScore79

An opioid efficacy switch for reversible optical control of analgesia.

An opioid efficacy switch for reversible optical control of analgesia.

In brief

A reversibly photoswitchable morphinan agonist, azo-morphine-3 (AM-3), interconverts between low (trans) and high (cis) efficacy states at the mu-opioid receptor under light, with each state showing distinct binding modes and ligand, receptor, and G protein dynamics. In mice, AM-3 enabled reversible, repeatable optical control of antinociception across pain models with a reduced side effect profile, owing to limited brain accumulation and local activation.

Why it matters

It offers light-gated, reversible control of mu-opioid receptor analgesia with fewer side effects in mice.

Source: Cell · doi.org

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