keyword
MENU ▼
Read by QxMD icon Read
search

Nociceptin

keyword
https://www.readbyqxmd.com/read/29753041/nociceptin-orphanin-fq-opioid-peptide-nop-receptor-and-%C3%A2%C2%B5-opioid-peptide-mop-receptors-both-contribute-to-the-anti-hypersensitive-effect-of-cebranopadol-in-a-rat-model-of-arthritic-pain
#1
Klaus Schiene, Wolfgang Schröder, Klaus Linz, Stefanie Frosch, Thomas M Tzschentke, Ulla Jansen, Thomas Christoph
Cebranopadol is a novel, first-in-class analgesic with agonist activity at the nociceptin/orphanin FQ opioid peptide (NOP) receptor as well as the classical opioid peptide receptors. This study investigated the anti-hypersensitive effect of cebranopadol in a rat model of arthritic pain. Selective antagonists were used to probe the involvement of the NOP receptor and the µ-opioid peptide (MOP) receptors. Experimental mono-arthritis was induced by intra-articular injection of complete Freund's adjuvant into the left hind knee joint...
May 9, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29738766/development-of-a-novel-photoaffinity-probe-for-labeling-nocistatin-receptor
#2
Masashi Harada, Toshiaki Minami, Seiji Ito, Emiko Okuda-Ashitaka
Nocistatin (NST) is a neuropeptide produced from the same precursor protein of opioid peptide nociceptin/orphanin FQ (N/OFQ), and it is involved in a broad range of central functions including pain transmission in the nervous system. However, the composition and structure of the receptor(s) for NST remain unclear. Here, we developed NST photoaffinity probe to identify NST-binding receptor. The NST photoaffinity probe contains an azide moiety for the tagging of the binding protein as well as biotin for protein detection...
May 5, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29705547/nociceptin-orphanin-fq-receptors-modulate-the-discriminative-stimulus-effects-of-oxycodone-in-c57bl-6-mice
#3
D Matthew Walentiny, Jason M Wiebelhaus, Patrick M Beardsley
BACKGROUND: Nociceptin/orphanin FQ (NOP) receptor ligands have shown efficacy as putative analgesics and can modulate the abuse-related effects of opioids, suggesting therapeutic applications. The discriminative stimulus effects of a drug are related to their subjective effects, a predictor of abuse potential. To determine whether activation of NOP receptors could alter the subjective effects of an abused opioid analgesic, a novel oxycodone discrimination was established in mice, characterized with positive and negative controls, and its expression evaluated with a NOP receptor agonist...
April 15, 2018: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29678771/prenatal-ethanol-induces-an-anxiety-phenotype-and-alters-expression-of-dynorphin-nociceptin-orphanin-fq-genes
#4
Aranza Wille-Bille, Roberto Sebastián Miranda-Morales, Mariangela Pucci, Fabio Bellia, Claudio D'Addario, Ricardo Marcos Pautassi
Animal models have suggested that prenatal ethanol exposure (PEE) alters the κ opioid receptor system. The present study investigated the brain expression of dynorphin and nociceptin/orphanin FQ related genes and assessed anxiety-like behavior in the light-dark box (LDB), shelter-seeking and risk-taking behaviors in the concentric square field (CSF) test, and ethanol-induced locomotion in the open field (OF), in infant or adolescent Wistar rats that were exposed to PEE (0.0 or 2.0 g/kg, intragastrically, gestational days 17-20)...
April 17, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29615517/the-nociceptin-receptor-inhibits-axonal-regeneration-and-recovery-from-spinal-cord-injury
#5
Yuichi Sekine, Chad S Siegel, Tomoko Sekine-Konno, William B J Cafferty, Stephen M Strittmatter
Axonal growth after traumatic spinal cord injury is limited by endogenous inhibitors, selective blockade of which promotes partial neurological recovery. The partial repair phenotypes suggest that compensatory pathways limit improvement. Gene expression profiles of mice deficient in Ngr1 , which encodes a receptor for myelin-associated inhibitors of axonal regeneration such as Nogo, revealed that trauma increased the mRNA expression of ORL1 , which encodes the receptor for the opioid-related peptide nociceptin...
April 3, 2018: Science Signaling
https://www.readbyqxmd.com/read/29582417/dissecting-the-spinal-nop-receptor-distribution-under-a-chronic-pain-model-using-nop-egfp-knock-in-mice
#6
Akihiko Ozawa, Gloria Brunori, Andrea Cippitelli, Nicholas Toll, Jennifer Schoch, Brigitte L Kieffer, Lawrence Toll
BACKGROUND AND PURPOSE: The Nociceptin/orphanin FQ Opioid Peptide (NOP) receptor system plays a significant role in the regulation of pain, and functions differently in the spinal cord and brain. The mechanism by which the NOP receptor agonists regulate pain transmission in these regions is not clearly understood. Here we investigate the peripheral and spinal NOP receptor distribution and antinociceptive effects of intrathecally (i.t) administered nociceptin/orphanin FQ (N/OFQ) under chronic neuropathic pain state...
March 26, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29470146/towards-an-effective-peripheral-visceral-analgesic-responding-to-the-national-opioid-crisis
#7
Michael Camilleri
This is an editorial summarizing recent new developments in visceral analgesics. This promising field is important as a new approach to address abdominal pain with peripheral visceral analgesics is considered a key approach to addressing the current opioid crisis. Some of the novel compounds address peripheral pain mechanisms through modulation of opioid receptors through biased ligands, nociceptin/orphanin FQ opioid peptide (NOP) receptor or dual action on NOP and μ-opioid receptor, buprenorphine and morphiceptin analogs...
February 22, 2018: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/29391391/a-systematic-review-of-the-role-of-the-nociceptin-receptor-system-in-stress-cognition-and-reward-relevance-to-schizophrenia
#8
REVIEW
Muhammad Saad Khan, Isabelle Boileau, Nathan Kolla, Romina Mizrahi
Schizophrenia is a debilitating neuropsychiatric illness that is characterized by positive, negative, and cognitive symptoms. Research over the past two decades suggests that the nociceptin receptor system may be involved in domains affected in schizophrenia, based on evidence aligning it with hallmark features of the disorder. First, aberrant glutamatergic and striatal dopaminergic function are associated with psychotic symptoms, and the nociceptin receptor system has been shown to regulate dopamine and glutamate transmission...
February 2, 2018: Translational Psychiatry
https://www.readbyqxmd.com/read/29378191/involvement-of-the-n-ofq-nop-system-in-rat-morphine-antinociceptive-tolerance-are-astrocytes-the-crossroad
#9
Laura Micheli, Elena Lucarini, Francesca Corti, Roberto Ciccocioppo, Girolamo Calò, Anna Rizzi, Carla Ghelardini, Lorenzo Di Cesare Mannelli
The development of tolerance to the antinociceptive effect is a main problem associated with the repeated administration of opioids. The progressively higher doses required to relieve pain reduce safety and exacerbate the side effects of classical opioid receptor agonists like morphine. Nociceptin/orphanin FQ (N/OFQ) and its NOP receptor constitute the fourth endogenous opioid system that is involved in the control of broad spectrum of biological functions, including pain transmission. Aim of this work was to evaluate the relevance of the N/OFQ-NOP system in morphine antinociceptive action and in the development of morphine tolerance in the rat...
March 15, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29340866/-in-silico-study-of-the-binding-of-two-novel-antagonists-to-the-nociceptin-receptor
#10
Stefano Della Longa, Alessandro Arcovito
Antagonists of the nociceptin receptor (NOP) are raising interest for their possible clinical use as antidepressant drugs. Recently, the structure of NOP in complex with some piperidine-based antagonists has been revealed by X-ray crystallography. In this study, a multi-flexible docking (MF-docking) procedure, i.e. docking to multiple receptor conformations extracted by preliminary molecular dynamics trajectories, together with hybrid quantum mechanics/molecular mechanics (QM/MM) simulations have been carried out to provide the binding mode of two novel NOP antagonists, one of them selective (BTRX-246040, formerly named LY-2940094) and one non selective (AT-076), i...
January 16, 2018: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/29332567/nociceptin-orphanin-fq-peptide-nop-receptor-modulators-an-update-in-structure-activity-relationships
#11
Carlo Mustazza, Stefano Pieretti, Francesca Marzoli
Nociceptin /Orphanin FQ Peptide" receptor (NOPr) is a G-protein-coupled receptor with the nociceptin/orphanin FQ peptide (N/OFQ) as endogenous agonist. It is expressed in the nervous system as well as in some non-neural tissues. Its activation has pronociceptive effect at the supraspinal level, whereas at the spinal level it produces nociceptive effects at low doses and antinociceptive effects at higher doses. NOPr is also involved in mood and blood pressure regulation, immunoregulation, airway constriction, feeding, urination, bowel motility, learning and memory...
January 10, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29316911/the-standardized-withania-somnifera-dunal-root-extract-alters-basal-and-morphine-induced-opioid-receptor-gene-expression-changes-in-neuroblastoma-cells
#12
Francesca Felicia Caputi, Elio Acquas, Sanjay Kasture, Stefania Ruiu, Sanzio Candeletti, Patrizia Romualdi
BACKGROUND: Behavioral studies demonstrated that the administration of Withania somnifera Dunal roots extract (WSE), prolongs morphine-elicited analgesia and reduces the development of tolerance to the morphine's analgesic effect; however, little is known about the underpinning molecular mechanism(s). In order to shed light on this issue in the present paper we explored whether WSE promotes alterations of μ (MOP) and nociceptin (NOP) opioid receptors gene expression in neuroblastoma SH-SY5Y cells...
January 10, 2018: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29233847/pharmacologic-evidence-for-a-putative-conserved-allosteric-site-on-opioid-receptors
#13
Kathryn E Livingston, M Alexander Stanczyk, Neil T Burford, Andrew Alt, Meritxell Canals, John R Traynor
Allosteric modulators of G protein-coupled receptors, including opioid receptors, have been proposed as possible therapeutic agents with enhanced selectivity. BMS-986122 is a positive allosteric modulator (PAM) of the μ -opioid receptor ( µ -OR). BMS-986187 is a structurally distinct PAM for the δ -opioid receptor ( δ -OR) that has been reported to exhibit 100-fold selectivity in promoting δ -OR over μ -OR agonism. We used ligand binding and second-messenger assays to show that BMS-986187 is an effective PAM at the μ -OR and at the κ -opioid receptor ( κ -OR), but it is ineffective at the nociceptin receptor...
February 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29232769/anti-parkinsonian-and-anti-dyskinetic-profiles-of-two-novel-potent-and-selective-nociceptin-orphanin-fq-receptor-agonists
#14
Ludovico Arcuri, Salvatore Novello, Martina Frassineti, Daniela Mercatelli, Clarissa Anna Pisanò, Ilaria Morella, Stefania Fasano, Blair V Journigan, Michael E Meyer, Willma E Polgar, Riccardo Brambilla, Nurulain T Zaveri, Michele Morari
BACKGROUND AND PURPOSE: We previously showed that nociceptin/orphanin FQ opioid peptide (NOP) receptor agonists attenuate the expression of levodopa-induced dyskinesia in animal models of Parkinson's disease. We now investigate the efficacy of two novel, potent and chemically distinct NOP receptor agonists, AT-390 and AT-403, to improve Parkinsonian disabilities and attenuate dyskinesia development and expression. EXPERIMENTAL APPROACH: Binding affinity and functional efficacy of AT-390 and AT-403 at the opioid receptors were determined in radioligand displacement assays and in GTPγS binding assays respectively, conducted in CHO cells...
March 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29231765/imaging-corticotropin-releasing-factor-and-nociceptin-in-addiction-and-ptsd-models
#15
Savannah Tollefson, Michael Himes, Rajesh Narendran
Addiction is composed of three phases: intoxication, withdrawal, and craving. Negative reinforcement, strengthening a behaviour by removing an aversive stimulus, has been associated with the withdrawal phase. An imbalance of neurotransmitters within the brain's stress (nociceptin, neuropeptide Y) and anti-stress (CRF, norepinephrine, etc.) system is attributed to negatively reinforced compulsive behaviours associated with relapse. Similarly, post-traumatic stress disorder is characterized by an overactive stress system...
December 2017: International Review of Psychiatry
https://www.readbyqxmd.com/read/29215139/a-novel-and-selective-nociceptin-receptor-nop-agonist-1-1-cis-4-isopropylcyclohexyl-piperidin-4-yl-1h-indol-2-yl-methanol-at-312-decreases-acquisition-of-ethanol-induced-conditioned-place-preference-in-mice
#16
Nurulain T Zaveri, Paul V Marquez, Michael E Meyer, Willma E Polgar, Abdul Hamid, Kabirullah Lutfy
BACKGROUND: Nociceptin/orphanin FQ, the endogenous peptide agonist for the opioid receptor-like receptor (also known as NOP or the nociceptin receptor), has been shown to block the acquisition and expression of ethanol (EtOH)-induced conditioned place preference (CPP). Here, we report the characterization of a novel small-molecule NOP ligand AT-312 (1-(1-((cis)-4-isopropylcyclohexyl)piperidin-4-yl)-1H-indol-2-yl)methanol) in receptor binding and GTPγS functional assays in vitro. We then investigated the effect of AT-312 on the rewarding action of EtOH in mice using the CPP paradigm...
February 2018: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29197086/methylation-of-oprl1-mediates-the-effect-of-psychosocial-stress-on-binge-drinking-in-adolescents
#17
Barbara Ruggeri, Christine Macare, Serena Stopponi, Tianye Jia, Fabiana M Carvalho, Gabriel Robert, Tobias Banaschewski, Arun L W Bokde, Uli Bromberg, Christian Büchel, Anna Cattrell, Patricia J Conrod, Sylvane Desrivières, Herta Flor, Vincent Frouin, Jürgen Gallinat, Hugh Garavan, Penny Gowland, Andreas Heinz, Bernd Ittermann, Jean Luc Martinot, Marie-Laure Paillère Martinot, Frauke Nees, Dimitri Papadopoulos-Orfanos, Tomáš Paus, Luise Poustka, Michael N Smolka, Nora C Vetter, Henrik Walter, Robert Whelan, Wolfgang H Sommer, Georgy Bakalkin, Roberto Ciccocioppo, Gunter Schumann
BACKGROUND: Nociceptin is a key regulator linking environmental stress and alcohol drinking. In a genome-wide methylation analysis, we recently identified an association of a methylated region in the OPRL1 gene with alcohol-use disorders. METHODS: Here, we investigate the biological basis of this observation by analysing psychosocial stressors, methylation of the OPRL1 gene, brain response during reward anticipation and alcohol drinking in 660 fourteen-year-old adolescents of the IMAGEN study...
December 2, 2017: Journal of Child Psychology and Psychiatry, and Allied Disciplines
https://www.readbyqxmd.com/read/29180970/cebranopadol-a-mixed-opioid-agonist-reduces-cocaine-self-administration-through-nociceptin-opioid-and-mu-opioid-receptors
#18
Qianwei Shen, Yulin Deng, Roberto Ciccocioppo, Nazzareno Cannella
Cocaine addiction is a widespread psychiatric condition still waiting for approved efficacious medications. Previous studies suggested that simultaneous activation of nociceptin opioid (NOP) and mu opioid (MOP) receptors could be a successful strategy to treat cocaine addiction, but the paucity of molecules co-activating both receptors with comparable potency has hampered this line of research. Cebranopadol is a non-selective opioid agonist that at nanomolar concentration activates both NOP and MOP receptors and that recently reached phase-III clinical trials for cancer pain treatment...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29155273/mu-opioid-peptide-mop-and-nociceptin-orphanin-fq-peptide-nop-receptor-activation-both-contribute-to-the-discriminative-stimulus-properties-of-cebranopadol-in-the-rat
#19
Thomas M Tzschentke, Kris Rutten
The novel potent analgesic cebranopadol is an agonist at nociceptin/orphanin FQ peptide (NOP) and classical opioid receptors, with the highest in-vitro activity at NOP and mu-opioid peptide (MOP) receptors, and somewhat lower activity at kappa-opioid peptide (KOP) and delta-opioid peptide (DOP) receptors. We addressed the question of which of these pharmacological activities contribute to the stimulus properties of cebranopadol using a rat drug discrimination procedure. First, cebranopadol was tested in generalization tests against a morphine cue, including receptor-specific antagonism...
February 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29102248/nociceptin-and-the-nop-receptor-in-aversive-learning-in-mice
#20
Abdu Adem, Nather Madjid, Ulrika Kahl, Sarah Holst, Bassem Sadek, Johan Sandin, Lars Terenius, Sven Ove Ögren
The endogenous neuropeptide nociceptin (N/OFQ), which mediates its actions via the nociceptin receptor (NOP), is implicated in multiple behavioural and physiological functions. This study examined the effects of the NOP agonists N/OFQ and the synthetic agonist Ro 64-6198, the antagonists NNN and NalBzoH, as well as deletion of the Pronociceptin gene on emotional memory in mice. The animals were tested in the passive avoidance (PA) task, dependent on hippocampal and amygdala functions. N/OFQ injected intraventricularly (i...
December 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
keyword
keyword
69868
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"