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Opioid antagonism

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https://www.readbyqxmd.com/read/29155273/mu-opioid-peptide-mop-and-nociceptin-orphanin-fq-peptide-nop-receptor-activation-both-contribute-to-the-discriminative-stimulus-properties-of-cebranopadol-in-the-rat
#1
Thomas M Tzschentke, Kris Rutten
The novel potent analgesic cebranopadol is an agonist at nociceptin/orphanin FQ peptide (NOP) and classical opioid receptors, with the highest in-vitro activity at NOP and mu-opioid peptide (MOP) receptors, and somewhat lower activity at kappa-opioid peptide (KOP) and delta-opioid peptide (DOP) receptors. We addressed the question of which of these pharmacological activities contribute to the stimulus properties of cebranopadol using a rat drug discrimination procedure. First, cebranopadol was tested in generalization tests against a morphine cue, including receptor-specific antagonism...
November 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29146290/sustained-opioid-antagonism-modulates-striatal-sensitivity-to-baby-schema-in-opioid-use-disorder
#2
An-Li Wang, Steven B Lowen, Igor Elman, Zhenhao Shi, Victoria P Fairchild, Alexander Bouril, Ruben C Gur, Daniel D Langleben
BACKGROUND: Chronic opioid misuse is associated with reduced sensitivity to natural rewards and social motivation deficits that include impaired caregiving. The neurobiological mechanisms underlying these deficits and their response to treatment are not well understood. Baby schema (Kindchenschema) is a set of juvenile physical features, which is perceived as "cute" and triggers motivation for caregiving. Recent studies suggest that the "baby schema effect" is mediated by the brain "reward" network...
October 18, 2017: Journal of Substance Abuse Treatment
https://www.readbyqxmd.com/read/29100992/antagonism-of-the-kappa-opioid-receptor-attenuates-thc-induced-place-aversions-in-adult-male-sprague-dawley-rats
#3
Matthew M Clasen, Shaun M Flax, Briana J Hempel, Kejun Cheng, Kenner C Rice, Anthony L Riley
RATIONALE: Prior research with transgenic mice in which the kappa opioid receptor (KOR) has been suppressed or activated suggests that the aversive effects of THC are mediated by activity of this receptor subtype. If the activity of the KOR system is responsible for mediating the THC's aversive effects, then selective antagonism of the KOR by norBNI should block such aversive effects. To test this hypothesis, rats were pretreated with norBNI 24h prior to place conditioning with THC to assess its effect on the acquisition of THC-induced place aversions...
October 31, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29042247/murine-genetic-variance-in-muscarinic-cholinergic-receptor-antagonism-of-sucrose-and-saccharin-solution-intakes-in-three-inbred-mouse-strains
#4
Faye Bourie, Kerstin Olsson, Ben Iskhakov, Agata Buras, Gabriela Fazilov, Merna Shenouda, Julia Zhezherya, Richard J Bodnar
Nutritive (e.g., sucrose) and non-nutritive (e.g., saccharin) sweeteners stimulate intake in inbred mouse strains. BALB/c, SWR and C57BL/6 mice differ in the ability of dopamine (DA) D1 (SCH23390) and opioid (naltrexone) receptor antagonism to alter sucrose intake. Whereas SCH23390 comparably reduced cumulative sucrose intake in all three strains, naltrexone reduced cumulative sucrose intake maximally in C57/BL/6 mice, in intermediate fashion in BALB/c mice, but not in SWR mice. Whereas cumulative saccharin intake was reduced by DA D1 receptor antagonism in BALB/c and SWR mice, naltrexone was more potent in SWR relative to BALB/c mice...
October 16, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28991118/truncated-%C3%AE-opioid-receptors-with-6-transmembrane-domains-are-essential-for-opioid-analgesia
#5
Zhigang Lu, Jin Xu, Mingming Xu, Grace C Rossi, Susruta Majumdar, Gavril W Pasternak, Ying-Xian Pan
BACKGROUND: Most clinical opioids act through μ-opioid receptors. They effectively relieve pain but are limited by side effects, such as constipation, respiratory depression, dependence, and addiction. Many efforts have been made toward developing potent analgesics that lack side effects. Three-iodobenzoyl-6β-naltrexamide (IBNtxA) is a novel class of opioid active against thermal, inflammatory, and neuropathic pain, without respiratory depression, physical dependence, and reward behavior...
October 4, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28986667/prolonged-release-oxycodone-naloxone-improves-anal-sphincter-relaxation-compared-to-oxycodone-plus-macrogol-3350
#6
RANDOMIZED CONTROLLED TRIAL
Jakob Lykke Poulsen, Christina Brock, Debbie Grønlund, Donghua Liao, Hans Gregersen, Klaus Krogh, Asbjørn Mohr Drewes
BACKGROUND: Opioid analgesics inhibit anal sphincter function and contribute to opioid-induced bowel dysfunction (OIBD). However, it is unknown whether the inhibition can be reduced by opioid antagonism with prolonged-release (PR) naloxone and how this compares to laxative treatment. AIMS: To compare the effects of combined PR oxycodone/naloxone or PR oxycodone plus macrogol 3350 on anal sphincter function and gastrointestinal symptoms. METHODS: A randomized, double-blind, crossover trial was conducted in 20 healthy men...
November 2017: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/28965364/bupropion-for-attention-deficit-hyperactivity-disorder-adhd-in-adults
#7
REVIEW
Wim Verbeeck, Geertruida E Bekkering, Wim Van den Noortgate, Cornelis Kramers
BACKGROUND: Attention deficit hyperactivity disorder (ADHD) is a prevalent neurobiological condition, characterised by behavioral and cognitive symptoms such as inattention, impulsivity and/or excessive activity. The syndrome is commonly accompanied by psychiatric comorbidities and is associated with educational and occupational underachievement.Although psychostimulant medications are the mainstay of treatment for ADHD, not all adults respond optimally to, or can tolerate, these medicines...
October 2, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28958601/ghrelin-receptor-antagonism-of-morphine-induced-conditioned-place-preference-and-behavioral-and-accumbens-dopaminergic-sensitization-in-rats
#8
Pavel Jerabek, Tereza Havlickova, Nina Puskina, Chrysostomos Charalambous, Marek Lapka, Petr Kacer, Magdalena Sustkova-Fiserova
An increasing number of studies over the past few years have demonstrated ghrelin's role in alcohol, cocaine and nicotine abuse. However, the role of ghrelin in opioid effects has rarely been examined. Recently we substantiated in rats that ghrelin growth hormone secretagogue receptors (GHS-R1A) appear to be involved in acute opioid-induced changes in the mesolimbic dopaminergic system associated with the reward processing. The aim of the present study was to ascertain whether a ghrelin antagonist (JMV2959) was able to inhibit morphine-induced biased conditioned place preference and challenge-morphine-induced accumbens dopaminergic sensitization and behavioral sensitization in adult male rats...
September 27, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/28946783/peripherally-acting-%C3%A2%C2%B5-opioid-receptor-antagonists-for-the-treatment-of-opioid-related-side-effects-mechanism-of-action-and-clinical-implications
#9
John M Streicher, Edward J Bilsky
Opioid receptors are distributed throughout the central and peripheral nervous systems and on many nonneuronal cells. Therefore, opioid administration induces effects beyond analgesia. In the enteric nervous system (ENS), stimulation of µ-opioid receptors triggers several inhibitory responses that can culminate in opioid-induced bowel dysfunction (OBD) and its most common side effect, opioid-induced constipation (OIC). OIC negatively affects patients' quality of life (QOL), ability to work, and pain management...
January 1, 2017: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/28891868/bivalent-ligand-that-activates-mu-opioid-receptor-and-antagonizes-mglur5-receptor-reduces-neuropathic-pain-in-mice
#10
Cristina D Peterson, Kelley F Kitto, Eyup Akgün, Mary M Lunzer, Maureen S Riedl, Lucy Vulchanova, George L Wilcox, Philip S Portoghese, Carolyn A Fairbanks
The mu opioid receptor (MOR) and metabotropic glutamate receptor 5 (mGluR5) are well-established pharmacological targets in the management of chronic pain. Both receptors are expressed in the spinal cord. MMG22, a bivalent ligand containing 2 pharmacophores separated by 22 atoms, which simultaneously activates MOR and antagonizes mGluR5, has been shown to produce potent reversal of tactile hypersensitivity in rodent models of lipopolysaccharide (LPS)-and bone cancer-induced chronic pain. This study assessed whether intrathecal MMG22 also is effective in reducing pain of neuropathic origin...
December 2017: Pain
https://www.readbyqxmd.com/read/28888954/central-antagonism-of-orexin-type-1-receptors-attenuates-the-development-of-morphine-dependence-in-rat-locus-coeruleus-neurons
#11
Mojgan Fakhari, Hossein Azizi, Saeed Semnanian
Prolonged use/abuse of opioid agonists leads to development of severe dependence to these drugs. Orexin-A has a crucial role in development of morphine dependence. The locus coeruleus (LC) is implicated in the expression of morphine withdrawal signs. Hyperactivity of LC neurons as well as increased intracellular cyclic adenosine monophosphate (cAMP) level temporally corresponds to the expression of opioid withdrawal behaviors. In this study the effect of central OX1R blockade on neuronal activity and cAMP content of LC neurons was investigated following naloxone administration in morphine-dependent rats...
November 5, 2017: Neuroscience
https://www.readbyqxmd.com/read/28888771/c-terminal-hydrazide-modification-changes-the-spinal-antinociceptive-profiles-of-endomorphins-in-mice
#12
Chang-Lin Wang, Dai-Jun Yang, Bi-Yu Yuan, Yu Wang
Previously, we have demonstrated that endomorphins (EMs) analogs with C-terminal hydrazide modification retained the μ-opioid receptor affinity and selectivity, and exhibited potent antinociception after intracerebroventricular (i.c.v.) administration. In the present study, we extended our studies to evaluate the antinociceptive profiles of EMs and their analogs EM-1-NHNH2, EM-2-NHNH2 given spinally in the radiant heat paw withdrawal test. Following intrathecal (i.t.) administration, EM-1, EM-2, EM-1-NHNH2 and EM-2-NHNH2 dose-dependently increased the latency for paw withdrawal response...
September 6, 2017: Peptides
https://www.readbyqxmd.com/read/28826482/anti-nociceptive-action-of-peripheral-mu-opioid-receptors-by-g-beta-gamma-protein-mediated-inhibition-of-trpm3-channels
#13
Sandeep Dembla, Marc Behrendt, Florian Mohr, Christian Goecke, Julia Sondermann, Franziska M Schneider, Marlene Schmidt, Julia Stab, Raissa Enzeroth, Michael G Leitner, Paulina Nuñez-Badinez, Jochen Schwenk, Bernd Nürnberg, Alejandro Cohen, Stephan E Philipp, Wolfgang Greffrath, Moritz Bünemann, Dominik Oliver, Eleonora Zakharian, Manuela Schmidt, Johannes Oberwinkler
Opioids, agonists of µ-opioid receptors (µORs), are the strongest pain killers clinically available. Their action includes a strong central component, which also causes important adverse effects. However, µORs are also found on the peripheral endings of nociceptors and their activation there produces meaningful analgesia. The cellular mechanisms downstream of peripheral µORs are not well understood. Here, we show in neurons of murine dorsal root ganglia that pro-nociceptive TRPM3 channels, present in the peripheral parts of nociceptors, are strongly inhibited by µOR activation, much more than other TRP channels in the same compartment, like TRPV1 and TRPA1...
August 15, 2017: ELife
https://www.readbyqxmd.com/read/28807162/chinese-herbal-medicine-for-the-treatment-of-drug-addiction
#14
Weili Zhu, Yinan Zhang, Yingjie Huang, Lin Lu
This chapter summarizes recent developments in preclinical and clinical research on Chinese herbal medicines and their neurochemical mechanism of action for the treatment of drug addiction. We searched Chinese and English scientific literature and selected several kinds of Chinese herbal medicines that have beneficial effects on drug addiction. Ginseng (Renshen) may be clinically useful for the prevention of opioid abuse and dependence. Rhizoma Corydalis (Yanhusuo) may be used to prevent relapse to chronic drug dependence...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/28797641/b2-kinin-receptors-in-the-dorsal-periaqueductal-gray-are-implicated-in-the-panicolytic-like-effect-of-opiorphin
#15
Caio César Sestile, Jhonatan Christian Maraschin, Marcel Pereira Rangel, Rosangela Getirana Santana, Hélio Zangrossi, Frederico Guilherme Graeff, Elisabeth Aparecida Audi
Reported results have shown that the pentapeptide opiorphin inhibits oligopeptidases that degrade brain neuropeptides, and has analgesic and antidepressant effects in experimental animals, without either tolerance or dependency after chronic administration. In a previous study we showed that opiorphin has a panicolytic-like effect in the dorsal periaqueductal gray (dPAG) electrical stimulation test (EST), mediated by the μ-opioid receptor (MOR). This study further analyzes the mechanism of opiorphin panicolytic action, using the EST and drug injection inside the dPAG...
October 3, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28734666/development-of-novel-lp1-based-analogues-with-enhanced-delta-opioid-receptor-profile
#16
Lorella Pasquinucci, Rita Turnaturi, Orazio Prezzavento, Emanuela Arena, Giuseppina Aricò, Zafiroula Georgoussi, Rosalba Parenti, Giuseppina Cantarella, Carmela Parenti
Pain relief achieved by co-administration of drugs acting at different targets is more effective than that obtained with conventional MOR selective agonists usually associated to relevant side effects. It has been demonstrated that simultaneously targeting different opioid receptors is a more effective therapeutic strategy. Giving the promising role for DOR in pain management, novel LP1-based analogues with different N-substituents were designed and synthesized with the aim to improve DOR profile. For this purpose, we maintained the phenyl ring in the N-substituent of 6,7-benzomorphan scaffold linked to an ethyl spacer bearing a hydroxyl/methyl or methoxyl group at carbon 2 or including it in a 1,4-benzodioxane ring...
September 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28716934/sigma-1-receptors-control-immune-driven-peripheral-opioid-analgesia-during-inflammation-in-mice
#17
Miguel A Tejada, Angeles Montilla-García, Shane J Cronin, Domagoj Cikes, Cristina Sánchez-Fernández, Rafael González-Cano, M Carmen Ruiz-Cantero, Josef M Penninger, José M Vela, José M Baeyens, Enrique J Cobos
Sigma-1 antagonism potentiates the antinociceptive effects of opioid drugs, so sigma-1 receptors constitute a biological brake to opioid drug-induced analgesia. The pathophysiological role of this process is unknown. We aimed to investigate whether sigma-1 antagonism reduces inflammatory pain through the disinhibition of the endogenous opioidergic system in mice. The selective sigma-1 antagonists BD-1063 and S1RA abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute (3 h) inflammation...
August 1, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28716608/opioidergic-and-dopaminergic-modulation-of-cost-benefit-decision-making-in-long-evans-rats
#18
Ileana Morales, Paul J Currie, Timothy D Hackenberg, Raúl Pastor
Eating disorders are associated with impaired decision-making and dysfunctional reward-related neurochemistry. The present study examined the potential contributions of dopamine and opioid signaling to these processes using two different decision-making tasks. In one task, Long Evans Rats chose between working for a preferred food (high-carbohydrate banana-flavored sucrose pellets) by lever pressing on a progressive-ratio schedule of reinforcement vs. obtaining less preferred laboratory chow that was concurrently available...
July 14, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28714716/cb%C3%A2-receptor-antagonism-in-the-bed-nucleus-of-the-stria-terminalis-interferes-with-affective-opioid-withdrawal-in-rats
#19
Kiri L Wills, Marieka V DeVuono, Cheryl L Limebeer, Kiran Vemuri, Alexandros Makriyannis, Linda A Parker
The bed nucleus of the stria terminalis (BNST) is a region of the extended amygdala that is implicated in addiction, anxiety, and stress related behaviors. This region has been identified in mediating the aversive state of naloxone-precipitated morphine withdrawal (MWD) and cannabinoid Type I (CB1) receptors have been found to modulate neurotransmission within this region. Previous findings suggest that the CB1 antagonist/inverse agonist, AM251, administered systemically or by infusion into the central nucleus of the amygdala (CeA) prevented the aversive affective properties of MWD as measured by conditioned place aversion learning...
August 2017: Behavioral Neuroscience
https://www.readbyqxmd.com/read/28680103/chemogenetic-silencing-of-gabaergic-dorsal-horn-interneurons-induces-morphine-resistant-spontaneous-nocifensive-behaviours
#20
Keisuke Koga, Kensho Kanehisa, Yuta Kohro, Miho Shiratori-Hayashi, Hidetoshi Tozaki-Saitoh, Kazuhide Inoue, Hidemasa Furue, Makoto Tsuda
Inhibitory interneurons in the spinal dorsal horn (SDH) are crucial for processing somatosensory information originating in the periphery. However, the effects of the acute and selective inactivation of GABAergic SDH interneurons on pain processing are not fully understood. In this study, we used designer receptors exclusively activated by designer drugs (DREADD) technology and vesicular GABA transporter-Cre (Vgat-Cre) mice to selectively express a modified human muscarinic Gi protein-coupled receptor (hM4Di) in Vgat-Cre (+) GABAergic SDH interneurons in the fourth lumbar segment...
July 5, 2017: Scientific Reports
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