IUPHAR themed review: Opioid efficacy, bias, and selectivity
Drugs acting at the opioid receptor family are clinically used to treat chronic and acute pain, though they represent the second line of treatment behind GABA analogs, antidepressants and SSRI’s.
Nokomis Ramos-Gonzalez+2 more
doaj
Scalable Production of Highly-Sensitive Nanosensors Based on Graphene Functionalized with a Designed G Protein-Coupled Receptor [PDF]
We have developed a novel, all-electronic biosensor for opioids that consists of an engineered mu opioid receptor protein, with high binding affinity for opioids, chemically bonded to a graphene field-effect transistor to read out ligand binding.
Crook, Alexander+10 more
core +4 more sources
The clinical utility of conventional IV opioids is limited by the occurrence of opioid‐related adverse events. Oliceridine is a novel G protein–biased μ‐opioid receptor agonist designed to provide analgesia with an improved safety and tolerability ...
N. Singla+6 more
semanticscholar +1 more source
Modeling buprenorphine reduction of fentanyl-induced respiratory depression
BACKGROUND Potent synthetic opioids, such as fentanyl, are increasingly abused, resulting in unprecedented numbers of fatalities from respiratory depression.
Erik Olofsen+8 more
doaj +1 more source
The Potential of Methocinnamox as a Future Treatment for Opioid Use Disorder: A Narrative Review
The opioid epidemic is an ongoing public health crisis, and the United States health system is overwhelmed with increasing numbers of opioid-related overdoses.
Colleen G. Jordan+5 more
doaj +1 more source
Synthesis, biological evaluation, and SAR studies of 14β-phenylacetyl substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones derivatives : Ligands with mixed NOP and opioid receptor profile [PDF]
© 2018 Kumar, Polgar, Cami-Kobeci, Thomas, Khroyan, Toll and Husbands.A series of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydronoroxymorphinone compounds has been synthesized and evaluated for affinity and efficacy for mu (MOP), kappa (KOP), and ...
Cami-Kobeci+47 more
core +3 more sources
Attenuation of Antidepressant Effects of Ketamine by Opioid Receptor Antagonism.
OBJECTIVE: In addition to N-methyl-d-aspartate receptor antagonism, ketamine produces opioid system activation. The objective of this study was to determine whether opioid receptor antagonism prior to administration of intravenous ketamine attenuates its
N. Williams+10 more
semanticscholar +1 more source
Emotional Impairment and Persistent Upregulation of mGlu5 Receptor following Morphine Abstinence: Implications of an mGlu5-MOPr Interaction. [PDF]
BACKGROUND: A difficult problem in treating opioid addicts is the maintenance of a drug-free state because of the negative emotional symptoms associated with withdrawal, which may trigger relapse.
Bailey, A+8 more
core +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