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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
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
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
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
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
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
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
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
Melanie M A Bisson, Mareike Kessenbrock, Lena Müller, Alexander Hofmann, Florian Schmitz, Simona M Cristescu, Georg Groth
The plant hormone ethylene is involved in the regulation of several processes with high importance for agricultural applications, e.g. ripening, aging and senescence. Previous work in our group has identified a small peptide (NOP-1) derived from the nuclear localization signal of the Arabidopsis ethylene regulator ETHYLENE INSENSITIVE-2 (EIN2) C-terminal part as efficient inhibitor of ethylene responses. Here, we show that NOP-1 is also able to efficiently disrupt EIN2-ETR1 complex formation in tomato, indicating that the NOP-1 inhibition mode is conserved across plant species...
August 1, 2016: Scientific Reports
Shazia Bano, Samina Nazir, Saeeda Munir, Mohamed Fahad AlAjmi, Muhammad Afzal, Kehkashan Mazhar
We report "smart" nickel oxide nanoparticles (NOPs) as multimodal cancer therapy agent. Water-dispersible and light-sensitive NiO core was synthesized with folic acid (FA) connected bovine serum albumin (BSA) shell on entrapped doxorubicin (DOX). The entrapped drug from NOP-DOX@BSA-FA was released in a sustained way (64 hours, pH=5.5, dark conditions) while a robust release was found under red light exposure (in 1/2 hour under λmax=655 nm, 50 mW/cm(2), at pH=5.5). The cell viability, thiobarbituric acid reactive substances and diphenylisobenzofuran assays conducted under light and dark conditions revealed a high photodynamic therapy potential of our construct...
2016: International Journal of Nanomedicine
Tomo Ando, Hisato Takagi
New-onset persistent left bundle branch block (NOP-LBBB) is one of the most common conduction disturbances after transcatheter aortic valve implantation (TAVI). We hypothesized that NOP-LBBB may have a clinically negative impact after TAVI. To find out, we conducted a systematic literature search of the MEDLINE/PubMed and Embase databases. Observational studies that reported clinical outcomes of NOP-LBBB patients after TAVI were included. The random-effects model was used to combine odds ratios, risk ratios, or hazard ratios (HRs) with 95% confidence intervals...
September 2016: Clinical Cardiology
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...
July 1, 2016: Fundamental & Clinical Pharmacology
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
Robert W Stackman, Sarah J Cohen, Joan C Lora, Lisa M Rios
Recognition of a previously experienced item or object depends upon the successful retrieval of memory for the object. The neural mechanisms that support object recognition memory in the mammalian brain are not well understood. The rodent hippocampus plays a well-established role in spatial memory, and we previously demonstrated that temporary inactivation of the mouse hippocampus impairs object memory, as assessed with a novel object preference (NOP) test. The present studies were designed to test some remaining issues regarding the contribution of the CA1 sub-region of the mouse dorsal hippocampus to long-term object memory...
September 2016: Neurobiology of Learning and Memory
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
Andrea Burón, Margarita Posso, Judit Sivilla, Jaume Grau, Rafael Guayta, Xavier Castells, Antoni Castells, Francesc Macià
BACKGROUND AND OBJECTIVE: Population-based bowel screening programmes with faecal occult blood (FOB) tests need to achieve high uptake rates and offer quality services. We invited participants in the Barcelona Programme to complete a satisfaction survey, in order to explore factors influencing uptake and respondents' opinion and satisfaction with each step of the screening process. MATERIAL AND METHOD: Telephone survey using an ad hoc questionnaire (see annex) administered to a final sample of 1189 people: 310 non-participants in the programme (NoP), 553 participants with a negative test result (PNeg), and 326 participants with a positive result (PPos)...
June 9, 2016: Gastroenterología y Hepatología
D Vyas, S M McGinn, S M Duval, M Kindermann, K A Beauchemin
The study objective was to evaluate the effects of sustained reduction of enteric methane (CH) emissions with dietary supplementation of the inhibitor 3-nitrooxypropanol (NOP) on growth rate and feed conversion efficiency of growing and finishing beef cattle. Eighty-four crossbred steers were used in a 238-d feeding study and fed a backgrounding diet for the first 105 d (backgrounding phase) and transition diets for 28 d followed by a finishing diet for 105 d (finishing phase) with 3 doses of NOP (0, 100, and 200 mg/kg DM)...
May 2016: Journal of Animal Science
Michael E Pichichero
This review summarizes a prospective, longitudinal 10-year study in Rochester, NY, with virtually every clinically diagnosed acute otitis media (AOM) confirmed by bacterial culture of middle ear fluid. Children experiencing 3 episodes within 6 months or 4 episodes in 12 months were considered stringently defined otitis prone (sOP). We found stringent diagnosis compared with clinical diagnosis reduced the frequency of children meeting the OP definition from 27% to 6% resulting in 14.8% and 2.4% receiving tympanostomy tubes, respectively...
September 2016: Pediatric Infectious Disease Journal
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
Eva Brod, Anne Falk Øgaard, Tore Krogstad, Trond Knapp Haraldsen, Emmanuel Frossard, Astrid Oberson
Minable rock phosphate is a finite resource. Replacing mineral phosphorus (P) fertilizer with P-rich secondary resources is one way to manage P more efficiently, but the importance of physicochemical and microbial soil processes induced by secondary resources for plant P uptake is still poorly understood. Using radioactive-labeling techniques, the fertilization effects of dairy manure, fish sludge, meat bone meal, and wood ash were studied as P uptake by barley after 44 days and compared with those of water-soluble mineral P (MinP) and an unfertilized control (NoP) in a pot experiment with an agricultural soil containing little available P at two soil pH levels, approximately pH 5...
2016: Frontiers in Nutrition
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