Agonist-selective NOP receptor phosphorylation correlates in vitro and in vivo and reveals differential post-activation signaling by chemically diverse agonists

Oliceridine (TRV130), a Novel G Protein-Biased Ligand at the μ-Opioid Receptor, Demonstrates a Predictable Relationship Between Plasma Concentrations and Pain Relief. I: Development of a Pharmacokinetic/Pharmacodynamic Model

(2018) Michael J. Fossler et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Pain Therapy Guided by Purpose and Perspective in Light of the Opioid Epidemic

(2018) Amie L. Severino et al.   Frontiers in Psychiatry

A bifunctional nociceptin and mu opioid receptor agonist is analgesic without opioid side effects in nonhuman primates

(2018) Huiping Ding et al.   Science Translational Medicine

Effects of acute and repeated treatment with the biased mu opioid receptor agonist TRV130 (oliceridine) on measures of antinociception, gastrointestinal function, and abuse liability in rodents

(2017) Ahmad A Altarifi et al.   JOURNAL OF PSYCHOPHARMACOLOGY

Usefulness for the combination of G protein- and β-arrestin-biased ligands of μ-opioid receptors: Prevention of antinociceptive tolerance

(2017) Tomohisa Mori et al.   Molecular Pain

Cebranopadol, a novel first-in-class analgesic drug candidate

(2017) Annette Christoph et al.   PAIN

Biased Opioid Receptor Ligands: Gain without Pain

(2017) Ravi Ranjan et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Antihyperalgesic, Antiallodynic, and Antinociceptive Effects of Cebranopadol, a Novel Potent Nociceptin/Orphanin FQ and Opioid Receptor Agonist, after Peripheral and Central Administration in Rodent Models of Neuropathic Pain

(2017) Thomas M. Tzschentke et al.   Pain Practice

A randomized, Phase IIb study investigating oliceridine (TRV130), a novel µ-receptor G-protein pathway selective (µ-GPS) modulator, for the management of moderate to severe acute pain following abdominoplasty

(2017) Neil Singla et al.   Journal of Pain Research

In vitro functional characterization of novel nociceptin/orphanin FQ receptor agonists in recombinant and native preparations

(2016) Federica Ferrari et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility

(2016) Nurulain T. Zaveri   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Phosphorylation Sites Regulating sst3Somatostatin Receptor Trafficking

(2016) Andreas Lehmann et al.   MOLECULAR ENDOCRINOLOGY

Research Resource: Real-Time Analysis of Somatostatin and Dopamine Receptor Signaling in Pituitary Cells Using a Fluorescence-Based Membrane Potential Assay

(2016) Thomas Günther et al.   MOLECULAR ENDOCRINOLOGY

2016 update of the PRIDE database and its related tools

(2016) Juan Antonio Vizcaíno et al.   NUCLEIC ACIDS RESEARCH

A randomized, phase 2 study investigating TRV130, a biased ligand of the μ-opioid receptor, for the intravenous treatment of acute pain

(2016) Eugene R. Viscusi et al.   PAIN

A key role for the N/OFQ-NOP receptor system in modulating nicotine taking in a model of nicotine and alcohol co-administration

(2016) Andrea Cippitelli et al.   Scientific Reports

Cardiac β2-Adrenergic Receptor Phosphorylation at Ser355/356 Regulates Receptor Internalization and Functional Resensitization

(2016) Xiaofang Fan et al.   PLoS One

Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (Ro 64-6198)

(2015) Steven D. Chang et al.   ACS Chemical Neuroscience

Phosphoproteomic analysis of the mouse brain mu-opioid (MOP) receptor

(2015) Lionel Moulédous et al.   FEBS LETTERS

Knock-In Mice with NOP-eGFP Receptors Identify Receptor Cellular and Regional Localization

(2015) Akihiko Ozawa et al.   JOURNAL OF NEUROSCIENCE

Nociceptin and the nociceptin receptor in learning and memory

(2015) Raül Andero   PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY

Loss of Morphine Reward and Dependence in Mice Lacking G Protein–Coupled Receptor Kinase 5

(2014) Laura Glück et al.   BIOLOGICAL PSYCHIATRY

Different mechanisms of homologous and heterologous μ-opioid receptor phosphorylation

(2014) Anika Mann et al.   BRITISH JOURNAL OF PHARMACOLOGY

Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers

(2014) David G. Soergel et al.   PAIN

Biased ligands at G-protein-coupled receptors: promise and progress

(2014) Jonathan D. Violin et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Opioid receptor desensitization: mechanisms and its link to tolerance

(2014) Stéphane Allouche et al.   Frontiers in Pharmacology

Heterologous regulation of agonist-independent μ-opioid receptor phosphorylation by protein kinase C

(2013) Susann Illing et al.   BRITISH JOURNAL OF PHARMACOLOGY

Advances in Analysis of Low Signal-to-Noise Images Link Dynamin and AP2 to the Functions of an Endocytic Checkpoint

(2013) François Aguet et al.   DEVELOPMENTAL CELL

Phosphorylation of Threonine 333 Regulates Trafficking of the Human sst5Somatostatin Receptor

(2013) Aline Petrich et al.   MOLECULAR ENDOCRINOLOGY

Deciphering µ-opioid receptor phosphorylation and dephosphorylation in HEK293 cells

(2012) Christian Doll et al.   BRITISH JOURNAL OF PHARMACOLOGY

Serine 363 Is Required for Nociceptin/Orphanin FQ Opioid Receptor (NOPR) Desensitization, Internalization, and Arrestin Signaling

(2012) Nancy R. Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

GRK2 Protein-mediated Transphosphorylation Contributes to Loss of Function of μ-Opioid Receptors Induced by Neuropeptide FF (NPFF2) Receptors

(2012) Lionel Moulédous et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Transplantable Phosphorylation Probe for Direct Assessment of G Protein-Coupled Receptor Activation

(2012) Andrea Kliewer et al.   PLoS One

Agonist-selective patterns of µ-opioid receptor phosphorylation revealed by phosphosite-specific antibodies

(2011) Christian Doll et al.   BRITISH JOURNAL OF PHARMACOLOGY

Mechanisms of rapid opioid receptor desensitization, resensitization and tolerance in brain neurons

(2011) Vu C Dang et al.   BRITISH JOURNAL OF PHARMACOLOGY

Pasireotide and Octreotide Stimulate Distinct Patterns of sst2ASomatostatin Receptor Phosphorylation

(2010) Florian Pöll et al.   MOLECULAR ENDOCRINOLOGY

The effects of nociceptin/orphanin FQ receptor agonist Ro 64-6198 and diazepam on antinociception and remifentanil self-administration in rhesus monkeys

(2010) Christopher A. Podlesnik et al.   PSYCHOPHARMACOLOGY

Kinase cascades and ligand-directed signaling at the kappa opioid receptor

(2010) Michael R. Bruchas et al.   PSYCHOPHARMACOLOGY

Nociceptin/Orphanin FQ Receptor Activation Attenuates Antinociception Induced by Mixed Nociceptin/Orphanin FQ/ -Opioid Receptor Agonists

(2009) T. V. Khroyan et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Comparison of the Antinociceptive and Antirewarding Profiles of Novel Bifunctional Nociceptin Receptor/ -Opioid Receptor Ligands: Implications for Therapeutic Applications

(2009) L. Toll et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Nocistatin and nociceptin given centrally induce opioid-mediated gastric mucosal protection

(2008) Zoltán S. Zádori et al.   PEPTIDES

Effects of nociceptin/orphanin FQ receptor (NOP) agonist, Ro64-6198, on reactivity to acute pain in mice: Comparison to morphine

(2007) David Reiss et al.   EUROPEAN JOURNAL OF PHARMACOLOGY