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https://www.readbyqxmd.com/read/29686629/critical-role-for-g-i-o-protein-activity-in-the-dorsal-striatum-in-the-reduction-of-voluntary-alcohol-intake-in-c57bl-6-mice
#1
Meridith T Robins, Terrance Chiang, Kendall L Mores, Doungkamol Alongkronrusmee, Richard M van Rijn
The transition from non-dependent alcohol use to alcohol dependence involves increased activity of the dorsal striatum. Interestingly, the dorsal striatum expresses a large number of inhibitory G-protein-coupled receptors (GPCRs), which when activated may inhibit alcohol-induced increased activity and can decrease alcohol consumption. Here, we explore the hypothesis that dorsal striatal Gi/o -protein activation is sufficient to reduce voluntary alcohol intake. Using a voluntary, limited-access, two-bottle choice, drink-in-the-dark model of alcohol (10%) consumption, we validated the importance of Gi/o signaling in this region by locally expressing neuron-specific, adeno-associated-virus encoded Gi/o -coupled muscarinic M4 designer receptors exclusively activated by designer drugs (DREADD) in the dorsal striatum and observed a decrease in alcohol intake upon DREADD activation...
2018: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29684591/in-vitro-and-in-vivo-activity-of-opioid-cyclopeptide-with-mu-delta-agonist-profile-biased-toward-%C3%AE-arrestin
#2
Katarzyna Gach-Janczak, Justyna Piekielna-Ciesielska, Anna Adamska-Bartłomiejczyk, Karol Wtorek, Federica Ferrari, Girolamo Calo, Agata Szymaszkiewicz, Joanna Piasecka-Zelga, Anna Janecka
Replacement of the tyrosine residue in the mu-selective opioid ligand Tyr-c[D-Lys-Phe-Asp]NH2 with 2',6'-dimethyltyrosine (Dmt) produced a cyclopeptide Dmt-c[D-Lys-Phe-Asp]NH2 with mu/delta opioid receptor agonist profile. This new analog showed improved antinociception in the hot-plate test as compared to the parent but also significantly inhibited the gastrointestinal transit. Using the bioluminescence resonance energy transfer (BRET) assay it was shown that this analog was biased toward β-arrestin.
April 20, 2018: Peptides
https://www.readbyqxmd.com/read/29681795/delta-opioid-receptor-signaling-promotes-resilience-to-stress-under-the-repeated-social-defeat-paradigm-in-mice
#3
Mathilde S Henry, Kanchan Bisht, Nathalie Vernoux, Louis Gendron, Angélica Torres-Berrio, Guy Drolet, Marie-Ève Tremblay
The adaptation to chronic stress is highly variable across individuals. Resilience to stress is a complex process recruiting various brain regions and neurotransmitter systems. The aim of this study was to investigate the involvement of endogenous opioid enkephalin (ENK) signaling in the development of stress resilience in mice. The translational model of repeated social defeat (RSD) stress was selected to mimic the unpredictable disruptions of daily life and induce resilience or vulnerability to stress. As in humans, adult C57BL/6J mice demonstrated a great variability in their response to stress under this paradigm...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29677442/synthesis-and-pharmacological-evaluation-of-novel-c-8-substituted-tetrahydroquinolines-as-balanced-affinity-mu-delta-opioid-ligands-for-the-treatment-of-pain
#4
Anthony F Nastase, Nicholas W Griggs, Jessica P Anand, Thomas J Fernandez, Aubrie A Harland, Tyler J Trask, Emily M Jutkiewicz, John R Traynor, Henry I Mosberg
The use of opioids for the treatment of pain, while largely effective, is limited by detrimental side effects including analgesic tolerance, physical dependence, and euphoria, which may lead to opioid abuse. Studies have shown that compounds with a -opioid receptor (MOR) agonist/-opioid receptor (DOR) antagonist profile reduce or eliminate some of these side effects including development of tolerance and dependence. Herein we report the synthesis and pharmacological evaluation of a series of tetrahydroquinoline-based peptidomimetics with substitutions at the C-8 position...
April 20, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29664203/trends-and-patterns-of-opioid-analgesic-prescribing-regional-and-rural-urban-variations-in-kentucky-from-2012-to-2015
#5
Huong Luu, Svetla Slavova, Patricia R Freeman, Michelle Lofwall, Steven Browning, Heather Bush
PURPOSE: Increased opioid analgesic prescribing (OAP) has been associated with increased risk of prescription opioid diversion, misuse, and abuse. We studied regional and rural-urban variations in OAP trends in Kentucky, from 2012 to 2015, and examined potential county-level risk and protective factors. METHODS: This study used prescription drug monitoring data. Marginal models employing generalized estimating equations were used to model repeated counts of residents with opioid analgesic prescriptions within county-quarter, 2012-2015, with offset for resident population, by rural-urban classification exposure, and adjusting for time-varying socioeconomic and relevant health status measures...
April 17, 2018: Journal of Rural Health
https://www.readbyqxmd.com/read/29659874/carfentanil-in-impaired-driving-cases-and-the-importance-of-drug-seizure-data
#6
Nicholas B Tiscione, Ilene Alford
Drug seizures containing carfentanil continue to increase in Palm Beach County, FL, USA despite international efforts to control the distribution of the drug. The analysis of drug seizures from the county in 2016 and 2017 demonstrated that carfentanil was the most commonly identified fentanyl analog and was most often detected in combination with heroin, fentanyl, furanyl fentanyl and/or other fentanyl analogs. Carfentanil is an ultra-potent opioid requiring a method with adequate sensitivity for detection in blood specimens from impairment cases...
April 12, 2018: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29651609/the-delta-opioid-peptide-dadle-represses-hypoxia-reperfusion-mimicked-stress-mediated-apoptotic-cell-death-in-human-mesenchymal-stem-cells-in-part-by-downregulating-the-unfolded-protein-response-and-ros-along-with-enhanced-anti-inflammatory-effect
#7
Madhubanti Mullick, Dwaipayan Sen
Hypoxia-reperfusion (H/R) emblems a plethora of pathological conditions which is potent in contributing to the adversities encountered by human mesenchymal stem cells (hMSCs) in post-transplant microenvironment, resulting in transplant failure. D-Alanine 2, Leucine 5 Enkephaline (DADLE)-mediated delta opioid receptor (DOR) activation is well-known for its recuperative properties in different cell types like neuronal and cardiomyocytes. In the current study its effectiveness in assuaging hMSC mortality under H/R-like insult has been delineated...
April 12, 2018: Stem Cell Reviews
https://www.readbyqxmd.com/read/29649744/synthesis-of-7%C3%AE-hydroxy-8-ketone-opioid-derivatives-with-antagonist-activity-at-mu-and-delta-opioid-receptors
#8
Tiina J Ahonen, Maiju Rinne, Peter Grutschreiber, Kert Mätlik, Mikko Airavaara, Dieter Schaarschmidt, Heinrich Lang, David Reiss, Henri Xhaard, Claire Gaveriaux-Ruff, Jari Yli-Kauhaluoma, Vânia M Moreira
Despite extensive years of research, the direct oxidation of the 7,8-double bond of opioids has so far received little attention and knowledge about the effects of this modification on activity at the different opioid receptors is scarce. We herein report that potassium permanganate supported on iron(II) sulfate heptahydrate can be used as a convenient oxidant in the one-step, heterogeneous conversion of Δ7,8 -opioids to the corresponding 7β-hydroxy-8-ketones. Details of the reaction mechanism are given and the effects of the substituent at position 6 of several opioids on the reaction outcome is discussed...
March 26, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29627297/neuropharmacological-effects-of-essential-oil-from-the-leaves-of-croton-conduplicatus-kunth-and-possible-mechanisms-of-action-involved
#9
Raimundo Gonçalves de Oliveira Júnior, Christiane Adrielly Alves Ferraz, Juliane Cabral Silva, Roxana Braga de Andrade Teles, Mariana Gama E Silva, Tâmara Coimbra Diniz, Uiliane Soares Dos Santos, Ana Valéria Vieira de Souza, Carlos Eduardo Pereira Nunes, Marcos José Salvador, Vitor Prates Lorenzo, Lucindo José Quintans Junior, Jackson Roberto Guedes da Silva Almeida
ETHNOPHARMACOLOGICAL RELEVANCE: Croton conduplicatus Kunth (Euphorbiaceae) is a Brazilian aromatic medicinal plant, widely known as "quebra-faca". In folk medicine, its leaves and stem-barks are used as a natural analgesic for the treatment of headaches. AIM OF THE STUDY: In this study, we describe for the first time the neuropharmacological potential of the essential oil obtained from the leaves of Croton conduplicatus (EO) in experimental models of pain, anxiety and insomnia...
April 5, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29616344/novel-pharmacological-nonopioid-therapies-in-chronic-pain
#10
REVIEW
Alan David Kaye, Elyse M Cornett, Brendon Hart, Shilpadevi Patil, Andrew Pham, Matthew Spalitta, Kenneth F Mancuso
PURPOSE OF REVIEW: Opioid use and abuse has led to a worldwide opioid epidemic. And while opioids are clinically useful when appropriately indicated, they are associated with a wide range of dangerous side effects and whether they are effective at treating or eliminating chronic pain is controversial. There has long been a need for the development of nonopioid alternative treatments for patients that live in pain, and until recently, only a few effective treatments were available. Today, there are a wide range of nonopioid treatments available including NSAIDs, acetaminophen, corticosteroids, nerve blocks, SSRIs, neurostimulators, and anticonvulsants...
April 3, 2018: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/29589835/snc80-and-naltrindole-modulate-voltage-dependent-sodium-potassium-and-calcium-channels-via-a-putatively-delta-opioid-receptor-independent-mechanism
#11
Lucia Moravčíková, Jana Královičová, Ľubica Lacinová
SNC80 was designed as a highly selective nonpeptide delta opioid receptor (DOR) agonist. Antidepressant-like and antinociceptive effects of this compound were demonstrated in animal models. Naltrindole was synthetized as a highly selective DOR antagonist. Its antitussive and antinociceptive effects were reported. Observed effects of SNC80 and naltrindole may be accompanied by changes in neuronal excitability including modulation of voltage-dependent ion channels. We investigated possible DOR-independent modulation of neuronal sodium, calcium and potassium currents by both agents...
March 28, 2018: General Physiology and Biophysics
https://www.readbyqxmd.com/read/29579315/co-expression-of-%C3%AE-and-%C3%A2-opioid-receptors-by-mouse-colonic-nociceptors
#12
Raquel Guerrero-Alba, Eduardo Emmanuel Valdez-Morales, Nestor Nivardo Jiménez-Vargas, Romke Bron, Daniel Poole, David Reed, Joel Castro, Melissa Campaniello, Patrick A Hughes, Stuart M Brierley, Nigel Bunnett, Alan E Lomax, Stephen Vanner
BACKGROUND AND PURPOSE: To better understand opioid signaling in visceral nociceptors, we examined the expression and selective activation of mu (MOR) and delta opioid receptors (DOR) by dorsal root ganglia (DRG) neurons innervating the mouse colon. EXPERIMENTAL APPROACH: DRG neurons projecting to the colon were identified by retrograde tracing. DOR-GFP reporter mice, in situ hybridization, single-cell RT-PCR, and MOR-specific antibodies were used to characterize expression of MOR and DOR...
March 26, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29576387/functional-divergence-of-delta-and-mu-opioid-receptor-organization-in-cns-pain-circuits
#13
Dong Wang, Vivianne L Tawfik, Gregory Corder, Sarah A Low, Amaury François, Allan I Basbaum, Grégory Scherrer
Cellular interactions between delta and mu opioid receptors (DORs and MORs), including heteromerization, are thought to regulate opioid analgesia. However, the identity of the nociceptive neurons in which such interactions could occur in vivo remains elusive. Here we show that DOR-MOR co-expression is limited to small populations of excitatory interneurons and projection neurons in the spinal cord dorsal horn and unexpectedly predominates in ventral horn motor circuits. Similarly, DOR-MOR co-expression is rare in parabrachial, amygdalar, and cortical brain regions processing nociceptive information...
March 14, 2018: Neuron
https://www.readbyqxmd.com/read/29572653/delta-mu-opioid-receptor-interactions-in-operant-conditioning-assays-of-pain-depressed-responding-and-drug-induced-rate-suppression-assessment-of-therapeutic-index-in-male-sprague-dawley-rats
#14
Katherine Cone, Janell Lanpher, Abigail Kinens, Philomena Richard, Sarah Couture, Rebecca Brackin, Emily Payne, Kylee Harrington, Kenner C Rice, Glenn W Stevenson
RATIONALE AND OBJECTIVES: Although delta/mu receptor interactions vary as a function of behavioral endpoint, there have been no assessments of these interactions using assays of pain-depressed responding. This is the first report of delta/mu interactions using an assay of pain-depressed behavior. METHODS: A mult-cycle FR10 operant schedule was utilized in the presence of (nociception) and in the absence of (rate suppression) a lactic acid inflammatory pain-like manipulation...
March 23, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29556136/secondary-metabolites-isolated-from-pinus-roxburghii-and-interpretation-of-their-cannabinoid-and-opioid-binding-properties-by-virtual-screening-and-in-vitro-studies
#15
Rola M Labib, Radhakrishnan Srivedavyasasri, Fadia S Youssef, Samir A Ross
Pinus roxburghii is highly popular as a potent analgesic and anti-inflammatory agent; however its exact mechanism of action was not fully elucidated. We aimed to interpret the analgesic and anti-inflammatory activity of the total ethanol extract of Pinus roxburghii bark (PRE) and its isolated compounds by both in silico molecular modelling and in-vitro cannabinoid and opioid binding activities evaluation for the first time. Comprehensive phytochemical investigation of PRE resulted in the isolation of sixteen compounds that were fully elucidated using1 H NMR and13 C NMR...
March 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/29547588/synthesis-and-structure-activity-relationships-of-lp1-derivatives-n-methyl-n-phenylethylamino-analogues-as-novel-mor-agonists
#16
Rita Turnaturi, Carmela Parenti, Orazio Prezzavento, Agostino Marrazzo, Paschalina Pallaki, Zafiroula Georgoussi, Emanuele Amata, Lorella Pasquinucci
The opioid pharmacological profile of cis -(-)- N -normetazocine derivatives is deeply affected by the nature of their N -substituents. Here, our efforts were focused on the synthesis and pharmacological evaluation of novel derivatives of the lead LP1, a multitarget opioid analgesic compound featuring an N -phenylpropanamido substituent. LP1 derivatives 5a - d and 6a - d were characterized by flexible groups at the N -substituent that allow them to reposition themselves relative to cis -(-)- N -normetazocine nucleus, thus producing different pharmacological profiles at the mu, delta and kappa opioid receptors (MOR, DOR and KOR) in in vitro and in vivo assays...
March 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29524334/in-vitro-and-in-vivo-characterisation-of-the-bifunctional-mop-dop-ligand-ufp-505
#17
N Dietis, H Niwa, R Tose, J McDonald, V Ruggieri, M Filaferro, G Vitale, L Micheli, C Ghelardini, S Salvadori, G Calo, R Guerrini, D J Rowbotham, D G Lambert
BACKGROUND AND PURPOSE: Targeting more than one opioid receptor type simultaneously may have analgesic advantages in reduced side effect profile. We have evaluated the mixed MOP (μ, mu) agonist/DOP (δ, delta) antagonist UFP-505 in vitro and in vivo. EXPERIMENTAL APPROACH: We measured receptor density and function in single MOP, DOP and MOP/DOP double expression systems. GTPγ35 S binding, cAMP formation and arrestin recruitment were measured. Antinociceptive activity was measured in vivo using tail withdrawal and paw pressure tests following acute and chronic treatment...
March 10, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29514324/tobacco-smoking-and-brain-endogenous-opioid-release-more-than-nicotine-alone
#18
Edward F Domino, Mika Hirasawa-Fujita
Introduction: The effects of smoking denicotinized (denic) and average nicotine (avnic) tobacco cigarettes were studied on brain mu opioid receptor binding by positron emission tomography with 11C carfentanil. The results indicated the importance of physiological and psychological effects induced by denic smoking. Methods: Regional mu opioid binding potential (non-displaceable binding potential, BPND) was measured in 20 adult male overnight abstinent chronic tobacco smokers...
March 5, 2018: Nicotine & Tobacco Research: Official Journal of the Society for Research on Nicotine and Tobacco
https://www.readbyqxmd.com/read/29513114/antinociceptive-potency-of-a-fluorinated-cyclopeptide-dmt-c-d-lys-phe-p-cf-3-phe-asp-nh-2
#19
Justyna Piekielna-Ciesielska, Adriano Mollica, Stefano Pieretti, Jakub Fichna, Agata Szymaszkiewicz, Marta Zielińska, Radzisław Kordek, Anna Janecka
Opioid peptides and opiate drugs such as morphine, mediate their analgesic effects, but also undesired side effects, mostly through activation of the mu opioid receptor. However, delta- and kappa-opioid receptors can also contribute to the analgesic effects of opioids. Recent findings showed that simultaneous activation of multiple opioid receptors may result in additional analgesia with fewer side effects. Here, we evaluated the pharmacological profile of our formerly developed mixed mu/kappa-opioid receptor ligands, Dmt-c[D-Lys-Phe-Phe-Asp]NH2 (C-36) and Dmt-c[D-Lys-Phe-p-CF3 -Phe-Asp]NH2 (F-81)...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29483406/-new-opioid-options-in-japan-methadone-tapentadol-and-hydromorphone
#20
Yusuke Takagi, Etsuko Aruga
In 2010s, several opioids became available in Japan, including methadone, tapentadol and hydromorphone. Methadone was approved in September 2012 by Japanese regulatory authority. Since methadone is positioned as so-called "step 4 opioid" in Japan, it must be prescribed as alternative opioid switched from another of 60mg/day or greater equivalent dose of oral morphine. Diversity of pharmacokinetics among individuals and various drug interactions require close monitoring of adverse events. In spite of these cautions, unique characteristics such as inhibiting N-methyl-D-aspartate(NMDA)and in- ducing internalization/degradation of mu-delta opioid receptor heterodimers underline the value of methadone in opioid switching...
February 2018: Gan to Kagaku Ryoho. Cancer & Chemotherapy
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