Results 101 to 110 of about 400 (115)

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

Pain, 2014
Opioids provide powerful analgesia but also efficacy-limiting adverse effects, including severe nausea, vomiting, and respiratory depression, by activating μ-opioid receptors. Preclinical models suggest that differential activation of signaling pathways downstream of these receptors dissociates analgesia from adverse effects; however, this has not yet ...
David G Soergel, Michael W Lark, Franck Skobieranda   +2 more
exaly   +3 more sources

Oliceridine (TRV130): a biased agonist of the μ opioid receptor as a novel analgesic

Jianjun Cheng
exaly   +2 more sources

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

Journal of Clinical Pharmacology, 2018
AbstractConventional opioids bind to μ‐opioid receptors and activate 2 downstream signaling pathways: G‐protein coupling, linked to analgesia, and β‐arrestin recruitment, linked to opioid‐related adverse effects and limiting efficacy. Oliceridine (TRV130) is a novel G protein–biased ligand at the μ‐opioid receptor that differentially activates G ...
Michael J Fossler, Colm Farrell, David A Burt   +2 more
exaly   +3 more sources

Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain

Journal of Medicinal Chemistry, 2013
The concept of "ligand bias" at G protein coupled receptors has been introduced to describe ligands which preferentially stimulate one intracellular signaling pathway over another. There is growing interest in developing biased G protein coupled receptor ligands to yield safer, better tolerated, and more efficacious drugs.
Xiao-Tao, Chen, Philip, Pitis, Guodong, Liu, Catherine, Yuan, Dimitar, Gotchev, Conrad L, Cowan, David H, Rominger, Michael, Koblish, Scott M, Dewire, Aimee L, Crombie, Jonathan D, Violin, Dennis S, Yamashita   +11 more
openaire   +2 more sources

I1. A Randomized, Placebo- and Active-Controlled Phase 2b Study Investigating Oliceridine (TRV130)

Pain Management Nursing, 2017
David Soergel, Harold Minkowitz, David Burt, Franck Skobieranda   +3 more
openaire   +1 more source

Abuse-related effects of the biased mu opioid receptor agonist trv130 on intracranial selfstimulation in rats

Drug and Alcohol Dependence, 2017
Ahmad Altarifi, Bruce Blough, S. Steven Negus   +2 more
openaire   +1 more source

I3. Oliceridine (TRV130) Has a Differentiated Profile of G Protein and β-arrestin Signaling Versus Select Opioids

Pain Management Nursing, 2017
Conrad Cowan, William Gowen-MacDonald, Thomas Graczyk, Mike Lark   +3 more
openaire   +1 more source

I2. Rapid Onset of Pain Relief with Oliceridine (TRV130) vs. Morphine: a Phase 2a/b Study Analysis

Pain Management Nursing, 2017
David Soergel, Eugene Viscusi, Lynn Webster, David Burt, Franck Skobieranda   +4 more
openaire   +1 more source

APOLLO-1: a Randomized, Controlled, Phase 3 Study of Oliceridine (TRV130) for the Treatment of Moderate to Severe Pain Following Bunionectomy

The Spine Journal, 2017
Neil K. Singla, Anthony Senagore, Eugene R. Viscusi, David A. Burt, David Soergel   +4 more
openaire   +1 more source

(478) TRV130, a novel biased opioid ligand, elicits increased analgesia with reduced adverse effects compared to morphine in healthy volunteers

The Journal of Pain, 2014
D. Soergel, R. Subach, I. James, J. Violin, F. Skobieranda, B. Sadler, N. Burnham, T. Theisen, M. Lark, L. Webster   +9 more
openaire   +1 more source