Results 21 to 30 of about 400 (115)

Morphine‐induced respiratory depression is independent of β‐arrestin2 signalling

British Journal of Pharmacology, Volume 177, Issue 13, Page 2923-2931, July 2020., 2020
Background and Purpose GPCRs can signal through both G proteins and β‐arrestin2. For the μ‐opioid receptor, early experimental evidence from a single study suggested that G protein signalling mediates analgesia, whereas β‐arrestin2 signalling mediates respiratory depression and constipation.
Andrea Kliewer, Alexander Gillis, Rob Hill, Frank Schmiedel, Chris Bailey, Eamonn Kelly, Graeme Henderson, Macdonald J. Christie, Stefan Schulz   +8 more
wiley   +1 more source

G protein‐biased kratom‐alkaloids and synthetic carfentanil‐amide opioids as potential treatments for alcohol use disorder

British Journal of Pharmacology, Volume 177, Issue 7, Page 1497-1513, April 2020., 2020
▪ Background and Purpose Mitragyna speciosa, more commonly known as kratom, is a plant that contains opioidergic alkaloids but is unregulated in most countries. Kratom is used in the self‐medication of chronic pain and to reduce illicit and prescription opioid dependence.
Anna M. Gutridge, Meridith T. Robins, Robert J. Cassell, Rajendra Uprety, Kendall L. Mores, Mee Jung Ko, Gavril W. Pasternak, Susruta Majumdar, Richard M. van Rijn   +8 more
wiley   +1 more source

Oliceridine: A Novel Drug for the Management of Moderate to Severe Acute Pain – A Review of Current Evidence

Journal of Pain Research, 2021
Hon Sen Tan,1 Ashraf S Habib2 1Department of Women’s Anesthesia, KK Women’s and Children’s Hospital, 229899, Singapore; 2Department of Anesthesiology, Division of Women’s Anesthesia, Duke University Medical Center, Durham, NC ...
Tan HS, Habib AS
doaj  

Identification of a Conformational Equilibrium That Determines the Efficacy and Functional Selectivity of the μ‐Opioid Receptor

Angewandte Chemie, Volume 127, Issue 52, Page 15997-16002, December 21, 2015., 2015
Ein offener und geschlossener Fall: Die NMR‐Analyse ligandgebundener Zustände des μ‐Opioid‐Rezeptors ergab, dass die intrazelluläre Kavität des Rezeptors im Gleichgewicht zwischen geschlossenen und mehreren offenen Konformationen vorliegt und die Population jeder offenen Konformation die vom G‐Protein und vom β‐Arrestin vermittelten ...
Junya Okude, Takumi Ueda, Yutaka Kofuku, Motohiko Sato, Naoyuki Nobuyama, Keita Kondo, Yutaro Shiraishi, Takuya Mizumura, Kento Onishi, Mei Natsume, Masahiro Maeda, Hideki Tsujishita, Takefumi Kuranaga, Masayuki Inoue, Ichio Shimada   +14 more
wiley   +2 more sources

A Review of the Therapeutic Potential of Recently Developed G Protein-Biased Kappa Agonists

Frontiers in Pharmacology, 2019
Between 2000 and 2005 several studies revealed that morphine is more potent and exhibits fewer side effects in beta-arrestin 2 knockout mice. These findings spurred efforts to develop opioids that signal primarily via G protein activation and do not, or ...
Kendall L. Mores, Benjamin R. Cummins, Robert J. Cassell, Robert J. Cassell, Richard M. van Rijn, Richard M. van Rijn, Richard M. van Rijn   +6 more
doaj   +1 more source

Oliceridine for the Management of Moderate to Severe Acute Postoperative Pain: A Narrative Review

Drug Design, Development and Therapy, 2023
Neil Daksla,1 Ashley Wang,1 Zhaosheng Jin,1 Abhishek Gupta,1 Sergio D Bergese1,2 1Department of Anesthesiology, Stony Brook University Health Science Center, Stony Brook, NY, 11794-8480, USA; 2Department of Neurosurgery, Stony Brook University Health ...
Daksla N, Wang A, Jin Z, Gupta A, Bergese SD   +4 more
doaj  

The G protein-biased PZM21 and TRV130 act as partial agonists of μ-opioid receptors signaling to ion channel targets [PDF]

, 2018
Opioids exert many of their acute effects through modulating ion channels via Gβγ subunits. Some of their side effects are attributed to β-arrestin recruitment, and several biased agonists that do not activate this pathway have been developed recently.
Yudin, Yevgen, Rohacs, Tibor
openaire   +1 more source

<p>ATHENA: A Phase 3, Open-Label Study Of The Safety And Effectiveness Of Oliceridine (TRV130), A G-Protein Selective Agonist At The μ-Opioid Receptor, In Patients With Moderate To Severe Acute Pain Requiring Parenteral Opioid Therapy</p> [PDF]

Journal of Pain Research, 2019
Pain management with conventional opioids can be challenging due to dose-limiting adverse events (AEs), some of which may be related to the simultaneous activation of β-arrestin (a signaling pathway associated with opioid-related AEs) and G-protein pathways.
Sergio D Bergese, Marek Brzezinski, Gregory B Hammer, Timothy L Beard, Peter H Pan, Sharon E Mace, Richard D Berkowitz, Kristina Cochrane, Linda Wase, Harold S Minkowitz, Ashraf Habib   +10 more
openaire   +5 more sources

Progress on the development of Class A GPCR‐biased ligands

British Journal of Pharmacology, Volume 182, Issue 14, Page 3249-3300, July 2025.
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales, Magdalena M. Scharf, Marcel Bermudez, Attila Egyed, Rafael Franco, Olivia K. Hansen, Nadine Jagerovic, Jan Jakubík, György M. Keserű, Dóra Judit Kiss, Pawel Kozielewicz, Olav Larsen, Maria Majellaro, Ana Mallo‐Abreu, Gemma Navarro, Rubén Prieto‐Díaz, Mette M. Rosenkilde, Eddy Sotelo, Holger Stark, Tobias Werner, Laura M. Wingler   +20 more
wiley   +1 more source

Bivalent and bitopic ligands of the opioid receptors: The prospects of a dual approach

Medicinal Research Reviews, Volume 44, Issue 6, Page 2545-2599, November 2024.
Abstract Opioid receptors belonging to the class A G‐protein coupled receptors (GPCRs) are the targets of choice in the treatment of acute and chronic pain. However, their on‐target side effects such as respiratory depression, tolerance and addiction have led to the advent of the ‘opioid crisis’.
Marie Emilie Hovah, Ulrike Holzgrabe
wiley   +1 more source