Results 91 to 100 of about 2,447,948 (384)
A lipidated peptide derived from the C-terminal tail of the vasopressin 2 receptor shows promise as a new $β$-arrestin inhibitor [PDF]
Pharmacological Research, 2025, 107597$\beta$-arrestins play pivotal roles in seven transmembrane receptor (7TMR) signalling and trafficking. To study their functional role in the regulation of specific receptor systems, current research relies mainly on genetic tools, as few pharmacological options are available.
arxiv +1 more source
Better agonist for the opioid receptors [PDF]
Chemistry Central Journal, 2018 This commentary highlights the recent work published in journal Nature on the structural based discovery of novel analgesic compounds for opioid receptors with minimal effects. Manglik et al. selectively targeted the Gi based μOR pathway instead of the β-arrestin pathway of the opioids. The computational screening of millions of compounds showed a list
Syed Lal Badshah +3 more
openaire +3 more sources
Structure and dynamics of dynorphin peptide and its receptor [PDF]
arXiv, 2019 Dynorphin is a neuropeptide involved in pain, addiction and mood regulation. It exerts its activity by binding to the kappa opioid receptor (KOP) which belongs to the large family of G-protein coupled receptors. The dynorphin peptide was discovered in 1975, while its receptor was cloned in 1993.
arxiv
Individualized Risk Assessment of Preoperative Opioid Use by Interpretable Neural Network Regression [PDF]
arXiv, 2022 Preoperative opioid use has been reported to be associated with higher preoperative opioid demand, worse postoperative outcomes, and increased postoperative healthcare utilization and expenditures. Understanding the risk of preoperative opioid use helps establish patient-centered pain management.
arxiv
Opioid system is necessary but not sufficient for antidepressive actions of ketamine in rodents
Proceedings of the National Academy of Sciences of the United States of America, 2020 Significance Ketamine, an NMDA receptor antagonist, has generated intense excitement as a therapy for treatment-resistant depression. However, ketamine and its metabolites can act on a wide range of targets, including opioid receptors, which has raised ...
Matthew E. Klein +3 more
semanticscholar +1 more source
Production Of 11C‐Labeled Amides Via “In‐Loop” 11C‐Carbonylation
Asian Journal of Organic Chemistry, EarlyView.The current work utilizes carbon‐11 labelled aroyl dimethylaminopyridinium salts in a two‐step in‐loop carbonylative cross‐coupling reaction of aryl halides with [¹¹C]CO yielding a diverse range of carbon‐11 labelled primary benzamides with good to excellent yields.
Tanpreet Kaur +3 more
wiley +1 more source
Annals of Medicine, 1995 Recent experimental and clinical research has demonstrated that opioids can produce potent and receptor-specific analgesic effects outside the central nervous system. Opioid receptors are localized on peripheral terminals of sensory nerves and their endogenous ligands, opioid peptides, have been discovered in immune cells within inflamed tissue.
Michael Schäfer +2 more
openaire +3 more sources
Machine Learning Harnesses Molecular Dynamics to Discover New $μ$ Opioid Chemotypes [PDF]
arXiv, 2018 Computational chemists typically assay drug candidates by virtually screening compounds against crystal structures of a protein despite the fact that some targets, like the $\mu$ Opioid Receptor and other members of the GPCR family, traverse many non-crystallographic states.
arxiv
Five Decades of Research on Opioid Peptides: Current Knowledge and Unanswered Questions
Molecular Pharmacology, 2020 In the mid-1970s, an intense race to identify endogenous substances that activated the same receptors as opiates resulted in the identification of the first endogenous opioid peptides.
L. Fricker +3 more
semanticscholar +1 more source
Animal Models and Experimental Medicine, EarlyView.Neuropathic pain management via repeated electroacupuncture. Abstract Background Existing remedial approaches for relieving neuropathic pain (NPP) are challenging and open the way for alternative therapeutic measures such as electroacupuncture (EA). The mechanism underlying the antinociceptive effects of repeated EA sessions, particularly concerning ...
Faisal Ayub Kiani +6 more
wiley +1 more source