keyword
MENU ▼
Read by QxMD icon Read
search

nop

keyword
https://www.readbyqxmd.com/read/28337331/light-regulated-no-release-as-a-novel-strategy-to-overcome-doxorubicin-multidrug-resistance
#1
Konstantin Chegaev, Aurore Fraix, Elena Gazzano, Gamal Eldein F Abd-Ellatef, Marco Blangetti, Barbara Rolando, Sabrina Conoci, Chiara Riganti, Roberta Fruttero, Alberto Gasco, Salvatore Sortino
Nitric oxide (NO) release from a suitable NO photodonor (NOP) can be fine-tuned by visible light stimuli at doses that are not toxic to cells but that inhibit several efflux pumps; these are mainly responsible for the multidrug resistance of the anticancer agent doxorubicin (DOX). The strategy may thus increase DOX toxicity against resistant cancer cells. Moreover, a novel molecular hybrid covalently joining DOX and NOP showed similar increased toxicity toward resistant cancer cells and, in addition, lower cardiotoxicity than DOX...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28299439/vitamin-b12-deficiency-evaluation-and-treatment-in-severe-dry-eye-disease-with-neuropathic-ocular-pain
#2
Serkan Ozen, Murat Atabey Ozer, Mehmet Orçun Akdemir
PURPOSE: This study aims to understand the effect of vitamin B12 deficiency on neuropathic ocular pain (NOP) and symptoms in patients with dry eye disease (DED). METHODS: Patients with severe DED (without receiving topical artificial tears treatment) and ocular pain were enrolled (n = 90). Patients with severe DED and vitamin B12 deficiency (group 1, n = 45) received parenteral vitamin B12 supplement + topical treatment (artificial tears treatment + cyclosporine), and patients with severe DED and normal serum vitamin B12 level (group 2, n = 45) received only topical treatment (artificial tears treatment + cyclosporine)...
March 15, 2017: Graefe's Archive for Clinical and Experimental Ophthalmology
https://www.readbyqxmd.com/read/28124644/differences-in-innate-immune-response-gene-regulation-in-the-middle-ear-of-children-who-are-otitis-prone-and-in-those-not-otitis-prone
#3
Ravinder Kaur, Janet Casey, Michael Pichichero
OBJECTIVE: Acute otitis media (AOM) causes an inflammatory response in the middle ear. We assessed differences in innate immune responses involved in bacterial defense at onset of AOM in children who were stringently defined as otitis prone (sOP) and children not otitis prone (NOP). STUDY DESIGN: Innate immune genes analysis from middle ear fluid (MEF) samples of children. METHODS: Genes of toll-like receptors (TLR), nod-like and retinoic acid-inducible gene-I-like receptors, downstream effectors important for inflammation and apoptosis, including cytokines and chemokines, were studied from MEF samples by using a real-time polymerase chain reaction array...
November 1, 2016: American Journal of Rhinology & Allergy
https://www.readbyqxmd.com/read/28116100/pharmacological-characterization-of-cebranopadol-a-novel-analgesic-acting-as-mixed-nociceptin-orphanin-fq-and-opioid-receptor-agonist
#4
Anna Rizzi, Maria Camilla Cerlesi, Chiara Ruzza, Davide Malfacini, Federica Ferrari, Sara Bianco, Tommaso Costa, Remo Guerrini, Claudio Trapella, Girolamo Calo'
The aim of the study was to investigate the in vitro and in vivo pharmacological profile of cebranopadol, a novel agonist for opioid and nociceptin/orphanin FQ (N/OFQ) receptors (NOP). In vitro cebranopadol was assayed in calcium mobilization studies in cells coexpressing NOP or opioid receptors and chimeric G-proteins and in a bioluminescence resonance energy transfer (BRET) assay for studying receptor interaction with G-protein and β-arrestin 2. The mouse tail withdrawal and formalin tests were used for investigating cebranopadol antinociceptive properties...
August 2016: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28112482/antihyperalgesic-antiallodynic-and-antinociceptive-effects-of-cebranopadol-a-novel-potent-nociceptin-orphanin-fq-and-opioid-receptor-agonist-after-peripheral-and-central-administration-in-rodent-models-of-neuropathic-pain
#5
Thomas M Tzschentke, Klaus Linz, Stefanie Frosch, Thomas Christoph
Cebranopadol is a novel and highly potent analgesic acting via nociceptin/orphanin FQ peptide (NOP) and opioid receptors. Since NOP and opioid receptors are expressed in the central nervous system as well as in the periphery, this study addressed the question of where cebranopadol exerts its effects in animal models of chronic neuropathic pain. Mechanical hypersensitivity in streptozotocin (STZ)-treated diabetic rats, cold allodynia in the chronic constriction injury (CCI) model in rats, and heat hyperalgesia and nociception in STZ-treated diabetic and control mice was determined after intraplantar (i...
January 23, 2017: Pain Practice: the Official Journal of World Institute of Pain
https://www.readbyqxmd.com/read/28100479/evidence-of-central-sensitisation-in-those-with-dry-eye-symptoms-and-neuropathic-like-ocular-pain-complaints-incomplete-response-to-topical-anaesthesia-and-generalised-heightened-sensitivity-to-evoked-pain
#6
Ashley M Crane, William Feuer, Elizabeth R Felix, Roy C Levitt, Allison L McClellan, Konstantinos D Sarantopoulos, Anat Galor
OBJECTIVE: To evaluate how closely neuropathic-like ocular pain (NOP) symptoms align with a metric of central sensitisation (ie, the presence of persistent ocular pain after topical anaesthetic placement) in individuals with dry eye (DE) symptoms. DESIGN: Cross-sectional study of 224 individuals with DE symptoms seen in the Miami Veterans Affairs eye clinic. An evaluation was performed consisting of questionnaires regarding DE symptoms, NOP descriptors and evoked pain sensitivity testing on the forehead and forearm, followed by a comprehensive ocular surface examination including corneal mechanical sensitivity testing...
January 18, 2017: British Journal of Ophthalmology
https://www.readbyqxmd.com/read/28097008/preclinical-findings-predicting-efficacy-and-side-effect-profile-of-ly2940094-an-antagonist-of-nociceptin-receptors
#7
Jeffrey M Witkin, Linda M Rorick-Kehn, Mark J Benvenga, Benjamin L Adams, Scott D Gleason, Karen M Knitowski, Xia Li, Steven Chaney, Julie F Falcone, Janice W Smith, Julie Foss, Kirsti Lloyd, John T Catlow, David L McKinzie, Kjell A Svensson, Vanessa N Barth, Miguel A Toledo, Nuria Diaz, Celia Lafuente, Alma Jiménez, Alfonso Benito, Conception Pedregal, Maria A Martínez-Grau, Anke Post, Michael A Ansonoff, John E Pintar, Michael A Statnick
Nociceptin/Orphanin FQ (N/OFQ) is a 17 amino acid peptide whose receptor is designated ORL1 or nociceptin receptor (NOP). We utilized a potent, selective, and orally bioavailable antagonist with documented engagement with NOP receptors in vivo to assess antidepressant- and anxiolytic-related pharmacological effects of NOP receptor blockade along with measures of cognitive and motor impingement. 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) displayed antidepressant-like behavioral effects in the forced-swim test in mice, an effect absent in NOP (-/-) mice...
December 2016: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28000999/n-ofq-system-in-brain-areas-of-nerve-injured-mice-its-role-in-different-aspects-of-neuropathic-pain
#8
M Palmisano, D Mercatelli, F F Caputi, D Carretta, P Romualdi, S Candeletti
Several studies showed that chronic pain causes reorganization and functional alterations of supraspinal brain regions. The nociceptin-NOP receptor system is one of the major systems involved in pain control and much evidence also suggested its implication in stress, anxiety and depression. Therefore, we investigated the nociceptin-NOP system alterations in selected brain regions in a neuropathic pain murine model. Fourteen days after the common sciatic nerve ligature, PCR analysis indicated a significant decrease of pronociceptin and NOP receptor mRNA levels in the thalamus; these alterations could contribute to the decrease of the thalamic inhibitory function reported in neuropathic pain condition...
December 21, 2016: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/27989838/opioid-gene-expression-changes-and-post-translational-histone-modifications-at-promoter-regions-in-the-rat-nucleus-accumbens-after-acute-and-repeated-3-4-methylenedioxy-methamphetamine-mdma-exposure
#9
Francesca Felicia Caputi, Martina Palmisano, Lucia Carboni, Sanzio Candeletti, Patrizia Romualdi
The recreational drug of abuse 3,4-methylenedioxymethamphetamine (MDMA) has been shown to produce neurotoxic damage and long-lasting changes in several brain areas. In addition to the involvement of serotoninergic and dopaminergic systems, little information exists about the contribution of nociceptin/orphaninFQ (N/OFQ)-NOP and dynorphin (DYN)-KOP systems in neuronal adaptations evoked by MDMA. Here we investigated the behavioral and molecular effects induced by acute (8mg/kg) or repeated (8mg/kg twice daily for seven days) MDMA exposure...
December 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27871910/pharmacological-studies-on-the-nop-and-opioid-receptor-agonist-pwt2-dmt-1-n-ofq-1-13
#10
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...
January 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27806703/neuropathic-pain-in-patients-with-rotator-cuff-tears
#11
Tatsuki Karasugi, Junji Ide, Toshio Kitamura, Nobukazu Okamoto, Takuya Tokunaga, Hiroshi Mizuta
BACKGROUND: Recent studies have confirmed the existence of neuropathic pain (NeP) components in patients with musculoskeletal disorders. However, the presence of NeP in patients with rotator cuff tears has not been investigated thus far. Therefore, we studied the prevalence of NeP and the prognostic factors for NeP in patients with rotator cuff tears. METHODS: Data were collected from 110 patients with rotator cuff tears, diagnosed by physical examination and magnetic resonance imaging, who attended an outpatient clinic between August 2013 and August 2014...
November 2, 2016: BMC Musculoskeletal Disorders
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
#12
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
#13
Federica Ferrari, Maria Camilla Cerlesi, Davide Malfacini, Laila Asth, Elaine C Gavioli, Blair V Journigan, Uma Gayathri 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...
December 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27778406/cebranopadol-novel-dual-opioid-nop-receptor-agonist-analgesic
#14
REVIEW
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...
February 2017: 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
#15
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)...
January 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27667485/functional-pharmacological-characterisation-of-ser100-in-cardiovascular-health-and-disease
#16
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/27595926/no-privacy-a-xenopus-tropicalis-mutant-is-a-model-of-human-hermansky-pudlak-syndrome-and-allows-visualization-of-internal-organogenesis-during-tadpole-development
#17
Takuya Nakayama, Keisuke Nakajima, Amanda Cox, Marilyn Fisher, Mary Howell, Margaret B Fish, Yoshio Yaoita, Robert M Grainger
We describe a novel recessive and nonlethal pigmentation mutant in Xenopus tropicalis. The mutant phenotype can be initially observed in tadpoles after stage 39/40, when mutant embryos display markedly reduced pigmentation in the retina and the trunk. By tadpole stage 50 almost all pigmented melanophores have disappeared. Most interestingly, those embryos fail entirely to make pigmented iridophores. The combined reduction/absence of both pigmented iridophores and melanophores renders these embryos virtually transparent, permitting one to easily observe both the developing internal organs and nervous system; accordingly, we named this mutant no privacy (nop)...
September 2, 2016: Developmental Biology
https://www.readbyqxmd.com/read/27573832/a-novel-orvinol-analog-bu08028-as-a-safe-opioid-analgesic-without-abuse-liability-in-primates
#18
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
#19
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
#20
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 NOP/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...
February 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
keyword
keyword
38970
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"