Results 21 to 30 of about 2,447,948 (384)

Co-Evolution of Opioid and Adrenergic Ligands and Receptors: Shared, Complementary Modules Explain Evolution of Functional Interactions and Suggest Novel Engineering Possibilities

open access: yesLife, 2021
Cross-talk between opioid and adrenergic receptors is well-characterized and involves second messenger systems, the formation of receptor heterodimers, and the presence of extracellular allosteric binding regions for the complementary ligand; however ...
Robert Root-Bernstein, Beth Churchill
doaj   +1 more source

The Peptide PnPP-19, a Spider Toxin Derivative, Activates μ-Opioid Receptors and Modulates Calcium Channels

open access: yesToxins, 2018
The synthetic peptide PnPP-19 comprehends 19 amino acid residues and it represents part of the primary structure of the toxin δ-CNTX-Pn1c (PnTx2-6), isolated from the venom of the spider Phoneutria nigriventer.
Ana C. N. Freitas   +11 more
doaj   +1 more source

Pain relief devoid of opioid side effects following central action of a silylated neurotensin analog [PDF]

open access: yesEur J Pharmacol, 173174 (2020), 2020
Neurotensin (NT) exerts naloxone-insensitive antinociceptive action through its binding to both NTS1 and NTS2 receptors and NT analogs provide stronger pain relief than morphine on a molecular basis. Here, we examined the analgesic/adverse effect profile of a new NT(8-13) derivative denoted JMV2009, in which the Pro10 residue was substituted by a ...
arxiv   +1 more source

Adverse maternal environment alters Oprl1 variant expression in mouse hippocampus

open access: yesThe Anatomical Record, Volume 306, Issue 1, Page 162-175, January 2023., 2023
Abstract An adverse maternal environment (AME) and Western diet (WD) in early life predispose offspring toward cognitive impairment in humans and mice. Cognitive impairment associates with hippocampal dysfunction. An important regulator of hippocampal function is the hippocampal Nociceptin/Orphanin FQ (N/OFQ) system. Previous studies find links between
Xingrao Ke   +5 more
wiley   +1 more source

Phosphorylation-deficient G-protein-biased μ-opioid receptors improve analgesia and diminish tolerance but worsen opioid side effects

open access: yesNature Communications, 2019
Opioid analgesics are powerful pain relievers; however, over time, pain control diminishes as analgesic tolerance develops. The molecular mechanisms initiating tolerance have remained unresolved to date.
A. Kliewer   +8 more
semanticscholar   +1 more source

Structure‐guided identification of a selective sulfonamide‐based inhibitor targeting the human carbonic anhydrase VA isoform

open access: yesArchiv der Pharmazie, Volume 356, Issue 1, January 2023., 2023
Combining ligand‐based and structure‐based methodologies, the applied virtual screening approach identified a collection of sulfonamides targeting the human carbonic anhydrase (hCA) VA isoform. 2‐(3,4‐Dihydro‐2H‐quinolin‐1‐yl)‐N‐(4‐sulfamoylphenyl)acetamide was identified as a potent and selective lead compound as a candidate for further exploitation ...
Laura De Luca   +4 more
wiley   +1 more source

Expression and Localization of Opioid Receptors in Male Germ Cells and the Implication for Mouse Spermatogenesis. [PDF]

open access: yesPLoS ONE, 2016
The presence of endogenous opioid peptides in different testicular cell types has been extensively characterized and provides evidence for the participation of the opioid system in the regulation of testicular function.
Haizea Estomba   +6 more
doaj   +1 more source

Mechanistic Characterization of the Pharmacological Profile of HS-731, a Peripherally Acting Opioid Analgesic, at the µ-, δ-, κ-Opioid and Nociceptin Receptors

open access: yesMolecules, 2022
Accumulated preclinical and clinical data show that peripheral restricted opioids provide pain relief with reduced side effects. The peripherally acting opioid analgesic HS-731 is a potent dual μ-/δ-opioid receptor (MOR/DOR) full agonist, and a weak ...
Kristina Puls   +3 more
doaj   +1 more source

3‐[3‐(Phenalkylamino)cyclohexyl]phenols: Synthesis, biological activity, and in silico investigation of a naltrexone‐derived novel class of MOR‐antagonists

open access: yesArchiv der Pharmazie, Volume 356, Issue 1, January 2023., 2023
Based on a simplified version of the morphinan scaffold, 3‐[3‐(phenalkylamino)cyclohexyl]phenol analogues were designed, synthesized and evaluated for their µ‐opioid receptor (MOR) antagonist activity in vitro and in silico. Docking studies indicate a peculiar combination of C‐1 stereochemistry and N‐substitutions as feasibly essential for MOR‐ligand ...
Graziella Tocco   +8 more
wiley   +1 more source

The Role of Opioid Receptors in Immune System Function

open access: yesFrontiers in Immunology, 2019
Research on the effects of opioids on immune responses was stimulated in the 1980s by the intersection of use of intravenous heroin and HIV infection, to determine if opioids were enhancing HIV progression.
T. Eisenstein
semanticscholar   +1 more source

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