Results 11 to 20 of about 400 (115)

In a Rat Model of Opioid Maintenance, the G Protein–Biased Mu Opioid Receptor Agonist TRV130 Decreases Relapse to Oxycodone Seeking and Taking and Prevents Oxycodone-Induced Brain Hypoxia [PDF]

Biological Psychiatry, 2020
Maintenance treatment with opioid agonists (buprenorphine, methadone) is effective for opioid addiction but does not eliminate opioid use in all patients. We modeled maintenance treatment in rats that self-administered the prescription opioid oxycodone.
Jennifer M Bossert, Eugene A Kiyatkin, David Perekopskiy   +2 more
exaly   +5 more sources

APOLLO‐2: A Randomized, Placebo and Active‐Controlled Phase III Study Investigating Oliceridine (TRV130), a G Protein–Biased Ligand at the μ‐Opioid Receptor, for Management of Moderate to Severe Acute Pain Following Abdominoplasty

Pain Practice, Volume 19, Issue 7, Page 715-731, September 2019., 2019
Abstract Objectives The clinical utility of conventional IV opioids is limited by the occurrence of opioid‐related adverse events. Oliceridine is a novel G protein–biased μ‐opioid receptor agonist designed to provide analgesia with an improved safety and tolerability profile.
Neil K. Singla, Franck Skobieranda, David G. Soergel, Monica Salamea, David A. Burt, Mark A. Demitrack, Eugene R. Viscusi   +6 more
wiley   +3 more sources

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

Journal of Pain Research, 2017
Neil Singla,1 Harold S Minkowitz,2 David G Soergel,3 David A Burt,3 Ruth Ann Subach,3 Monica Y Salamea,3 Michael J Fossler,3 Franck Skobieranda3 1Lotus Clinical Research, Pasadena, CA, 2Memorial Hermann Memorial City Medical Center, Houston, TX, 3Trevena,
Singla N, Minkowitz HS, Soergel DG, Burt DA, Subach RA, Salamea MY, Fossler MJ, Skobieranda F   +7 more
doaj   +1 more source

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

Journal of Pain Research, 2019
Sergio D Bergese,1 Marek Brzezinski,2 Gregory B Hammer,3 Timothy L Beard,4 Peter H Pan,5 Sharon E Mace,6 Richard D Berkowitz,7 Kristina Cochrane,8 Linda Wase,8 Harold S Minkowitz,9 Ashraf S Habib10 1School of Medicine, Stony Brook University, Stony Brook,
Bergese SD, Brzezinski M, Hammer GB, Beard TL, Pan PH, Mace SE, Berkowitz RD, Cochrane K, Wase L, Minkowitz HS, Habib AS   +10 more
doaj   +1 more source

The Oxford Catalogue of Opioids: A systematic synthesis of opioid drug names and their pharmacology

British Journal of Clinical Pharmacology, Volume 87, Issue 10, Page 3790-3812, October 2021., 2021
Aim The growing demand for analgesia, coupled with an increasing need to treat opioid dependence and overdose, has escalated the development of novel opioids. We aimed to quantify the number of opioid drugs developed and to catalogue them based on their pharmacology.
Georgia C. Richards, Konrad Sitkowski, Carl Heneghan, Jeffrey K. Aronson   +3 more
wiley   +1 more source

Addressing opioid tolerance and opioid‐induced hypersensitivity: Recent developments and future therapeutic strategies

Pharmacology Research &Perspectives, Volume 9, Issue 3, June 2021., 2021
The PAG‐RVM descending system under normal conditions. In the naïve state, GABAergic interneurons are tonically active, thus both PAG output neurons and OFF‐cells have low spontaneous firing rates. Activity in OFF‐cells causes antinociception, and activity in ON‐cells represents descending facilitation of pain.
Faris Khan, Aman Mehan
wiley   +1 more source

Biased versus Partial Agonism in the Search for Safer Opioid Analgesics

Molecules, 2020
Opioids such as morphine—acting at the mu opioid receptor—are the mainstay for treatment of moderate to severe pain and have good efficacy in these indications.
Joaquim Azevedo Neto, Anna Costanzini, Roberto De Giorgio, David G. Lambert, Chiara Ruzza, Girolamo Calò   +5 more
doaj   +1 more source

Synthesis, Radiosynthesis and Biological Evaluation of Buprenorphine‐Derived Phenylazocarboxamides as Novel μ‐Opioid Receptor Ligands

ChemMedChem, Volume 15, Issue 13, Page 1175-1186, July 3, 2020., 2020
Targeted replacement of a cinnamide for a phenylazocarboxamide moiety led to a novel type of buprenorphine‐derived opioid receptor ligand that display selectivity for the μ‐subtype. Besides good metabolic stability and no detectable cytotoxicity, the phenylazocarboxamide unit enabled straightforward access to an 18F‐fluorinated analogue, thus making ...
Jasmin Krüll, Stefanie K. Fehler, Laura Hofmann, Natascha Nebel, Simone Maschauer, Olaf Prante, Peter Gmeiner, Harald Lanig, Harald Hübner, Markus R. Heinrich   +9 more
wiley   +1 more source

The Influence of Renal or Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of Oliceridine

Clinical Pharmacology in Drug Development, Volume 9, Issue 5, Page 639-650, July 2020., 2020
Abstract Oliceridine is a G protein–biased ligand at the μ‐opioid receptor in development for treatment of moderate to severe acute pain. A phase 1, open‐label, single‐dose study investigated the pharmacokinetics and safety of oliceridine 0.5 mg intravenous (IV) in subjects with end‐stage renal disease (ESRD, n = 9) versus 1 mg in healthy controls (n =
Anne N. Nafziger, Kelly A. Arscott, Kristina Cochrane, Franck Skobieranda, David A. Burt, Michael J. Fossler   +5 more
wiley   +1 more source

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

Molecular Pain, 2017
Background µ-Opioid receptor internalization is considered to be critically linked to antinociceptive tolerance. Although µ-opioid receptor agonists have been administered simultaneously with other drugs to control pain, little information is available ...
Tomohisa Mori, Naoko Kuzumaki, Takamichi Arima, Michiko Narita, Ryunosuke Tateishi, Takashige Kondo, Yusuke Hamada, Hirotsugu Kuwata, Miho Kawata, Mitsuaki Yamazaki, Kazuyuki Sugita, Akinobu Matsuzawa, Kanae Baba, Takayasu Yamauchi, Kimio Higashiyama, Miki Nonaka, Kanako Miyano, Yasuhito Uezono, Minoru Narita   +18 more
doaj   +1 more source