Research ArticlePharmacology

Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria

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Science Signaling  29 Nov 2016:
Vol. 9, Issue 456, pp. ra117
DOI: 10.1126/scisignal.aai8441

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Itch relief from biased agonists

Activating the kappa opioid receptor (KOR) can relieve itching that is not caused by allergic reactions. However, compounds that activate this receptor also cause unwanted side effects, such as dysphoria and sedation. KOR activation can trigger multiple downstream signaling pathways. Brust et al. characterized a biased agonist of this receptor that preferentially activated one downstream pathway over another. This agonist relieved itch in rodents without causing dysphoria or sedation. Thus, biased KOR agonists may provide a long-sought therapeutic option for intractable itch without the unwanted side effects.

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