Results 21 to 30 of about 2,508,905 (426)

Adverse maternal environment alters Oprl1 variant expression in mouse hippocampus

The 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, Yingliu Huang, Qi Fu, Amber Majnik, Venkatesh Sampath, Robert H. Lane   +5 more
wiley   +1 more source

In Vitro Analyses of Spinach-Derived Opioid Peptides, Rubiscolins: Receptor Selectivity and Intracellular Activities through G Protein- and β-Arrestin-Mediated Pathways

Molecules, 2021
Activated opioid receptors transmit internal signals through two major pathways: the G-protein-mediated pathway, which exerts analgesia, and the β-arrestin-mediated pathway, which leads to unfavorable side effects. Hence, G-protein-biased opioid agonists
Yusuke Karasawa, Kanako Miyano, Hideaki Fujii, Takaaki Mizuguchi, Yui Kuroda, Miki Nonaka, Akane Komatsu, Kaori Ohshima, Masahiro Yamaguchi, Keisuke Yamaguchi, Masako Iseki, Yasuhito Uezono, Masakazu Hayashida   +12 more
doaj   +1 more source

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

Archiv 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, Andrea Angeli, Federico Ricci, Claudiu T. Supuran, Rosaria Gitto   +4 more
wiley   +1 more source

Computational Methods for Understanding the Selectivity and Signal Transduction Mechanism of Aminomethyl Tetrahydronaphthalene to Opioid Receptors

Molecules, 2022
Opioid receptors are members of the group of G protein-couple receptors, which have been proven to be effective targets for treating severe pain. The interactions between the opioid receptors and corresponding ligands and the receptor’s activation by ...
Peng Xie, Junjie Zhang, Baiyu Chen, Xinwei Li, Wenbo Zhang, Mengdan Zhu, Wei Li, Jianqi Li, Wei Fu   +8 more
doaj   +1 more source

Binding mode analyses of NAP derivatives as mu opioid receptor selective ligands through docking studies and molecular dynamics simulation [PDF]

, 2017
Mu opioid receptor selective antagonists are highly desirable because of their utility as pharmacological probes for receptor characterization and functional studies.
Wang, Huiqun, Zaidi, Saheem A., Zhang, Yan   +2 more
core   +2 more sources

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

Eur 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

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

Archiv 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, Antonio Laus, Maksims Vanejevs, Anastasija Ture, Rafaela Mostallino, Nicholas Pintori, Maria Antonietta De Luca, M. Paola Castelli, Gaetano Di Chiara   +8 more
wiley   +1 more source

Opioid Receptor-Mediated and Non-Opioid Receptor-Mediated Roles of Opioids in Tumour Growth and Metastasis

Frontiers in Oncology, 2021
Opioids are administered to cancer patients in the period surrounding tumour excision, and in the management of cancer-associated pain. The effects of opioids on tumour growth and metastasis, and their consequences on disease outcome, continue to be the ...
Claudia A. Scroope, Zane Singleton, Markus W. Hollmann, Marie-Odile Parat   +3 more
doaj   +1 more source

In vitro and in vivo pharmacological activities of 14-o-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice [PDF]

, 2018
Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Lattanzi, Roberta, Negri, Lucia, Rief, Silvia, Schmidhammer, Helmut, Spetea, Mariana.   +4 more
core   +2 more sources

Structure of the μ Opioid Receptor-Gi Protein Complex

Nature, 2018
The μ-opioid receptor (μOR) is a G-protein-coupled receptor (GPCR) and the target of most clinically and recreationally used opioids. The induced positive effects of analgesia and euphoria are mediated by μOR signalling through the adenylyl cyclase ...
A. Koehl, Hongli Hu, S. Maeda, Yan Zhang, Q. Qu, Joseph M. Paggi, Naomi R. Latorraca, D. Hilger, R. Dawson, H. Matile, G. Schertler, S. Granier, W. Weis, R. Dror, A. Manglik, G. Skiniotis, B. Kobilka   +16 more
semanticscholar   +1 more source