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NOP Receptor

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https://www.readbyqxmd.com/read/29340866/-in-silico-study-of-the-binding-of-two-novel-antagonists-to-the-nociceptin-receptor
#1
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
#2
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
#3
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/29232769/antiparkinsonian-and-antidyskinetic-profiles-of-two-novel-potent-and-selective-nociceptin-orphanin-fq-receptor-agonists
#4
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 assay respectively, conducted in Chinese hamster ovary cells...
December 12, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29231765/imaging-corticotropin-releasing-factor-and-nociceptin-in-addiction-and-ptsd-models
#5
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 12, 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
#6
Nurulain T Zaveri, Paul V Marquez, Michael E Meyer, Willma E Polgar, Abdul Hamid, Kabirullah Lutfy
BACKGROUND: Nociceptin/Orphanin FQ (N/OFQ), the endogenous peptide agonist for the opioid receptor-like (ORL1) receptor (also known as NOP or the nociceptin receptor), has been shown to block the acquisition and expression of ethanol-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...
December 7, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29180970/cebranopadol-a-mixed-opioid-agonist-reduces-cocaine-self-administration-through-nociceptin-opioid-and-mu-opioid-receptors
#7
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
#8
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...
November 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29102248/nociceptin-and-the-nop-receptor-in-aversive-learning-in-mice
#9
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...
October 25, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29038479/probing-ligand-recognition-of-the-opioid-pan-antagonist-at-076-at-nociceptin-kappa-mu-and-delta-opioid-receptors-through-structure-activity-relationships
#10
V Blair Journigan, Willma E Polgar, Edward W Tuan, James Lu, Pankaj R Daga, Nurulain T Zaveri
Few opioid ligands binding to the three classic opioid receptor subtypes, mu, kappa and delta, have high affinity at the fourth opioid receptor, the nociceptin/orphanin FQ receptor (NOP). We recently reported the discovery of AT-076 (1), (R)-7-hydroxy-N-((S)-1-(4-(3-hydroxyphenyl)piperidin-1-yl)-3-methylbutan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, a pan antagonist with nanomolar affinity for all four subtypes. Since AT-076 binds with high affinity at all four subtypes, we conducted a structure-activity relationship (SAR) study to probe ligand recognition features important for pan opioid receptor activity, using chemical modifications of key pharmacophoric groups...
October 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29038035/biochemical-and-pharmacological-characterization-of-three-opioid-nociceptin-hybrid-peptide-ligands-reveals-substantially-differing-modes-of-their-actions
#11
Anna I Erdei, Adina Borbély, Anna Magyar, Nóra Taricska, András Perczel, Ottó Zsíros, Győző Garab, Edina Szűcs, Ferenc Ötvös, Ferenc Zádor, Mihály Balogh, Mahmoud Al-Khrasani, Sándor Benyhe
In an attempt to design opioid-nociceptin hybrid peptides, three novel bivalent ligands, H-YGGFGGGRYYRIK-NH2, H-YGGFRYYRIK-NH2 and Ac-RYYRIKGGGYGGFL-OH were synthesized and studied by biochemical, pharmacological, biophysical and molecular modelling tools. These chimeric molecules consist of YGGF sequence, a crucial motif in the N-terminus of natural opioid peptides, and Ac-RYYRIK-NH2, which was isolated from a combinatorial peptide library as an antagonist or partial agonist that inhibits the biological activity of the endogenously occurring heptadecapeptide nociceptin...
October 13, 2017: Peptides
https://www.readbyqxmd.com/read/28944554/limited-potential-of-cebranopadol-to-produce-opioid-type-physical-dependence-in-rodents
#12
Thomas M Tzschentke, Babette Y Kögel, Stefanie Frosch, Klaus Linz
Cebranopadol is a novel potent analgesic agonist at the nociceptin/orphanin FQ peptide (NOP) and classical opioid receptors. As NOP receptor activation has been shown to reduce side effects related to the activation of μ-opioid peptide (MOP) receptors, the present study evaluated opioid-type physical dependence produced by cebranopadol in mice and rats. In a naloxone-precipitated withdrawal assay in mice, a regimen of seven escalating doses of cebranopadol over 2 days produced only very limited physical dependence as evidenced by very little withdrawal symptoms (jumping) even at cebranopadol doses clearly exceeding the analgesic dose range...
September 25, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28928762/novel-protein-protein-inhibitor-based-approach-to-control-plant-ethylene-responses-synthetic-peptides-for-ripening-control
#13
Mareike Kessenbrock, Simone M Klein, Lena Müller, Mauricio Hunsche, Georg Noga, Georg Groth
Ethylene signaling is decisive for many plant developmental processes. Among these, control of senescence, abscission and fruit ripening are of fundamental relevance for global agriculture. Consequently, detailed knowledge of the signaling network along with the molecular processes of signal perception and transfer are expected to have high impact on future food production and agriculture. Recent advances in ethylene research have demonstrated that signaling of the plant hormone critically depends on the interaction of the ethylene receptor family with the NRAMP-like membrane protein ETHYLENE INSENSITIVE 2 (EIN2) at the ER membrane, phosphorylation-dependent proteolytic processing of ER-localized EIN2 and subsequent translocation of the cleaved EIN2 C-terminal polypeptide (EIN2-CEND) to the nucleus...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28856406/panicolytic-like-effects-caused-by-substantia-nigra-pars-reticulata-pretreatment-with-low-doses-of-endomorphin-1-and-high-doses-of-ctop-or-the-nop-receptors-antagonist-jtc-801-in-male-rattus-norvegicus
#14
Juliana Almeida da Silva, Audrey Franceschi Biagioni, Rafael Carvalho Almada, Renato Leonardo de Freitas, Norberto Cysne Coimbra
RATIONALE: Gamma-aminobutyric acid (GABA)ergic neurons of the substantia nigra pars reticulata (SNpr) are connected to the deep layers of the superior colliculus (dlSC). The dlSC, in turn, connect with the SNpr through opioid projections. Nociceptin/orphanin FQ peptide (N/OFQ) is a natural ligand of a Gi protein-coupled nociceptin receptor (ORL1; NOP) that is also found in the SNpr. Our hypothesis is that tectonigral opioid pathways and intranigral orphanin-mediated mechanisms modulate GABAergic nigrotectal connections...
October 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28805972/in-vitro-pharmacological-characterization-of-a-novel-unbiased-nop-receptor-selective-nonpeptide-agonist-at-403
#15
Federica Ferrari, Davide Malfacini, Blair V Journigan, Mark F Bird, Claudio Trapella, Remo Guerrini, David G Lambert, Girolamo Calo', Nurulain T Zaveri
Nociceptin/orphanin FQ (N/OFQ) regulates several biological functions via selective activation of the N/OFQ receptor (NOP), a member of the opioid receptor family. We recently identified a new high affinity and highly selective NOP agonist AT-403. In this study, we characterized the functional profile of AT-403 and compared it to other known nonpeptide NOP agonists Ro 65-6570, Ro 2q, SCH-221510, MCOPPB, AT-202 and SCH-486757, using the following assays: GTPγ[(35) S] stimulated binding, calcium mobilization assay in cells-expressing human NOP or classical opioid receptors and chimeric G proteins, bioluminescence resonance energy transfer (BRET) based assay for studying NOP receptor interaction with G protein and arrestin, and the electrically stimulated mouse vas deferens bioassay...
August 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28711193/nociceptin-receptors-in-alcohol-use-disorders-a%C3%A2-positron-emission-tomography-study-using-11-c-nop-1a
#16
Rajesh Narendran, Roberto Ciccocioppo, Brian Lopresti, Jennifer Paris, Michael L Himes, N Scott Mason
BACKGROUND: The neuropeptide transmitter nociceptin, which binds to the nociceptin/orphanin FQ peptide (NOP) receptor, is a core component of the brain's antistress system. Nociceptin exerts its antistress effect by counteracting the functions of corticotropin-releasing factor, the primary stress-mediating neuropeptide in the brain. Basic investigations support a role for medications that target nociceptin receptors in the treatment of alcohol use disorders. Thus, it is of high interest to measure the in vivo status of NOP receptors in individuals with alcohol use disorders...
May 31, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28705439/activation-of-nociceptin-orphanin-fq-receptors-inhibits-contextual-fear-memory-reconsolidation
#17
Khaoula Rekik, Raquel Faria Da Silva, Morgane Colom, Salvatore Pacifico, Nurulain T Zaveri, Girolamo Calo', Claire Rampon, Bernard Frances, Lionel Mouledous
Several neuropeptidergic systems act as modulators of cognitive performances. Among them, nociceptin, an opioid-like peptide also known as orphanin FQ (N/OFQ), has recently gained attention. Stimulation of its receptor, the N/OFQ opioid receptor (NOP), which is expressed in brain regions involved in emotion, memory and stress response, has inhibitory effects on the acquisition and/or consolidation of spatial and emotional memory in rodents. Recently, N/OFQ was also proposed to be linked to the pathogenesis of Post-Traumatic Stress Disorder in humans...
July 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28704271/mitigation-of-adverse-behavioral-impact-from-predator-exposure-by-the-nociceptin-orphanin-fq-peptide-antagonist-j-113397-in-rats
#18
Raymond F Genovese, Stefania Dobre
The nociceptin/orphanin FQ peptide (NOP) receptor is believed to have an integral modulatory function in the stress response system. We evaluated the highly selective NOP antagonist J-113397 (7.5 and 20.0 mg/kg), using a predator exposure in which rats were exposed to predator cats as a stressor. A single dose of J-113397 or vehicle was administered (intraperitoneally) shortly before exposure to the predators or a sham exposure. Behavioral impact was measured using elevated plus maze (EPM), open field activity (OFA), and an olfactory discrimination (OD)...
July 12, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28697954/antinociceptive-action-of-nop-and-opioid-receptor-agonists-in-the-mouse-orofacial-formalin-test
#19
A Rizzi, C Ruzza, S Bianco, C Trapella, G Calo'
Nociceptin/orphanin FQ (N/OFQ) modulates several biological functions, including pain transmission via selective activation of a specific receptor named NOP. The aim of this study was the investigation of the antinociceptive properties of NOP agonists and their interaction with opioids in the trigeminal territory. The orofacial formalin (OFF) test in mice was used to investigate the antinociceptive potential associated to the activation of NOP and opioid receptors. Mice subjected to OFF test displayed the typical biphasic nociceptive response and sensitivity to opioid and NSAID drugs...
August 2017: Peptides
https://www.readbyqxmd.com/read/28645915/cebranopadol-blocks-the-escalation-of-cocaine-intake-and-conditioned-reinstatement-of-cocaine-seeking-in-rats
#20
Giordano de Guglielmo, Alessandra Matzeu, Jenni Kononoff, Julia Mattioni, Rémi Martin-Fardon, Olivier George
Cebranopadol is a novel agonist of nociceptin/orphanin FQ peptide (NOP) and opioid receptors with analgesic properties that is being evaluated in clinical Phase 2 and Phase 3 trials for the treatment of chronic and acute pain. Recent evidence indicates that the combination of opioid and NOP receptor agonism may be a new treatment strategy for cocaine addiction. We sought to extend these findings by examining the effects of cebranopadol on cocaine self-administration (0.5 mg/kg/infusion) and cocaine conditioned reinstatement in rats with extended access to cocaine...
September 2017: Journal of Pharmacology and Experimental Therapeutics
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