Pharmacology

Partners in Pain Prevention

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Science  30 Jul 2010:
Vol. 329, Issue 5991, pp. 492
DOI: 10.1126/science.329.5991.492-c

Opioid receptors mediate the physiologic effects of morphine, which allows patients to tolerate otherwise debilitating pain, but chronic exposure to morphine results in diminished analgesia. Gupta et al. have explored the changes that occur as tolerance develops. The µ- and δ-opioid receptors have distinct preferences for ligands and interact to form heterodimeric receptors with new properties. When the two receptors work together, low concentrations of a δ receptor agonist that on its own is not sufficient to trigger signaling can potentiate activation of the heterodimer by µ- receptor agonists. Using a monoclonal antibody that recognized only the heterodimeric receptor, the authors showed that heterodimeric receptors accumulated in brain regions that process pain perception in mice as they developed tolerance to chronically administered morphine. These results implicate opioid receptor heterodimers as potential targets for therapeutics designed to manage pain or addiction.

Sci. Signal. 3, ra54 (2010).

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