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Mu opioid receptor

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https://www.readbyqxmd.com/read/28529734/differential-regulation-of-mouse-and-human-mu-opioid-receptor-gene-depends-on-the-single-stranded-dna-structure-of-its-promoter-and-%C3%AE-complex-protein-1
#1
Dong-Sun Lee, Ping-Yee Law, Wei Ln, Horace H Loh, Kyu Young Song, Hack Sun Choi
The Mu opioid receptor (MOR) mediates various functions of opioid-induced analgesia, euphoria and respiratory depression, and is a major target of opioid analgesics. Understanding of MOR gene expression among species is important for understanding its analgesic function in humans. In the current study, the polypyrimidine/polypurine (PPy/u) region, a key element of MOR gene expression, was compared in humans and mice. The mouse PPy/u element is highly homologous to its human element (84%), and the mouse MOR (mMOR) reporter drives luciferase activity 35-fold more effectively than the human MOR (hMOR) reporter...
May 2017: Biomedical Reports
https://www.readbyqxmd.com/read/28506204/antibiotic-effects-of-loperamide-homology-of-human-targets-of-loperamide-with-targets-in-acanthamoeba-spp
#2
Abdul Mannan Baig, Zohaib Rana, M Mohsin Mannan, S Sumayya Tariq, H R Ahmad
BACKGROUND: Loperamide is an anti-diarrheal drug prescribed for non-infectious diarrhea. The drug is an opioid receptor agonist, a blocker of voltage-dependent calcium channel (Cav) and a calmodulin (CaM) inhibitor on human cells. Loperamide has been reported to exert anti-amoebic effects against pathogenic strains of Acanthamoeba castellanii. OBJECTIVES: The precise mode of antibiotic action, cellular target homology with human counterparts and the pattern of cell death induced by loperamide in Acanthamoeba castellanii remain to be established...
April 25, 2017: Recent Patents on Anti-infective Drug Discovery
https://www.readbyqxmd.com/read/28501425/the-effects-of-kratom-on-restraint-stress-induced-analgesia-and-its-mechanisms-of-action
#3
José Luis Vázquez López, Lorenz Schild, Thomas Günther, Stefan Schulz, Hartmud Neurath, Axel Becker
ETHNOPHARMACOLOGICAL RELEVANCE: Mitragyna speciosa and its extracts are called kratom (dried leaves, extract). They contain several alkaloids with an affinity for different opioid receptors. They are used in traditional medicine for the treatment of different diseases, as a substitute by opiate addicts, and to mitigate opioid withdrawal symptoms. Apart from their medical properties, they are used to enhance physical endurance and as a means of overcoming stress. PURPOSE: The aim of this study was to determine the mechanisms underlying the effects of kratom on restraint-stress-induced analgesia which occurs during or following exposure to a stressful or fearful stimulus...
May 10, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28488261/use-of-tramadol-in-psychiatric-care-a-comprehensive-review-and-report-of-two-cases
#4
Ansgar Rougemont-Bücking, Franziska Gamma, Jaak Panksepp
Tramadol is widely prescribed for treating acute and chronic forms of pain. It is a weak mu-receptor opioid agonist and also increases concentrations of serotonin and noradrenaline within the limbic system of the brain. The therapeutic range of tramadol is relatively wide. Compared with other opioid agonists, there is little risk for developing tolerance and for abuse. Recent models of depression emphasise the subjective experience of a depressive mood as being, in part, a psychologically painful state. It is well established that psychological stress due to social separation/loss, disruption or be-trayal of pre-existent significant interpersonal bonds is mediated by the activation of the mammalian PANIC (separation-distress) system...
May 10, 2017: Swiss Medical Weekly
https://www.readbyqxmd.com/read/28473894/role-of-%C3%AE-opioid-receptor-in-parafascicular-nucleus-of-thalamus-on-morphine-induced-antinociception-in-a-rat-model-of-acute-trigeminal-pain
#5
Esmaeal Tamaddonfard, Amir Erfanparast
The parafascicular nucleus (PFN) of thalamus, as a supraspinal structure, has an important role in processing of nociceptive information. In addition, μ-opioid receptor contributes to supraspinal modulation of nociception. In the present study, the effects of microinjection of naloxone (a non-specific opioid-receptor antagonist) and naloxonazine (a specific μ-opioid receptor antagonist) were investigated on morphine-induced antinociception in a rat model of acute trigeminal pain. Right and left sides of PFN of thalamus were implanted with two guide cannulas...
2017: Veterinary Research Forum
https://www.readbyqxmd.com/read/28466423/chronic-pruritus-current-and-emerging-treatment-options
#6
REVIEW
Manuel P Pereira, Sonja Ständer
Chronic pruritus remains a central societal issue because of its high occurrence and the substantial decrease in quality of life it may cause to affected individuals. Not only dermatological conditions, but also systemic, neurological, or psychiatric diseases may lead to chronic pruritus. Additionally, various underlying conditions may coexist or the cause may be unknown. Due to its heterogeneity, the therapeutic approach is complex and remains a challenge for the clinician. Basic measures such as emollients to avoid xerosis and treatment of the underlying disease should be initiated regardless of the duration of the symptom...
June 2017: Drugs
https://www.readbyqxmd.com/read/28457972/the-rewarding-effects-of-ethanol-are-modulated-by-binge-eating-of-a-high-fat-diet-during-adolescence
#7
M Carmen Blanco-Gandía, Juan Carlos Ledesma, Auxiliadora Aracil-Fernández, Francisco Navarrete, Sandra Montagud-Romero, Maria A Aguilar, Jorge Manzanares, José Miñarro, Marta Rodríguez-Arias
Binge-eating is considered a specific form of overeating characterized by intermittent and high caloric food intake in a short period of time. Epidemiologic studies support a positive relation between the ingestion of fat and ethanol (EtOH), specifically among adolescent subjects. The aim of this work was to clarify the role of the compulsive, limited and intermittent intake of a high-fat food during adolescence on the rewarding effects of EtOH. After binge-eating for 2 h, three days a week from postnatal day (PND) 29, the reinforcing effects of EtOH were tested with EtOH self-administration (SA), conditioned place preference (CPP) and ethanol locomotor sensitization procedures in young adult mice...
April 27, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28456841/changes-in-gene-expression-and-sensitivity-of-cocaine-reward-produced-by-a-continuous-fat-diet
#8
M Carmen Blanco-Gandía, Auxiliadora Aracil-Fernández, Sandra Montagud-Romero, Maria A Aguilar, Jorge Manzanares, José Miñarro, Marta Rodríguez-Arias
RATIONALE: Preclinical studies report that free access to a high-fat diet (HFD) alters the response to psychostimulants. OBJECTIVES: The aim of the present study was to examine how HFD exposure during adolescence modifies cocaine effects. Gene expression of CB1 and mu-opioid receptors (MOr) in the nucleus accumbens (N Acc) and prefrontal cortex (PFC) and ghrelin receptor (GHSR) in the ventral tegmental area (VTA) were assessed. METHODS: Mice were allowed continuous access to fat from PND 29, and the locomotor (10 mg/kg) and reinforcing effects of cocaine (1 and 6 mg/kg) on conditioned place preference (CPP) were evaluated on PND 69...
April 29, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28456745/oprm1-methylation-contributes-to-opioid-tolerance-in-cancer-patients
#9
Chi T Viet, Dongmin Dang, Bradley E Aouizerat, Christine Miaskowski, Yi Ye, Dan T Viet, Kentaro Ono, Brian L Schmidt
Cancer patients in pain require high doses of opioids and quickly become opioid-tolerant. Previous studies have shown that both chronic cancer pain and high dose opioid use lead to mu-opioid receptor down-regulation. In this study we explore down-regulation of OPRM1, the mu-opioid receptor gene, as a mechanism f,or opioid tolerance in the setting of opioid use for cancer pain. We demonstrate in a cohort of 84 cancer patients that high dose opioid use correlates with OPRM1 hypermethylation in peripheral leukocytes of these patients...
April 26, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28455226/the-effect-of-selective-opioid-receptor-agonists-and-antagonists-on-epileptiform-activity-in-morphine-dependent-infant-mice-hippocampal-slices
#10
Yousef Panahi, Ehsan Saboory, Ali Rassouli, Goudarz Sadeghi-Hashjin, Shiva Roshan-Milani, Leila Derafshpour, Yousef Rasmi
Hippocampal slices of mouse brain were used to estimate how selective agonist and antagonist of opioid receptors alter Low-Mg(+2) artificial cerebrospinal fluid (LM-ACSF)-induced epileptiform activities in normal and morphine-dependent mice. Brain slices were obtained from control and morphine-dependent mice. The morphine-dependent group received morphine once a day for 5 consecutive days, and the control group received saline. All injections were administered subcutaneously (s.c) in a volume of 0.1mL on postnatal days 14-18...
April 25, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28450396/heat-shock-protein-90-hsp90-promotes-opioid-induced-anti-nociception-by-an-erk-mitogen-activated-protein-kinase-mapk-mechanism-in-mouse-brain
#11
Wei Lei, Nathan Mullen, Sarah McCarthy, Courtney Brann, Philomena Richard, James Cormier, Katie Edwards, Edward J Bilsky, John M Streicher
Recent advances in developing opioid treatments for pain with reduced side effects have focused on the signaling cascades of the mu opioid receptor (MOR). However, few such signaling targets have been identified for exploitation. To address this need, we explored the role of Heat shock protein 90 (Hsp90) in opioid-induced MOR signaling and pain, which has only been studied in 4 previous papers. First, in 4 cell models of MOR signaling, we found that Hsp90 inhibition for 24 hours with the inhibitor 17-N-allylamino-17-demethoxygeldanamycin (17-AAG) had different effects on protein expression and opioid signaling in each line, suggesting that cell models may not be reliable for predicting pharmacology with this protein...
April 27, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28446883/in-vitro-and-in-vivo-profile-of-ppl-101-and-ppl-103-mixed-opioid-partial-agonist-analgesics-with-low-abuse-potential
#12
Taline V Khroyan, Andrea Cippitelli, Nicholas Toll, John A Lawson, William Crossman, Willma E Polgar, Lawrence Toll
Opiates are still the most effective and widely used treatments for acute and chronic pain. However, the problems associated with morphine and other standard opioid analgesics severely limit their effectiveness in the clinic. PPL-101 and PPL-103 derived from morphine and morphinan ring systems contain a chiral N-substituent, which confers it with a unique combination of high-binding affinities and partial agonist activities at mu, delta, and kappa opioid receptors, leading to unique in vivo pharmacology compared to other conventional opioids...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28443503/kratom-and-future-treatment-for-the-opioids-addiction-and-chronic-pain-periculo-beneficium
#13
Ismaliza Ismail, Suzaily Wahab, Hatta Sidi, Srijit Das, Loo Jiann Lin, Rosdinom Razali
Kratom (Mitragynaspeciosa), a natural existing plant found in South-East Asia, is tradi-tionally used as an herb to help to elevate a person's energy and also to treat numerous medical ailments. Other than the analgesic property, kratom has been used as an agent to overcome opioid withdrawal as it contains natural alkaloids, i.e. mitragynine, 7-hydroxymitragynine, and MGM-9, which has agonist affinity on the opioid receptors, including mu (μ) and kappa (κ). The role of neural reward pathway linked to μ-opioid receptors and both dopaminergic and GABA-ergic interneurons that express μ-opioid receptors were deliberated...
April 25, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28442370/modulation-of-drug-choice-by-extended-drug-access-and-withdrawal-in-rhesus-monkeys-implications-for-negative-reinforcement-as-a-driver-of-addiction-and-target-for-medications-development
#14
REVIEW
S Stevens Negus, Matthew L Banks
Chronic drug exposure is hypothesized to recruit negative reinforcement processes that increase the magnitude and alter the mechanisms of drug reinforcement. Candidate substrates of negative reinforcement include increased signaling via stress-related neurotransmitters such as corticotropin releasing factor (CRF, acting at CRF receptors) or dynorphin (acting at kappa opioid receptors) and/or decreased signaling via reward-related neurotransmitters such as dopamine. Determinants of drug reinforcement can be examined with choice procedures, in which subjects choose between a drug of interest (e...
April 22, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28431630/kynurenic-acid-and-its-analogue-can-alter-the-opioid-receptor-g-protein-signaling-after-acute-treatment-via-nmda-receptor-in-rat-cortex-and-striatum
#15
Reza Samavati, Ferenc Zádor, Edina Szűcs, Bernadett Tuka, Diána Martos, Gábor Veres, Róbert Gáspár, István M Mándity, Ferenc Fülöp, László Vécsei, Sándor Benyhe, Anna Borsodi
Previously, we have shown that the N-methyl d-aspartate (NMDA)-receptor antagonist kynurenic acid (KYNA) and its analogue KYNA1 do not bind directly to mu, kappa and delta opioid receptors in vitro. On the other hand, chronic administration of KYNA and KYNA1 resulted in region (cortex vs striatum) and opioid receptor-type specific alterations in G-protein activation of mouse brain homogenates. Here we describe for the first time the acute effect of KYNA and KYNA1 on opioid receptor function with the possible involvement of the NMDA receptor...
May 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28412878/-top-down-mu-opioid-system-function-in-humans-mu-opioid-receptors-in-ventrolateral-prefrontal-cortex-mediate-the-relationship-between-hedonic-tone-and-executive-function-in-major-depressive-disorder
#16
Sharee N Light, Linas A Bieliauskas, Jon-Kar Zubieta
Cognitive dysfunction and anhedonia, the reduced ability to experience pleasure, are commonly comorbid symptoms that are persistent following successful resolution of negative affect in major depressive disorder (MDD). Little is known about whether they share common etiology. In the present study, the relationship between ventrolateral prefrontal cortex (VLPFC) activity, cognitive dysfunction (i.e., executive dysfunction), and positive emotionality was investigated in conjunction with mu-opioid neurotransmission in a sample of 39 MDD patients...
April 17, 2017: Journal of Neuropsychiatry and Clinical Neurosciences
https://www.readbyqxmd.com/read/28411124/m3-muscarinic-acetylcholine-receptor-facilitates-the-endocytosis-of-mu-opioid-receptor-mediated-by-morphine-independently-of-the-formation-of-heteromeric-complexes
#17
Juan F Lopez-Gimenez, Elisa Alvarez-Curto, Graeme Milligan
Morphine inefficiency to induce the internalization of mu opioid (MOP) receptors observed in numerous experimental models constitutes a paradigm of G-protein coupled receptor (GPCR) functional selectivity. We recently described that activation of Gαq/11 proteins through 5-HT2A serotonin receptors co-expressed in the same cells facilitates MOP receptor endocytosis promoted by morphine. In order to explore whether a different Gαq/11 coupled GPCR would emulate this effect, a double stable Flp-In T-REx HEK293 cell line permanently expressing MOP-YFP receptors along with FLAG-M3-Cerulean receptors expressed in an inducible manner was generated...
April 11, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28407740/mu-opioid-receptor-and-delta-opioid-receptor-differentially-regulate-microglial-inflammatory-response-to-control-proopiomelanocortin-neuronal-apoptosis-in-the-hypothalamus-effects-of-neonatal-alcohol
#18
Pallavi Shrivastava, Miguel A Cabrera, Lucy G Chastain, Nadka I Boyadjieva, Shaima Jabbar, Tina Franklin, Dipak K Sarkar
BACKGROUND: Opioid receptors are known to control neurotransmission of various peptidergic neurons, but their potential role in regulation of microglia and neuronal cell communications is unknown. We investigated the role of mu-opioid receptors (MOR) and delta-opioid receptors (DOR) on microglia in the regulation of apoptosis in proopiomelanocortin (POMC) neurons induced by neonatal ethanol in the hypothalamus. METHODS: Neonatal rat pups were fed a milk formula containing ethanol or control diets between postnatal days 2-6...
April 14, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28394447/mu-opioid-receptor-signaling-in-the-nucleus-accumbens-shell-increases-responsiveness-of-satiety-modulated-lateral-hypothalamus-neurons
#19
Shashank Tandon, Kristen A Keefe, Sharif A Taha
Opioid signaling in the nucleus accumbens shell (sNAcc) has been implicated in hedonic feeding and binge eating behavior. The sNAcc projects to the lateral hypothalamus (LH), and this pathway has been suggested to modulate palatability-driven feeding behavior. In this study, we investigated the effects of sNAcc mu opioid receptor (MOR) stimulation on firing rates of LH neurons in previously sated rats. Neural firing in the LH was recorded while food-deprived rats performed an operant task to obtain sweetened Intralipid (a 4% fat emulsion containing 5% sucrose) before and after bilateral sNAcc infusion of either a MOR agonist [D-Ala2, N-MePhe4, Gly-ol]-enkephalin (DAMGO) or a saline control solution...
April 10, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28381559/identification-of-a-signaling-cascade-that-maintains-constitutive-delta-opioid-receptor-incompetence-in-peripheral-sensory-neurons
#20
Allison Doyle Brackley, Shayda Sarrami, Ruben Gomez, Kristi A Guerrero, Nathaniel A Jeske
Mu opioid receptor (MOR) agonists are often used to treat severe pain, but can result in adverse side effects. To circumvent systemic side effects, targeting peripheral opioid receptors is an attractive alternative treatment for severe pain. Activation of the delta opioid receptor (DOR) produces similar analgesia with reduced side effects. However, until primed by inflammation, peripheral DOR is analgesically incompetent, raising interest in the mechanism. We recently identified a novel role for G protein-coupled receptor kinase 2 (GRK2) that renders DOR analgesically incompetent at the plasma membrane...
April 5, 2017: Journal of Biological Chemistry
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