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NOP Receptor

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https://www.readbyqxmd.com/read/27871910/pharmacological-studies-on-the-nop-and-opioid-receptor-agonist-pwt2-dmt-1-n-ofq-1-13
#1
Maria Camilla Cerlesi, Huiping Ding, Mark F Bird, Norikazu Kiguchi, Federica Ferrari, Davide Malfacini, Anna Rizzi, Chiara Ruzza, David G Lambert, Mei-Chuan Ko, Girolamo Calo, Remo Guerrini
An innovative chemical strategy named peptide welding technology (PWT) has been developed for the facile synthesis of tetrabranched peptides. [Dmt(1)]N/OFQ(1-13)-NH2 acts as a universal agonist for nociceptin/orphanin FQ (N/OFQ) and classical opioid receptors. The present study investigated the pharmacological profile of the PWT derivative of [Dmt(1)]N/OFQ(1-13)NH2 (PWT2-[Dmt(1)]) in several assays in vitro and in vivo after spinal administration in monkeys subjected to the tail withdrawal assay. PWT2-[Dmt(1)] mimicked the effects of [Dmt(1)]N/OFQ(1-13)-NH2 displaying full agonist activity, similar affinity/potency and selectivity at human recombinant N/OFQ (NOP) and opioid receptors in receptor binding, stimulation of [(35)S]GTPγS binding, calcium mobilization in cells expressing chimeric G proteins, and BRET studies for measuring receptor/G-protein and receptor/β-arrestin 2 interaction...
November 19, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27793733/post-blast-treatment-with-nociceptin-orphanin-fq-peptide-nop-receptor-antagonist-reduces-brain-injury-induced-hypoxia-and-signaling-proteins-in-vestibulomotor-related-brain-regions
#2
Hibah O Awwad, Cindy D Durand, Larry P Gonzalez, Paul Tompkins, Yong Zhang, Megan R Lerner, Daniel J Brackett, David M Sherry, Vibhudutta Awasthi, Kelly M Standifer
Mild traumatic brain injury (mTBI) diagnoses have increased due to aggressive sports and blast-related injuries, but the cellular mechanisms and pathology underlying mTBI are not completely understood. Previous reports indicate that Nociceptin Orphanin/FQ (N/OFQ), an endogenous neuropeptide, contributes to post-injury ischemia following mechanical brain injury, yet its specific role in cerebral hypoxia, vestibulomotor function and injury marker expression following blast-induced TBI is not known. This study is the first to identify a direct association of N/OFQ and its N/OFQ peptide (NOP) receptor with TBI-induced changes following a single 80psi head blast exposure in male rats...
October 25, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27780725/in-vitro-functional-characterization-of-novel-nociceptin-orphanin-fq-receptor-agonists-in-recombinant-and-native-preparations
#3
Federica Ferrari, Maria Camilla Cerlesi, Davide Malfacini, Laila Asth, Elaine C Gavioli, Velvet B Journigan, Uma G Kamakolanu, Michael E Meyer, Dennis Yasuda, Willma E Polgar, Anna Rizzi, Remo Guerrini, Chiara Ruzza, Nurulain T Zaveri, Girolamo Calo
Nociceptin/Orphanin FQ (N/OFQ) regulates several biological functions via selective activation of the N/OFQ receptor (NOP). In this study novel nonpeptide NOP ligands were characterized in vitro in receptor binding and [(35)S]GTPγS stimulated binding in membranes of cells expressing human NOP and classical opioid receptors, calcium mobilization assay in cells coexpressing the receptors and chimeric G proteins, bioluminescence resonance energy transfer (BRET) based assay for studying NOP receptor interaction with G protein and arrestin, the electrically stimulated mouse vas deferens and the mouse colon bioassays...
October 22, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27778406/cebranopadol-novel-dual-opioid-nop-receptor-agonist-analgesic
#4
R B Raffa, G Burdge, J Gambrah, H E Kinecki, F Lin, B Lu, J T Nguyen, V Phan, A Ruan, M A Sesay, T N Watkins
WHAT IS KNOWN AND OBJECTIVE: Chronic pain presents a difficult clinical challenge because of the limited efficacy, the limiting adverse-effect profile or the abuse potential of current analgesic options. Cebranopadol is a novel new agent in clinical trials that combines dual agonist action at opioid and nociceptin/orphanin FQ peptide (NOP) receptors. It is the first truly unique, centrally acting analgesic in several years. We here review the basic and clinical pharmacology of cebranopadol...
October 24, 2016: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/27751964/altered-expression-of-glial-markers-chemokines-and-opioid-receptors-in-the-spinal-cord-of-type-2-diabetic-monkeys
#5
Norikazu Kiguchi, Huiping Ding, Christopher M Peters, Nancy D Kock, Shiroh Kishioka, J Mark Cline, Janice D Wagner, Mei-Chuan Ko
Neuroinflammation is a pathological condition that underlies diabetes and affects sensory processing. Given the high prevalence of pain in diabetic patients and crosstalk between chemokines and opioids, it is pivotal to know whether neuroinflammation-associated mediators are dysregulated in the central nervous system of diabetic primates. Therefore, the aim of this study was to investigate whether mRNA expression levels of glial markers, chemokines, and opioid receptors are altered in the spinal cord and thalamus of naturally occurring type 2 diabetic monkeys (n=7) compared with age-matched non-diabetic monkeys (n=6)...
October 14, 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27667485/functional-pharmacological-characterisation-of-ser100-in-cardiovascular-health-and-disease
#6
Inmaculada C Villar, Kristen J Bubb, Amie J Moyes, Eva Steiness, Trygve Gulbrandsen, Finn Olav Levy, Adrian J Hobbs
BACKGROUND AND PURPOSE: SER100 is a selective nociceptin receptor (NOP) agonist with sodium-potassium-sparing aquaretic and anti-natriuretic activity. This study was designed to characterize the functional cardiovascular pharmacology of SER100 in vitro and in vivo, including experimental models of cardiovascular disease. EXPERIMENTAL APPROACH: Haemodynamic, ECG parameters and heart rate variability (HRV) were determined using radiotelemetry in healthy, conscious mice...
September 25, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27573832/a-novel-orvinol-analog-bu08028-as-a-safe-opioid-analgesic-without-abuse-liability-in-primates
#7
Huiping Ding, Paul W Czoty, Norikazu Kiguchi, Gerta Cami-Kobeci, Devki D Sukhtankar, Michael A Nader, Stephen M Husbands, Mei-Chuan Ko
Despite the critical need, no previous research has substantiated safe opioid analgesics without abuse liability in primates. Recent advances in medicinal chemistry have led to the development of ligands with mixed mu opioid peptide (MOP)/nociceptin-orphanin FQ peptide (NOP) receptor agonist activity to achieve this objective. BU08028 is a novel orvinol analog that displays a similar binding profile to buprenorphine with improved affinity and efficacy at NOP receptors. The aim of this preclinical study was to establish the functional profile of BU08028 in monkeys using clinically used MOP receptor agonists for side-by-side comparisons in various well-honed behavioral and physiological assays...
September 13, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27562660/nociceptin-reduces-the-inflammatory-immune-microenvironment-in-a-conventional-murine-model-of-airway-hyperresponsiveness
#8
G Spaziano, R Sorrentino, M Matteis, G Malgieri, M Sgambato, T P Russo, M Terlizzi, F Roviezzo, F Rossi, A Pinto, R Fattorusso, B D'Agostino
BACKGROUND: Nociceptin/orphanin FQ (N/OFQ) and its receptor (NOP) are involved in airway hyperresponsiveness (AHR) and inflammation. However, the role of nociceptin at modulating the inflammatory immune microenvironment in asthma is still unclear. OBJECTIVE: To understand the role of N/OFQ in the regulation of a Th2-like environment, we used a conventional murine model of AHR. METHODS: Balb/c and CD1 mice were sensitized to ovalbumin (OVA) and treated with saline solution or N/OFQ, at days 0 and 7...
October 5, 2016: Clinical and Experimental Allergy: Journal of the British Society for Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/27562376/genetic-deletion-of-the-nociceptin-orphanin-fq-receptor-in-the-rat-confers-resilience-to-the-development-of-drug-addiction
#9
Marsida Kallupi, Giulia Scuppa, Giordano de Guglielmo, Girolamo Calò, Friedbert Weiss, Michael A Statnick, Linda M Rorick-Kehn, Roberto Ciccocioppo
The nociceptin (NOP) receptor is a G-protein-coupled receptor whose natural ligand is the nociceptin/orphanin FQ (N/OFQ) peptide. Evidence from pharmacological studies suggests that the N/OFQ system is implicated in the regulation of several addiction-related phenomena, such as drug intake, withdrawal and relapse. Here, to further explore the role of NOP system in addiction, we used NOP (-/-) rats to study the motivation for cocaine, heroin and alcohol self-administration in the absence of N/OFQ function. Conditioned place preference (CPP) and saccharin (0...
August 26, 2016: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27515665/the-nociceptin-orphanin-fq-receptor-agonist-sr-8993-as-a-candidate-therapeutic-for-alcohol-use-disorders-validation-in-rat-models
#10
Abdul Maruf Asif Aziz, Shaun Brothers, Gregory Sartor, Lovisa Holm, Markus Heilig, Claes Wahlestedt, Annika Thorsell
RATIONALE: Alcoholism is a complex disorder in which diverse pathophysiological processes contribute to initiation and progression, resulting in a high degree of heterogeneity among patients. Few pharmacotherapies are presently available, and patient responses to these are variable. The nociceptin/orphanin FQ (NOP) receptor has been suggested to play a role both in alcohol reward and in negatively reinforced alcohol seeking. Previous studies have shown that NOP-receptor activation reduces alcohol intake in genetically selected alcohol-preferring as well as alcohol-dependent rats...
October 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27371029/changes-in-nociceptin-orphanin-fq-levels-in-rat-brain-regions-after-acute-and-chronic-cannabinoid-treatment-in-conjunction-with-the-development-of-antinociceptive-tolerance
#11
Ahmet Ulugol, Ruhan D Topuz, Ozgur Gunduz, Gulnur Kizilay, Hakan C Karadag
It has been indicated that acute and chronic morphine administrations enhance nociceptin/orphanin FQ (N/OFQ) levels in the brain, which might play role in the development of tolerance to the antinociceptive effect of morphine. Accordingly, N/OFQ receptor (NOP) antagonists have been shown to prevent the development of antinociceptive tolerance to morphine. Our aim is to observe whether cannabinoids, similarly to opioids, enhance N/OFQ levels in pain-related brain regions and whether antagonism of NOP receptors attenuates the development of tolerance to the antinociceptive effect of cannabinoids...
December 2016: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27353045/occupancy-of-nociceptin-orphanin-fq-peptide-receptors-by-the-antagonist-ly2940094-in-rats-and-healthy-human-subjects
#12
Eyas Raddad, Amy Chappell, Jeffery Meyer, Alan Wilson, Charles E Ruegg, Johannes Tauscher, Michael A Statnick, Vanessa Barth, Xin Zhang, Steven J Verfaille
Therapeutic benefits from nociceptin opioid peptide receptor (NOP) antagonism were proposed for obesity, eating disorders, and depression. LY2940094 ([2-[4-[(2-chloro-4,4-difluoro-spiro[5H-thieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)methyl]-3-methyl-pyrazol-1-yl]-3-pyridyl]methanol) is a novel, orally bioavailable, potent, and selective NOP antagonist. We studied NOP receptor occupancy (RO) after single oral LY2940094 doses in rat hypothalamus and human brain by use of liquid chromatography with tandem mass spectrometry (LC-MS/MS) (LSN2810397) and positron emission tomography (PET) ([(11)C]NOP-1A) tracers, respectively...
September 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27321161/intra-perirhinal-cortex-administration-of-estradiol-but-not-an-er%C3%AE-agonist-modulates-object-recognition-memory-in-ovariectomized-rats
#13
Nicole J Gervais, Laurie M Hamel, Wayne G Brake, Dave G Mumby
Intra-rhinal cortical infusion of 17-β estradiol (E2, 244.8pg/μl) enhances performance on the Novel-Object Preference (NOP) test and impairs accuracy on the delayed nonmatching-to-sample (DNMS) task in the same set of ovariectomized rats (Gervais, Jacob, Brake, & Mumby, 2013). These results appear paradoxical, as normal performance on both tests require intact object-recognition memory (ORM) ability. While demonstrating a preference for the novel object requires recognizing the sample object, rodents can recognize the sample object and still fail to demonstrate a preference...
September 2016: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/27272042/characterisation-of-the-novel-mixed-mu-nop-peptide-ligand-dermorphin-n-ofq-deno
#14
Mark F Bird, Maria Camilla Cerlesi, Mark Brown, Davide Malfacini, Vanessa Vezzi, Paola Molinari, Laura Micheli, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Remo Guerrini, Girolamo Calò, David G Lambert
INTRODUCTION: Opioid receptors are currently classified as Mu (μ), Delta (δ), Kappa (κ) plus the opioid related nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP). Despite compelling evidence for interactions and benefits of targeting more than one receptor type in producing analgesia, clinical ligands are Mu agonists. In this study we have designed a Mu-NOP agonist named DeNo. The Mu agonist component is provided by dermorphin, a peptide isolated from the skin of Phyllomedusa frogs and the NOP component by the endogenous agonist N/OFQ...
2016: PloS One
https://www.readbyqxmd.com/read/27238748/g%C3%AE-7-proteins-contribute-to-coupling-of-nociceptin-orphanin-fq-peptide-nop-opioid-receptors-and-voltage-gated-ca-2-channels-in-rat-stellate-ganglion-neurons
#15
Saifeldin Mahmoud, Mohamed Farrag, Victor Ruiz-Velasco
The nociceptin/orphanin FQ peptide (NOP) opioid receptors regulate neurotransmitter release via inhibition of voltage-gated Ca(2+) channels (CaV2.2) in sympathetic and sensory neurons. Stimulation of NOP receptors by its endogenous agonist, nociception (Noc), leads to membrane-delimited, voltage-dependent (VD) block of CaV2.2 channel currents mediated by Gβγ protein subunits. Previously we reported that the pertussis toxin-sensitive Gαi1 and Gβ2/β4 isoforms mediate the functional coupling of NOP opioid receptors with CaV channels in rat stellate ganglion (SG) sympathetic neurons...
August 3, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27225498/discriminative-stimulus-properties-of-opioid-ligands-progress-and-future-directions
#16
Eduardo R Butelman, Mary Jeanne Kreek
Opioid receptors (MOP-r, KOP-r, DOP-r, as well as NOP-r) and their endogenous neuropeptide agonist systems are involved in diverse neurobiological and behavioral functions, in health and disease. These functions include pain and analgesia, addictions, and psychiatric diseases (e.g., depression-, anxiety-like, and stress-related disorders). Drug discrimination assays have been used to characterize the behavioral pharmacology of ligands with affinity at MOP-r, KOP-r, or DOP-r (and to a lesser extent NOP-r). Therefore, drug discrimination studies with opioid ligands have an important continuing role in translational investigations of diseases that are affected by these neurobiological targets and their pharmacotherapy...
May 26, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27199205/a-key-role-for-the-n-ofq-nop-receptor-system-in-modulating-nicotine-taking-in-a-model-of-nicotine-and-alcohol-co-administration
#17
Andrea Cippitelli, Jennifer Schoch, Ginamarie Debevec, Gloria Brunori, Nurulain T Zaveri, Lawrence Toll
Alcohol and nicotine are often co-abused. Although the N/OFQ-NOP receptor system is considered a potential target for development of drug abuse pharmacotherapies, especially for alcoholism, little is known about the role of this system in nicotine dependence. Furthermore, the effect of prior history of nicotine dependence on subsequent nicotine and alcohol taking is understudied. Using an operant co-administration paradigm, in which rats concurrently self-administer nicotine and alcohol, we found that nicotine dependent rats increased nicotine self-administration over time as compared to non-dependent animals, while patterns of alcohol lever pressing did not change between groups...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27129865/antidepressant-activity-of-nociceptin-orphanin-fq-receptor-antagonists-in-the-mouse-learned-helplessness
#18
Victor A D Holanda, Iris U Medeiros, Laila Asth, Remo Guerrini, Girolamo Calo', Elaine C Gavioli
RATIONALE: Pharmacological and genetic evidence support antidepressant-like effects elicited by the blockade of the NOP receptor. The learned helplessness (LH) model employs uncontrollable and unpredictable electric footshocks as a stressor stimulus to induce a depressive-like phenotype that can be reversed by classical antidepressants. OBJECTIVES: The present study aimed to evaluate the action of NOP receptor antagonists in helpless mice. METHODS: Male Swiss mice were subjected to the three steps of the LH paradigm (i...
July 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27127846/nociceptin-orphanin-fq-receptor-expression-in-clinical-pain-disorders-and-functional-effects-in-cultured-neurons
#19
Praveen Anand, Yiangos Yiangou, Uma Anand, Gaurav Mukerji, Marco Sinisi, Michael Fox, Anthony McQuillan, Tom Quick, Yuri E Korchev, Peter Hein
The nociceptin/orphanin FQ peptide receptor (NOP), activated by its endogenous peptide ligand nociceptin/orphanin FQ (N/OFQ), exerts several effects including modulation of pain signalling. We have examined, for the first time, the tissue distribution of the NOP receptor in clinical visceral and somatic pain disorders by immunohistochemistry and assessed functional effects of NOP and μ-opioid receptor activation in cultured human and rat dorsal root ganglion (DRG) neurons. Quantification of NOP-positive nerve fibres within the bladder suburothelium revealed a remarkable several-fold increase in detrusor overactivity (P < 0...
September 2016: Pain
https://www.readbyqxmd.com/read/27100061/parsing-the-hedonic-and-motivational-influences-of-nociceptin-on-feeding-using-licking-microstructure-analysis-in-mice
#20
Ian A Mendez, Nigel T Maidment, Niall P Murphy
Opioid peptides are implicated in processes related to reward and aversion; however, how specific opioid peptides are involved remains unclear. We investigated the role of nociceptin (NOC) in voluntary licking for palatable and aversive tastants by studying the effect of intracerebroventricularly administered NOC on licking microstructure in wild-type and NOC receptor knockout (NOP KO) mice. Compared with the wild-type mice, NOP KO mice emitted fewer bouts of licking when training to lick for a 20% sucrose solution...
September 2016: Behavioural Pharmacology
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