References 7. Fossler MJ, Sadler BM, Farrell C, Burt DA, Pitsiu M, Skobieranda F, Soergel DG. Oliceridine (TRV130), a novel G protein-biased ligand at the mu-opioid receptor, a predictable relationship between plasma concentrations and pain relief. I: Development of pharmacokinetic/pharmacodynamic model. J Clin Pharmacol. 2018; 58: 750–61 doi: 10.1002/jcph.1076. 8. Dewire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violoin JD. A G protein-biased ligand at the -opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine. J Pharmacol Exp Ther. 2013; 344: 708–17 doi: 10.1124/jpet.112.201616. 9. Manglik A et al. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016; 537: 185–90 doi: 10.1038/nature19112. 10. Raehal KM, Walker JKL, Bohn LM. Morphine side effects in -arrestin 2 knockout mice. J Pharmacol Ther. 2005; 314: 1195–2001 doi: 10.1124/jpet.105.087254. 11. Gillis A et al. Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists. Sci Signal. 2020; 13: eaaz3140 doi: 10.1126/scisignal.aaz3140. 12. Stahl EL, Bohn LM. Low intrinsic efficacy alone cannot explain the improved side effect profiles of new opioid agonists. Biochem. 2021; doi: 10.1021/acs.biochem.1c00466. 13. Dahan A, Dam CJ van, Niesters M, Velzen M van, Fossler MJ, Demitrack MA, Olofsen E. Benefit and risk evaluation of biased -receptor agonist oliceridine versus morphine. Anesthesiology. 2020; 133: 559–568 doi: 10.1097/ALN.0000000000003441. 14. Soergel G, Subach RS, Burnam N, Lark MW, James IE, Sadler BM, Skobieranda F, Violin JD, Webster LR. Biased agonism of the µ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects vs. morphine: a randomized, double-blind, placebo-controlled, crossover study in healthy volunteers. Pain. 2014; 155: 1829–1835 doi: 10.1016/j.pain.2014.06.011. 15. Viscussi ER, Webster I, Kuss M, Daniels S, Bolognese JA, Zuckerman S, Soergel DG, Subach RA, Cook E, Skobieranda F. A randomized, phase-2 study investigating TRV130, a biased-ligand of the mu-opioid receptor, for intravenous treatment of pain. Pain. 2016; 157: 264–272 doi: 10.1097/j.pain.0000000000000363. 94
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