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Delta opioid receptor

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https://www.readbyqxmd.com/read/28204957/insights-into-the-role-of-opioid-receptors-in-the-gi-tract-experimental-evidence-and-therapeutic-relevance
#1
James J Galligan, Catia Sternini
Opioid drugs are prescribed extensively for pain treatment but when used chronically they induce constipation that can progress to opioid-induced bowel dysfunction. Opioid drugs interact with three classes of opioid receptors: mu opioid receptors (MORs), delta opioid receptors (DOR), and kappa opioid receptors (KORs), but opioid drugs mostly target the MORs. Upon stimulation, opioid receptors couple to inhibitory Gi/Go proteins that activate or inhibit downstream effector proteins. MOR and DOR couple to inhibition of adenylate cyclase and voltage-gated Ca(2+) channels and to activation of K(+) channels resulting in reduced neuronal activity and neurotransmitter release...
February 16, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28192197/characterization-of-3-h-oxymorphone-binding-sites-in-mouse-brain-quantitative-autoradiography-in-opioid-receptor-knockout-mice
#2
Ji Hoon Yoo, Anna Borsodi, Géza Tóth, Sándor Benyhe, Robert Gaspar, Audrey Matifas, Brigitte L Kieffer, Athanasios Metaxas, Ian Kitchen, Alexis Bailey
Oxymorphone, one of oxycodone's metabolic products, is a potent opioid receptor agonist which is thought to contribute to the analgesic effect of its parent compound and may have high potential abuse liability. Nonetheless, the in vivo pharmacological binding profile of this drug is still unclear. This study uses mice lacking mu (MOP), kappa (KOP) or delta (DOP) opioid receptors as well as mice lacking all three opioid receptors to provide full characterisation of oxymorphone binding sites in the brain. Saturation binding studies using [(3)H]oxymorphone revealed high affinity binding sites in mouse brain displaying Kd of 1...
February 9, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28162605/-364-morphine-tolerance-during-inflammatory-pain-role-of-delta-opioid-receptors-in-the-midbrain-periaqueductal-gray
#3
A Wilson-Poe, J Moron Concepcion
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28162602/-359-grk2-constitutively-downregulates-delta-opioid-receptor-activity-in-the-periphery
#4
A Doyle, R Gomez, M Henry, N Jeske
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28116100/pharmacological-characterization-of-cebranopadol-a-novel-analgesic-acting-as-mixed-nociceptin-orphanin-fq-and-opioid-receptor-agonist
#5
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/28105279/nanoconjugated-nap-as-a-potent-and-periphery-selective-mu-opioid-receptor-modulator-to-treat-opioid-induced-constipation
#6
Guoyan G Xu, Olga Yu Zolotarskaya, Dwight A Williams, Yunyun Yuan, Dana E Selley, William L Dewey, Hamid I Akbarali, Hu Yang, Yan Zhang
Opioids are the mainstay for cancer and noncancer pain management. However, their use is often associated with multiple adverse effects. Among them, the most common and persistent one is probably opioid-induced constipation (OIC). Periphery selective opioid antagonists may alleviate the symptoms of OIC without compromising the analgesic effects of opioids. Recently our laboratories have identified one novel lead compound, 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)acetamido]morphinan (NAP), as a peripherally selective mu opioid receptor ligand carrying subnanomolar affinity to the mu opioid receptor and over 100-folds of selectivity over both the delta and kappa opioid receptors, with reasonable oral availability and half-life, and potential to treat OIC...
January 12, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28088065/methionine-enkephalin-menk-mounts-antitumor-effect-via-regulating-dendritic-cells-dcs
#7
Yiming Meng, Xinghua Gao, Wenna Chen, Nicolas P Plotnikoff, Noreen Griffin, Guirong Zhang, Fengping Shan
MENK, an endogenous opioid peptide has been reported to have many immunological and antitumor activities. So far the detailed mechanisms of antitumor through regulating DCs by MENK have not been elucidated yet. The aim of this work was to investigate the antitumor mechanisms of MENK via regulating DC. The monitoring methods, such as ELISA, MTS assay, CFSE, Real-time PCR and Western blot were included in our research. We found bone marrow derived dendritic cells (BMDCs) in 36 female C57BL/6 mice treated with MENK enhanced expression of key surface molecules, increased production of critical cytokines reduced endocytosis of FITC-dextran, upregulated TLR4 through MyD88/NF-κB signaling pathway and mounted higher antitumor activity...
January 11, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28072812/is-kratom-the-new-legal-high-on-the-block-the-case-of-an-emerging-opioid-receptor-agonist-with-substance-abuse-potential
#8
George C Chang-Chien, Charles A Odonkor, Prin Amorapanth
Kratom is an unscheduled opioid receptor agonist that comes in the form of dietary supplements currently being abused by chronic pain patients on prescription opioids. Active alkaloids isolated from kratom such as mitragynine and 7-hydroxymitragynine are thought to act on mu- and delta-opioid receptors as well as alpha-2 adrenergic and 5-HT2A receptors. Animal studies suggest that kratom may be more potent than morphine. Consequently, kratom consumption produces analgesic and euphoric feelings among users. In particular, some chronic pain patients on opioids take kratom to counteract the effects of opioid withdrawal...
January 2017: Pain Physician
https://www.readbyqxmd.com/read/28041939/involvement-of-the-coatomer-protein-complex-i-in-the-intracellular-traffic-of-the-delta-opioid-receptor
#9
Étienne St-Louis, Jade Degrandmaison, Sébastien Grastilleur, Samuel Génier, Véronique Blais, Christine Lavoie, Jean-Luc Parent, Louis Gendron
The delta opioid receptor (DOPr) is known to be mainly expressed in intracellular compartments. It remains unknown why DOPr is barely exported to the cell surface, but it seems that a substantial proportion of the immature receptor is trapped within the endoplasmic reticulum (ER) and the Golgi network. In the present study, we performed LC-MS/MS analysis to identify putative protein partners involved in the retention of DOPr. Analysis of the proteins co-immunoprecipitating with Flag-DOPr in transfected HEK293 cells revealed the presence of numerous subunits of the coatomer protein complex I (COPI), a vesicle-coating complex involved in recycling resident proteins from the Golgi back to the ER...
December 30, 2016: Molecular and Cellular Neurosciences
https://www.readbyqxmd.com/read/28035534/oprd1-genetic-variation-and-human-disease
#10
Richard C Crist, Toni-Kim Clarke
The OPRD1 gene encodes the delta-opioid receptor, which has multiple functions including regulating reward pathways. The gene contains more than 2,000 verified genetic variants but only 2 currently have evidence for specific functions: rs1042114 disrupts maturation of the receptor and rs569356 affects OPRD1 expression. These polymorphisms and others in the gene have been found to be associated with human diseases. The most reproducible data are associations between opioid addiction and three variants in intron 1 (rs2236861, rs2236857, and rs3766951), which have been described in a number of independent populations...
December 30, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28035528/delta-opioid-receptors-learning-and-motivation
#11
L P Pellissier, C N Pujol, J A J Becker, J Le Merrer
Delta opioid receptor (DOR) displays a unique, highly conserved, structure and an original pattern of distribution in the central nervous system, pointing to a distinct and specific functional role among opioid peptide receptors. Over the last 15 years, in vivo pharmacology and genetic models have allowed significant advances in the understanding of this role. In this review, we will focus on the involvement of DOR in modulating different types of hippocampal- and striatal-dependent learning processes as well as motor function, motivation, and reward...
December 30, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28011222/benzylideneoxymorphone-a-new-lead-for-development-of-bifunctional-mu-delta-opioid-receptor-ligands
#12
Jason R Healy, Padmavani Bezawada, Nicholas W Griggs, Andrea L Devereaux, Rae R Matsumoto, John R Traynor, Andrew Coop, Christopher W Cunningham
Opioid analgesic tolerance remains a considerable drawback to chronic pain management. The finding that concomitant administration of delta opioid receptor (DOR) antagonists attenuates the development of tolerance to mu opioid receptor (MOR) agonists has led to interest in producing bifunctional MOR agonist/DOR antagonist ligands. Herein, we present 7-benzylideneoxymorphone (6, UMB 246) displaying MOR partial agonist/DOR antagonist activity, representing a new lead for designing bifunctional MOR/DOR ligands...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28005346/identification-of-crucial-amino-acid-residues-involved-in-agonist-signaling-at-the-gpr55-receptor
#13
Mary A Lingerfelt, Pingwei Zhao, Haleli P Sharir, Dow P Hurst, Patricia H Reggio, Mary E Abood
GPR55 is a newly deorphanized class A G-protein-coupled receptor that has been implicated in inflammatory pain, neuropathic pain, metabolic disorder, bone development, and cancer. Few potent GPR55 ligands have been identified to date. This is largely due to an absence of information about salient features of GPR55, such as residues important for signaling and residues implicated in the GPR55 signaling cascade. The goal of this work was to identify residues that are key for the signaling of the GPR55 endogenous ligand, l-α-lysophosphatidylinositol (LPI), as well as the signaling of the GPR55 agonist, ML184 {CID 2440433, 3-[4-(2,3-dimethylphenyl)piperazine-1-carbonyl]-N,N-dimethyl-4-pyrrolidin-1-ylbenzenesulfonamide}...
January 24, 2017: Biochemistry
https://www.readbyqxmd.com/read/28001096/targeting-delta-opioid-receptors-for-pain-treatment-drugs-in-phase-i-and-ii-clinical-development
#14
Viola Spahn, Christoph Stein
Opioids are widely used to treat severe pain. Most clinically used opioids activate µ-opioid receptors (MOR). Their ligands induce potent analgesia but also adverse effects. The δ-opioid receptor (DOR) is another member of the opioid receptor family that has been under intense investigation with the aim to avoid MOR-induced side effects. Areas covered: This article reviews DOR ligands which appeared to be promising after preclinical evaluation. A literature search using Pubmed, Cochrane library, ClinicalTrials...
February 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/27990618/lipid-emulsion-inhibits-apoptosis-induced-by-a-toxic-dose-of-verapamil-via-the-delta-opioid-receptor-in-h9c2-rat-cardiomyoblasts
#15
Seong-Ho Ok, Mun Hwan Choi, Il-Woo Shin, Soo Hee Lee, Sebin Kang, Jiah Oh, Jeong Yeol Han, Ju-Tae Sohn
The goals of this study were to investigate the effects of lipid emulsion (LE) on apoptosis induced by a toxic dose of verapamil in H9c2 cells and to elucidate the associated cellular mechanism. The effects of LE alone and combined with an inhibitor on the decreases in cell counts and viability induced by verapamil and diltiazem were examined using the MTT assay. The effects of verapamil alone, combined LE and verapamil treatment, and combined inhibitor, LE and verapamil treatment on cleaved caspase-3, caspase-8 and Bax expression, were examined using Western blotting...
December 19, 2016: Cardiovascular Toxicology
https://www.readbyqxmd.com/read/27981195/sex-differences-in-subcellular-distribution-of-delta-opioid-receptors-in-the-rat-hippocampus-in-response-to-acute-and-chronic-stress
#16
Sanoara Mazid, Baila S Hall, Shannon C Odell, Khalifa Stafford, Andreina D Dyer, Tracey A Van Kempen, Jane Selegean, Bruce S McEwen, Elizabeth M Waters, Teresa A Milner
Drug addiction requires associative learning processes that critically involve hippocampal circuits, including the opioid system. We recently found that acute and chronic stress, important regulators of addictive processes, affect hippocampal opioid levels and mu opioid receptor trafficking in a sexually dimorphic manner. Here, we examined whether acute and chronic stress similarly alters the levels and trafficking of hippocampal delta opioid receptors (DORs). Immediately after acute immobilization stress (AIS) or one-day after chronic immobilization stress (CIS), the brains of adult female and male rats were perfusion-fixed with aldehydes...
December 2016: Neurobiology of Stress
https://www.readbyqxmd.com/read/27916688/effects-of-repeated-treatment-with-a-delta-opioid-receptor-agonist-knt-127-on-hyperemotionality-in-olfactory-bulbectomized-rats
#17
Leo Gotoh, Akiyoshi Saitoh, Misa Yamada, Hideaki Fujii, Hiroshi Nagase, Mitsuhiko Yamada
We previously demonstrated that a single treatment of a non-peptidic delta opioid receptor agonist, KNT-127, has an antidepressant-like effect in rodents in the forced swim test. Here we evaluated the effect of repeated administration of the potential antidepressant KNT-127 in an olfactory-bulbectomized (OBX) rat model. Male Wistar rats (8-12 weeks old) underwent olfactory bulbectomy. From 14days after surgery each was weighed and administered either KNT-127 (3mgkg(-1)/day), the selective serotonin reuptake inhibitor (SSRI) fluoxetine (10mgkg(-1)/day), or vehicle, daily for 14 days...
December 1, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27913257/prodynorphin-and-kappa-opioid-receptor-mrna-expression-in-the-brain-relates-to-social-status-and-behavior-in-male-european-starlings
#18
Lauren V Riters, Melissa A Cordes, Sharon A Stevenson
Numerous animal species display behavioral changes in response to changes in social status or territory possession. For example, in male European starlings only males that acquire nesting sites display high rates of sexual and agonistic behavior. Past studies show that mu and delta opioid receptors regulate behaviors associated with social ascension or defeat. Opioids also act at kappa receptors, with dynorphin binding with the highest affinity; however, the role of these opioids in social behavior has not been well studied...
March 1, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/27862489/amygdala-mu-opioid-receptors-mediate-the-motivating-influence-of-cue-triggered-reward-expectations
#19
Nina T Lichtenberg, Kate M Wassum
Environmental reward-predictive stimuli can retrieve from memory a specific reward expectation that allows them to motivate action and guide choice. This process requires the basolateral amygdala (BLA), but little is known about the signaling systems necessary within this structure. Here we examined the role of the neuromodulatory opioid receptor system in the BLA in such cue-directed action using the outcome-specific Pavlovian-to-instrumental transfer (PIT) test in rats. Inactivation of BLA mu-, but not delta-opioid receptors was found to dose-dependently attenuate the ability of a reward-predictive cue to selectively invigorate the performance of actions directed at the same unique predicted reward (i...
February 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/27852962/anatomy-and-immunochemical-characterization-of-the-non-arterial-peptidergic-diffuse-dural-innervation-of-the-rat-and-rhesus-monkey-implications-for-functional-regulation-and-treatment-in-migraine
#20
Frank L Rice, Jennifer Y Xie, Phillip J Albrecht, Emily Acker, Justin Bourgeois, Edita Navratilova, David W Dodick, Frank Porreca
OBJECTIVE: The interplay between neuronal innervation and other cell types underlies the physiological functions of the dura mater and contributes to pathophysiological conditions such as migraine. We characterized the extensive, but understudied, non-arterial diffuse dural innervation (DDI) of the rat and Rhesus monkey. METHODS: We used a comprehensive integrated multi-molecular immunofluorescence labeling strategy to extensively profile the rat DDI and to a lesser extent that of the Rhesus monkey...
November 16, 2016: Cephalalgia: An International Journal of Headache
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