Results 51 to 60 of about 762 (132)

The c‐Src inhibitor eCF506 diminishes opioid tolerance and reduces β‐arrestin2 recruitment

British Journal of Pharmacology, EarlyView.
Morphine activation of μ receptors causes tolerance through c‐Src activation and β‐arrestin2 recruitment. c‐Src inhibition or degradation reduces β‐arrestin2 recruitment, μ receptor endocytosis, while causing receptor upregulation, all likely contributing to reduced morphine tolerance.
Samuel Singleton, Fraser Nunn, Erika Lace, Álvaro Lorente‐Macías, Rachel Toth, Asier Unciti‐Broceta, Tim G. Hales   +6 more
wiley   +1 more source

Oliceridine Exhibits Improved Tolerability Compared to Morphine at Equianalgesic Conditions: Exploratory Analysis from Two Phase 3 Randomized Placebo and Active Controlled Trials

, 2022
Introduction In the management of postoperative acute moderate-to-severe pain, opioids remain an important component. However, conventional opioids have a narrow therapeutic index and are associated with dose-limiting opioid-related ...
Wase, Linda, Hammer, Gregory B., Fossler, Michael J., Michalsky, Cathy, Khanna, Ashish K., Little, Roderick, Ayad, Sabry, Demitrack, Mark A.   +7 more
core   +1 more source

Low Incidence of Opioid-Induced Respiratory Depression Observed with Oliceridine Regardless of Age or Body Mass Index: Exploratory Analysis from a Phase 3 Open-Label Trial in Postsurgical Pain [PDF]

, 2021
IntroductionAdvanced age and obesity are reported to increase the risk of opioid-induced respiratory depression (OIRD). Oliceridine, an intravenous opioid, is a G-protein-biased agonist at the µ-opioid receptor that may provide improved safety.
Wase, Linda, Pan, Peter H, Michalsky, Cathy, Bourne, Michael H, Bergese, Sergio D, Candiotti, Keith A, Habib, Ashraf S, Hammer, Gregory B, Brzezinski, Marek, Demitrack, Mark A   +9 more
core   +1 more source

Spatiotemporal dynamics of β‐arrestin‐mediated Src activation in 5‐HT7 receptor signaling pathway

The FEBS Journal, Volume 293, Issue 16, Page 5008-5023, August 2026.
GPCRs induce distinct cellular responses via G protein‐ or β‐arrestin‐mediated signaling pathways. This study revealed that β‐arrestin‐biased 5‐HT7R ligand induces slow, sustained Src activation, contrasting with transient G protein‐mediated activation.
Hyunbin Kim, Yong Woo Lee, Huimin Lee, Eunseo Park, Jieon Lee, Hae Nim Lee, Kyeong‐Man Kim, Hyunah Choo, Jihye Seong   +8 more
wiley   +1 more source

Journey of Oliceridine: A Novel Opioid

Journal of Marine Medical Society, 2022
Opioid analgesics play a crucial role in the management of acute pain, but its use is often limited by various adverse effects, especially nausea, vomiting, and respiratory depression.
A Tejus, Sharmila Sinha, Prafull Mohan, A G Mathur   +3 more
doaj   +1 more source

Novel drugs approved by the EMA, the FDA and the MHRA in 2025: A year in review

British Journal of Pharmacology, Volume 183, Issue 9, Page 1779-1813, May 2026.
Abstract In the 2025 novel drug mini‐review, one can take a full measure of the ingenuity that underlies current drug design and development, despite the year's smaller harvest (46 novel drugs) compared to 2024 (53) and 2023 (70). 54% of the novel drugs are first‐in‐class (FIC).
Andreas Papapetropoulos, Stavros Topouzis, Steve P. H. Alexander, Miriam M. Cortese‐Krott, Zsuzsanna Helyes, Kirill Martemyanov, Claudio Mauro, Nithyanandan Nagercoil, Reynold A. Panettieri Jr, Hemal H. Patel, Rainer Schulz, Barbara Stefanska, Gary J. Stephens, Nathalie Vergnolle, Xin Wang, Stephen Ward, Péter Ferdinandy   +16 more
wiley   +1 more source

CHARMM force-field parameters for morphine, heroin, and oliceridine, and conformational dynamics of opioid drugs

, 2021
Opioid drug binding to specialized G protein-coupled receptors (GPCRs) can lead to analgesia upon activation via downstream Gi protein signaling and to severe side effects via activation of the β-arrestin signaling pathway.
Hodošček, M., Hodošček, Milan, Domratcheva, T., Domratcheva, Tatiana, Lešnik, Samo, Bren, U., Lešnik, S., Bondar, A., Giannos, Thomas, Giannos, T., Bren, Urban, Bondar, Ana-Nicoleta   +11 more
core   +1 more source

Novel Ligands for the Orphan Receptor GPR151 Modulate Morphine Action

Genes to Cells, Volume 31, Issue 3, May 2026.
The new GPR151 ligands altered the analgesic effects of morphine. ABSTRACT GPR151 is an orphan G‐protein‐coupled receptor expressed on specific neurons. Its expression has been reported to be upregulated in the dorsal root ganglia in mouse nerve injury models, suggesting a role in pain transmission.
Hijiri Yoshida, Takashi Suto, Hiroyuki Hirano, Hiroyuki Osada, Kazuto Nunomura, Bangzhong Lin, Shigeru Saito, Shigeki Takeda   +7 more
wiley   +1 more source

Differences of Gradient Connectivity and Ventricle Volumes in Long‐Term Sensorineural Hearing Loss Related Cognitive Impairment Correlate With Transcriptional Signatures

Human Brain Mapping, Volume 47, Issue 5, 1 April 2026.
Long‐term hearing loss with cognitive decline shows altered brain gradients, enlarged choroid plexus, and ventricles. These are linked to transcriptomic changes in synaptic, metabolic, and neurodegenerative pathways. ABSTRACT Long‐term sensorineural hearing loss (SNHL) is a prevalent condition associated with an increased risk of cognitive impairment ...
Xiao‐Min Xu, Zi‐Huai Fang, Yuting Xia, Shuo Li, Yuan Feng, Yuanqing Wu, Richard Salvi, Xindao Yin, Yu‐Chen Chen   +8 more
wiley   +1 more source

Oliceridine for Analgesia in Elderly Patients Undergoing Kyphoplasty: From a Clinical Trial

Pain Research and Management, Volume 2026, Issue 1, 2026.
Background As a G protein‐biased μ‐opioid receptor agonist, oliceridine can offer a relatively effective and safe analgesia. However, its effect on patients suffering from kyphoplasty was unexplored. Aim This study was aimed to determine the median effective dose (ED50) of oliceridine for analgesia during kyphoplasty in elderly patients across ...
Chenfang Miao, Digui Weng, Chengzhao Liu, Qingqing Huang, Kongning Chen, Bin Zou, Harleen Khatra   +6 more
wiley   +1 more source