Research ArticleNeuroscience

G protein signaling–biased agonism at the κ-opioid receptor is maintained in striatal neurons

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Sci. Signal.  07 Aug 2018:
Vol. 11, Issue 542, eaar4309
DOI: 10.1126/scisignal.aar4309

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Biasing pain treatment against side effects

Stimulating opioid receptors with targeted agonists can treat pain, but such drugs often cause unwanted and even dangerous side effects because they induce multiple intracellular pathways downstream of the receptor. Studies in cell lines and mouse models have proposed that so-called “biased” agonists, those that activate only antinociceptive G protein signaling, may lessen pain and itch without causing side effects. Ho et al. confirm this potential for targeting the κ-opioid receptor (KOR) by showing the biochemical and physiological effects of biased KOR agonists specifically on striatal neurons in mice. These findings indicate that cell culture–based predictions of biased KOR agonists may hold true in vivo and therefore may be a better way to treat pain in patients.