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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
#1
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
#2
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/29681324/expectancy-modulation-of-opioid-neurotransmission
#3
Marta Pecina, Jon-Kar Zubieta
Expectancies are powerful modulators of cognitive and emotional experiences, as well as the neurobiological responses linked to these processes. In medicine, placebo effects are a clear example of how expectancies activate opioid neurotransmission in a treatment context, leading to the experience of analgesia and the improvement of emotional states, among other symptoms. Molecular neuroimaging techniques using positron emission tomography (PET) and the selective μ-opioid receptor tracer [11 C]carfentanil have significantly contributed to our understanding of the neurobiological systems involved in the formation of placebo effects...
2018: International Review of Neurobiology
https://www.readbyqxmd.com/read/29680426/willis-ekbom-disease-restless-legs-syndrome-in-patients-with-opioid-withdrawal
#4
Ravi Gupta, Ramjan Ali, Rajat Ray
INTRODUCTION: Many patients with opioid use disorder report symptoms similar to restless legs syndrome (RLS) during withdrawal. However, whether these symptoms are true RLS, their predictors and effect of treatment with pregabalin are still unknown. METHOD: A total of 19 consecutive patients with opioid use disorder who were admitted for detoxification were included in this study after obtaining informed consent. Information regarding addiction was noted, and they were screened for RLS every morning and evening...
May 2018: Sleep Medicine
https://www.readbyqxmd.com/read/29679881/ventrolateral-orbital-cortex-oxytocin-attenuates-neuropathic-pain-through-periaqueductal-gray-opioid-receptor
#5
Mina Taati, Esmaeal Tamaddonfard
BACKGROUND: Oxytocin plays an important role in supraspinal modulation of pain. In the present study, we investigated the effects of ventrolateral orbital cortex (VLOC) microinjection of oxytocin on neuropathic pain after blockade of opioid receptors in this area and ventrolateral periaqueductal gray (vlPAG). METHODS: Neuropathic pain was induced by complete transcection of preoneal and tibial branches of sciatic nerve. The VLOC and vlPAG were unilaterally (contralateral to the sciatic nerve-injured side) and bilaterally implanted with guide cannulas, respectively...
December 21, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29679289/cross-state-dependency-of-learning-between-tramadol-and-mk-801-in-the-mouse-dorsal-hippocampus-involvement-of-nitric-oxide-no-signaling-pathway
#6
Majid Jafari-Sabet, Shiva Amiri, Ramin Ataee
RATIONALE: Tramadol, an atypical μ-opioid receptor agonist, as a psychoactive drug, is frequently abused by human beings. Understanding the neurobiological mechanisms of drug-associated learning and memory formation may help prevent drug addiction and relapse. Previous study revealed that dorsal hippocampus (CA1) plays a crucial role in the retrieval of tramadol-associated memory and that its role depends on the expression of CA1 N-methyl-D-aspartate (NMDA) receptors (Jafari-Sabet et al...
April 21, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29678771/prenatal-ethanol-induces-an-anxiety-phenotype-and-alters-expression-of-dynorphin-nociceptin-orphanin-fq-genes
#7
Aranza Wille-Bille, Roberto Sebastián Miranda-Morales, Mariangela Pucci, Fabio Bellia, Claudio D'Addario, Ricardo Marcos Pautassi
Animal models have suggested that prenatal ethanol exposure (PEE) alters the κ opioid receptor system. The present study investigated the brain expression of dynorphin and nociceptin/orphanin FQ related genes and assessed anxiety-like behavior in the light-dark box (LDB), shelter-seeking and risk-taking behaviors in the concentric square field (CSF) test, and ethanol-induced locomotion in the open field (OF), in infant or adolescent Wistar rats that were exposed to PEE (0.0 or 2.0 g/kg, intragastrically, gestational days 17-20)...
April 17, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
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
#8
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/29677019/mu-opioid-receptors-in-nociceptive-afferents-produce-a-sustained-suppression-of-hyperalgesia-in-chronic-pain
#9
Amie Severino, Wenling Chen, Joshua K Hakimian, Brigitte L Kieffer, Claire Gaveriaux-Ruff, Wendy Walwyn, Juan Carlos Marvizon
The latent sensitization model of chronic pain reveals that recovery from some types of long-term hyperalgesia is an altered state in which nociceptive sensitization persists but is suppressed by the ongoing activity of analgesic receptors such as µ-opioid receptors (MORs). To determine whether these MORs are the ones present in nociceptive afferents, we bred mice expressing Cre-recombinase under the Nav1.8 channel promoter (Nav1.8cre) with MOR-floxed mice (flMOR). These Nav1.8cre/flMOR mice had reduced MOR expression in primary afferents, as revealed by quantitative PCR, in situ hybridization and immunofluorescence colocalization with the neuropeptide CGRP...
April 17, 2018: Pain
https://www.readbyqxmd.com/read/29675582/multifunctional-opioid-ligands
#10
Jessica P Anand, Deanna Montgomery
The opioid receptor system plays a major role in the regulation of mood, reward, and pain. The opioid receptors therefore make attractive targets for the treatment of many different conditions, including pain, depression, and addiction. However, stimulation or blockade of any one opioid receptor type often leads to on-target adverse effects that limit the clinical utility of a selective opioid agonist or antagonist. Literature precedent suggests that the opioid receptors do not act in isolation and that interactions among the opioid receptors and between the opioid receptors and other proteins may produce clinically useful targets...
April 20, 2018: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/29669731/involvement-of-activated-brain-stress-responsive-systems-in-excessive-and-relapse-alcohol-drinking-in-rodent-models-implications-for-therapeutics
#11
Yan Zhou, Mary Jeanne Kreek
Addictive diseases, including addiction to alcohol pose massive public health costs. Addiction is a chronic relapsing disease, caused by both the direct effects induced by drugs and persistent neuroadaptations at several (molecular, cellular and behavioral) levels. These drug-type specific neuro-adaptations are brought on largely by the reinforcing effects of drugs on the central nervous system and environment, including stress. Results from animal experiments have demonstrated important interactions between alcohol and the stress responsive systems...
April 18, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29669290/non-canonical-opioid-signaling-inhibits-itch-transmission-in-the-spinal-cord-of-mice
#12
Admire Munanairi, Xian-Yu Liu, Devin M Barry, Qianyi Yang, Jun-Bin Yin, Hua Jin, Hui Li, Qing-Tao Meng, Jia-Hang Peng, Zhen-Yu Wu, Jun Yin, Xuan-Yi Zhou, Li Wan, Ping Mo, Seungil Kim, Fu-Quan Huo, Joseph Jeffry, Yun-Qing Li, Rita Bardoni, Michael R Bruchas, Zhou-Feng Chen
Chronic itch or pruritus is a debilitating disorder that is refractory to conventional anti-histamine treatment. Kappa opioid receptor (KOR) agonists have been used to treat chronic itch, but the underlying mechanism remains elusive. Here, we find that KOR and gastrin-releasing peptide receptor (GRPR) overlap in the spinal cord, and KOR activation attenuated GRPR-mediated histamine-independent acute and chronic itch in mice. Notably, canonical KOR-mediated Gαi signaling is not required for desensitizing GRPR function...
April 17, 2018: Cell Reports
https://www.readbyqxmd.com/read/29667742/genetic-association-and-expression-analyses-of-the-phosphatidylinositol-4-phosphate-5-kinase-pip5k1c-gene-in-alcohol-use-disorder-relevance-for-pain-signaling-and-alcohol-use
#13
Ji Soo Lee, Jill L Sorcher, Allison D Rosen, Ruslan Damadzic, Hui Sun, Melanie Schwandt, Markus Heilig, John Kelly, Kelsey L Mauro, Audrey Luo, Daniel Rosoff, Christine Muench, Jeesun Jung, Zachary A Kaminsky, Falk W Lohoff
BACKGROUND: The gene encoding Phosphatidylinositol-4-Phosphate 5-Kinase (PIP5K1C) has been recently implicated in pain regulation. Interestingly, a recent cross-tissue and cross-phenotypic epigenetic analysis identified the same gene in alcohol use disorder (AUD). Given the high comorbidity between AUD and chronic pain, we hypothesized that genetic variation in PIP5K1C might contribute to susceptibility to AUD. METHODS: We conducted a case-control association study of genetic variants in PIP5K1C...
April 18, 2018: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29663822/the-effect-of-intrathecal-sufentanil-preconditioning-against-myocardial-ischemia-reperfusion-injury
#14
Y Tire, G Sarkilar, H Esen, R Onoglu, S T Uzun
OBJECTIVES: We aimed to investigate the cardioprotective effect and hemodynamic response of intrathecally administered sufentanil on myocardial IR injury. BACKGROUND: Sufentanil, mu opioid receptor agonist, intravenously administered during clinical and experimental studies, has been shown to have a cardioprotective effect on myocardial ischemia-reperfusion injury. METHODS: Thirty-two New Zealand type rabbits, which were anesthetized, were divided into four equal groups: sham, ischemia-reperfusion, sufentanil and ischemia-reperfusion+sufentanil...
2018: Bratislavské Lekárske Listy
https://www.readbyqxmd.com/read/29663077/is-patient-reported-outcome-improved-by-nalfurafine-hydrochloride-in-patients-with-primary-biliary-cholangitis-and-refractory-pruritus-a-post-marketing-single-arm-prospective-study
#15
Minami Yagi, Atsushi Tanaka, Tadashi Namisaki, Atsushi Takahashi, Masanori Abe, Akira Honda, Yasushi Matsuzaki, Hiromasa Ohira, Hitoshi Yoshiji, Hajime Takikawa
BACKGROUND: Patients with primary biliary cholangitis (PBC) frequently suffer from pruritus, which can severely impair their health-related quality of life (HRQOL). Nalfurafine hydrochloride, a selective κ-opioid receptor agonist, was recently approved in Japan for refractory pruritus in patients with chronic liver diseases, but it still remains unclear whether this treatment improves the patient-reported outcome (PRO) in PBC patients with refractory pruritus. Herein, we conducted a multicenter, post-marketing, single-arm prospective study to investigate the efficacy of nalfurafine in terms of PRO, and the associations of the efficacy with any clinical characteristics...
April 16, 2018: Journal of Gastroenterology
https://www.readbyqxmd.com/read/29662095/%C3%AE-opioid-receptor-system-mediates-reward-processing-in-humans
#16
Lauri Nummenmaa, Tiina Saanijoki, Lauri Tuominen, Jussi Hirvonen, Jetro J Tuulari, Pirjo Nuutila, Kari Kalliokoski
The endogenous μ-opioid receptor (MOR) system regulates motivational and hedonic processing. We tested directly whether individual differences in MOR are associated with neural reward responses to food pictures in humans. We scanned 33 non-obese individuals with positron emission tomography (PET) using the MOR-specific radioligand [11 C]carfentanil. During a functional magnetic resonance imaging (fMRI) scan, the subjects viewed pictures of appetizing versus bland foods to elicit reward responses. MOR availability was measured in key components of the reward and emotion circuits and used to predict BOLD-fMRI responses to foods...
April 16, 2018: Nature Communications
https://www.readbyqxmd.com/read/29659201/evaluation-of-eluxadoline-effect-on-cardiac-repolarization
#17
Laura Bonifacio, Thomas L Hunt, Gail McIntyre, Leonard S Dove, Paul S Covington
This study evaluated the effects of eluxadoline, a mixed μ-opioid receptor (OR) and κ-OR agonist and δ-OR antagonist, on cardiac repolarization. This evaluator-blinded, placebo- and positive-controlled, 4-period crossover study randomized healthy men and women to single oral doses of eluxadoline (therapeutic dose 100 mg or supratherapeutic dose 1000 mg), moxifloxacin 400 mg, or placebo. QT data were corrected using individual custom correction (QTcI). The primary endpoint was the change from baseline in QTcI intervals (ΔQTcI) between eluxadoline and placebo (ΔΔQTcI)...
April 16, 2018: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29655552/binge-eating-disorder-and-morbid-obesity-are-associated-with-lowered-mu-opioid-receptor-availability-in-the-brain
#18
Juho Joutsa, Henry K Karlsson, Joonas Majuri, Pirjo Nuutila, Semi Helin, Valtteri Kaasinen, Lauri Nummenmaa
Both morbid obesity and binge eating disorder (BED) have previously been linked with aberrant brain opioid function. Behaviorally these two conditions are however different suggesting also differences in neurotransmitter function. Here we directly compared mu-opioid receptor (MOR) availability between morbidly obese and BED subjects. Seven BED and nineteen morbidly obese (non-BED) patients, and thirty matched control subjects underwent positron emission tomography (PET) with MOR-specific ligand [11 C]carfentanil...
March 9, 2018: Psychiatry research. Neuroimaging
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
#19
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/29651005/differential-effect-of-morphine-on-gastrointestinal-transit-colonic-contractions-and-nerve-evoked-relaxations-in-toll-like-receptor-deficient-mice
#20
Elizabeth A H Beckett, Vasiliki Staikopoulos, Mark R Hutchinson
Toll-like receptors (TLRs) are expressed in enteric neurons, glia, gastrointestinal (GI) smooth muscle and mucosa, yet their functional roles in the GI tract are not fully understood. TLRs have been linked to many of the undesirable central effects of chronic opioid administration including hyperalgesia and dependence via activation of central microglia. Opioid-induced bowel dysfunction (OIBD) remains a primary reason for the reduction or withdrawal of opioid analgesics. Morphine-induced inhibition of colonic motility was assessed in vivo by GI transit studies and in vitro using isolated colons from wildtype (WT) and TLR deficient mice...
April 12, 2018: Scientific Reports
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