Results 21 to 30 of about 55,107 (272)
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
Patterns of Routes of Administration and Drug Tampering for Nonmedical Opioid Consumption: Data Mining and Content Analysis of Reddit Discussions [PDF]
The complex unfolding of the US opioid epidemic in the last 20 years has been the subject of a large body of medical and pharmacological research, and it has sparked a multidisciplinary discussion on how to implement interventions and policies to effectively control its impact on public health.
arxiv +1 more source
Buprenorphine is a Schedule III opioid analgesic with unique pharmacodynamic and pharmacokinetic properties that may be preferable to those of Schedule II full μ-opioid receptor agonists.
Jeffrey Gudin, Jeffrey Fudin
doaj +1 more source
Receptors for morphine and opioids
Two points concerning enzymatic systems acting on disposal of morphine are discussed, namely the multiplicity of glucuronyltransferase and the effect of nalorphine on N-demethylation of morphine. Evidences of the presence of at least two different glucuronyltransferases in microsomes of rat liver, kidney and intestine are presented. These evidences are
Sánchez, Emílio+2 more
openaire +4 more sources
Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors
Background The aim of the present study was to characterize the activation profiles of 15 opioid ligands in transfected human embryonic kidney cells expressing only δ opioid receptors.
Clark J+3 more
doaj +1 more source
Historical Review: Opiate Addiction and Opioid Receptors
Substance use disorders (SUDs), defined as a collection of symptoms including tolerance and withdrawal, are chronic illnesses characterized by relapse and remission. In the United States, billions of dollars have been lost due to SUDs.
Shaocheng Wang
doaj +1 more source
The Use of Computational Approaches in the Discovery and Mechanism Study of Opioid Analgesics
Opioid receptors that belong to class A G protein-coupled receptors (GPCRs) are vital in pain control. In the past few years, published high-resolution crystal structures of opioid receptor laid a solid basis for both experimental and computational ...
Bangyi Zhao, Wei Li, Lijie Sun, Wei Fu
doaj +1 more source
The opioid receptor: emergence through millennia of pharmaceutical sciences
Throughout history humanity has searched for an optimal approach to the use of opioids that maximizes analgesia while minimizing side effects. This review reflects upon the conceptualization of the opioid receptor and the critical role that the ...
Carolyn A. Fairbanks+4 more
doaj +1 more source
Machine-learning Analysis of Opioid Use Disorder Informed by MOR, DOR, KOR, NOR and ZOR-Based Interactome Networks [PDF]
Opioid use disorder (OUD) continuously poses major public health challenges and social implications worldwide with dramatic rise of opioid dependence leading to potential abuse. Despite that a few pharmacological agents have been approved for OUD treatment, the efficacy of said agents for OUD requires further improvement in order to provide safer and ...
arxiv