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. 2018 Apr 5;9:112. doi: 10.3389/fpsyt.2018.00112

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Copyright © 2018 Robins, Chiang, Mores, Alongkronrusmee and van Rijn.

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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SNC80 is a β-arrestin-biased agonist with comparable potency across species in heterologous cell systems. At the hDOR, SNC80 acts as a β-arrestin-2 super-agonist compared with the endogenous agonist leu-enkephalin and the weak β-arrestin-2 recruiter TAN-67 (A). SNC80 and TAN-67 bind to hDOR with similar affinity (B). Schematic representation of the observed ligand bias of TAN-67 and SNC80 at hDOR, with calculated bias factor (C). SNC80 and Leu-enkephalin have similar potency to inhibit forskolin-induced cAMP production at hDOR (D), rDOR (E), and mDOR (F). A representative summation is shown (n ≥ 3).