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https://www.readbyqxmd.com/read/28488261/use-of-tramadol-in-psychiatric-care-a-comprehensive-review-and-report-of-two-cases
#1
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/28455226/the-effect-of-selective-opioid-receptor-agonists-and-antagonists-on-epileptiform-activity-in-morphine-dependent-infant-mice-hippocampal-slices
#2
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...
August 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28414967/pharmacodynamics-of-remifentanil-induced-intracranial-spike-activity-in-mesial-temporal-lobe-epilepsy
#3
Troels Wesenberg Kjaer, Hans Hogenhaven, Andrea P Lee, Flemming Find Madsen, Bo Jespersen, Jannick Brennum, Lennart Derm, Finn Borgbjerg Moltke
Patients with medically refractory epilepsy may benefit from resective epilepsy surgery. However even the best centers experience surgical failures. It is therefore important to find techniques that may aid in neurosurgical planning of epileptic focus resection. Recordings of electrical brain activity with EEG during seizures reveal abnormal cortical hypersynchronization. Between seizures the EEG often shows interictal depolarizing phenomena such as spikes reflecting an irritable focus of the brain. In the present study we investigated the effect of intravenous remifentanil on the spike activity in the temporal neocortex and hippocampus...
March 31, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28343361/genetic-dissociation-of-morphine-analgesia-from-hyperalgesia-in-mice
#4
Gina F Marrone, Valerie Le Rouzic, Andras Varadi, Jin Xu, Anjali M Rajadhyaksha, Susruta Majumdar, Ying-Xian Pan, Gavril W Pasternak
RATIONALE: Morphine is the prototypic mu opioid, producing its analgesic actions through traditional 7 transmembrane domain (7TM) G-protein-coupled receptors generated by the mu opioid receptor gene (Oprm1). However, the Oprm1 gene undergoes extensive alternative splicing to yield three structurally distinct sets of splice variants. In addition to the full-length 7TM receptors, it produces a set of truncated variants comprised of only 6 transmembrane domains (6TM). OBJECTIVES: This study explored the relative contributions of 7TM and 6TM variants in a range of morphine actions...
June 2017: Psychopharmacology
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/27909104/loss-of-plasticity-in-the-d2-accumbens-pallidal-pathway-promotes-cocaine-seeking
#6
J A Heinsbroek, D N Neuhofer, W C Griffin, G S Siegel, A-C Bobadilla, Y M Kupchik, P W Kalivas
Distinct populations of D1- and D2-dopamine receptor expressing medium spiny neurons (D1-/D2-MSNs) comprise the nucleus accumbens, and activity in D1-MSNs promotes, while activity in D2-MSNs inhibits motivated behaviors. We used chemogenetics to extend D1-/D2-MSN cell specific regulation to cue-reinstated cocaine seeking in a mouse model of self-administration and relapse, and found that either increasing activity in D1-MSNs or decreasing activity in D2-MSNs augmented cue-induced reinstatement. Both D1- and D2-MSNs provide substantial GABAergic innervation to the ventral pallidum, and chemogenetic inhibition of ventral pallidal neurons blocked the augmented reinstatement elicited by chemogenetic regulation of either D1- or D2-MSNs...
December 1, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27903758/oprm1-and-comt-gene-gene-interaction-is-associated-with-postoperative-pain-and-opioid-consumption-after-orthopedic-trauma
#7
Heba Khalil, Susan M Sereika, Feng Dai, Sheila Alexander, Yvette Conley, Gary Gruen, Li Meng, Peter Siska, Ivan Tarkin, Richard Henker
BACKGROUND: mu-opioid receptor ( OPRM1) and catechol-O-methyltransferase ( COMT) contribute to the neurotransmission pathway of pain. COMT affects mu receptor expression and density in the brain. The aim of this study was to explore the OPRM1 and COMT interaction effects on postoperative pain and opioid consumption. METHODS: This cross-sectional exploratory study used genotype and clinical data from 153 postoperative patients. Using multiple regression analyses, four single-nucleotide polymorphisms of COMT (rs6269, rs4633, rs4818, and rs4680), their haplotypes, and diplotypes were considered for their interactions with A118G of OPRM1 regarding postoperative pain and opioid consumption...
March 2017: Biological Research for Nursing
https://www.readbyqxmd.com/read/27736284/continuous-perioperative-sublingual-buprenorphine
#8
Marcelina Jasmine Silva, Andrea Rubinstein
Buprenorphine, a semisynthetic thebaine derivative, is a unique opioid, as it has activity at multiple receptors, including mu (partial agonist), kappa (antagonist), OLR-1 (agonist), and delta (antagonist). Because buprenorphine's pharmacology is relatively complex, misconceptions about its actions are common. Most other opioids act solely or predominately as full mu receptor agonists. Common practice at many institutions calls for the cessation of regular buprenorphine use 48-72 hours prior to surgery. This practice is based on three foundational theories that have come from scant data about the properties of buprenorphine: (1) that buprenorphine is only a partial mu agonist and therefore is not a potent analgesic; (2) because buprenorphine has a ceiling effect on respiratory depression, it also has a ceiling effect on analgesia; and (3) that buprenorphine acts as a "blockade" to the analgesic effects of other opiates when coadministered due to its strong binding affinity...
December 2016: Journal of Pain & Palliative Care Pharmacotherapy
https://www.readbyqxmd.com/read/27671662/deletion-of-the-mu-opioid-receptor-gene-in-mice-reshapes-the-reward-aversion-connectome
#9
Anna E Mechling, Tanzil Arefin, Hsu-Lei Lee, Thomas Bienert, Marco Reisert, Sami Ben Hamida, Emmanuel Darcq, Aliza Ehrlich, Claire Gaveriaux-Ruff, Maxime J Parent, Pedro Rosa-Neto, Jürgen Hennig, Dominik von Elverfeldt, Brigitte Lina Kieffer, Laura-Adela Harsan
Connectome genetics seeks to uncover how genetic factors shape brain functional connectivity; however, the causal impact of a single gene's activity on whole-brain networks remains unknown. We tested whether the sole targeted deletion of the mu opioid receptor gene (Oprm1) alters the brain connectome in living mice. Hypothesis-free analysis of combined resting-state fMRI diffusion tractography showed pronounced modifications of functional connectivity with only minor changes in structural pathways. Fine-grained resting-state fMRI mapping, graph theory, and intergroup comparison revealed Oprm1-specific hubs and captured a unique Oprm1 gene-to-network signature...
October 11, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27223691/mediation-of-buprenorphine-analgesia-by-a-combination-of-traditional-and-truncated-mu-opioid-receptor-splice-variants
#10
Steven G Grinnell, Michael Ansonoff, Gina F Marrone, Zhigang Lu, Ankita Narayan, Jin Xu, Grace Rossi, Susruta Majumdar, Ying-Xian Pan, Daniel L Bassoni, John Pintar, Gavril W Pasternak
Buprenorphine has long been classified as a mu analgesic, although its high affinity for other opioid receptor classes and the orphanin FQ/nociceptin ORL1 receptor may contribute to its other actions. The current studies confirmed a mu mechanism for buprenorphine analgesia, implicating several subsets of mu receptor splice variants. Buprenorphine analgesia depended on the expression of both exon 1-associated traditional full length 7 transmembrane (7TM) and exon 11-associated truncated 6 transmembrane (6TM) MOR-1 variants...
October 2016: Synapse
https://www.readbyqxmd.com/read/27125653/gastrointestinal-complications-in-patients-who-undergo-radical-cystectomy-with-enhanced-recovery-protocol
#11
REVIEW
Hooman Djaladat, Siamak Daneshmand
Gastrointestinal (GI) complications are among the most common complications following radical cystectomy and urinary diversion. The most common is postoperative ileus, although its precise pathophysiology is not completely understood. Enhanced recovery after surgery (ERAS) protocols include evidence-based steps to optimize postoperative recovery and shorten hospital stay, mainly through expedited GI function recovery. They include avoiding bowel preparation and postoperative nasogastric tube, early feeding, non-narcotic pain management, and the use of cholinergic and mu-receptor opioid antagonists...
July 2016: Current Urology Reports
https://www.readbyqxmd.com/read/27101321/multimodal-analgesia-in-the-hip-fracture-patient
#12
David W Fabi
Hip fracture is one of the most common injuries among the elderly and, because the population is aging, it is expected to remain a major clinical challenge and public health problem for the foreseeable future. The clinical importance of early mobilization and prompt participation in physical therapy after hip fracture surgery is now widely recognized. Because postoperative pain can impair mobility and delay physical therapy, much attention is now being paid to finding more effective ways of controlling pain after hip fracture...
May 2016: Journal of Orthopaedic Trauma
https://www.readbyqxmd.com/read/27038094/redoubling-the-ring-size-of-an-endomorphin-2-analog-transforms-a-centrally-acting-mu-opioid-receptor-agonist-into-a-pure-peripheral-analgesic
#13
Justyna Piekielna, Rossella De Marco, Luca Gentilucci, Maria Camilla Cerlesi, Girolamo Calo', Csaba Tömböly, Roberto Artali, Anna Janecka
The study reports the synthesis and biological evaluation of two opioid analogs, a monomer and a dimer, obtained as products of the solid-phase, side-chain to side-chain cyclization of the pentapeptide Tyr-d-Lys-Phe-Phe-AspNH2 . The binding affinities to the mu, delta, and kappa opioid receptors, as well as results obtained in a calcium mobilization functional assay are reported. Tyr-[d-Lys-Phe-Phe-Asp]2 -NH2 1 was a potent and selective full agonist of mu with sub-nanomolar affinity, while the dimer (Tyr-[d-Lys-Phe-Phe-Asp]2 -NH2 )2 2 showed a significant mixed mu/kappa affinity, acting as an agonist at the mu...
May 2016: Biopolymers
https://www.readbyqxmd.com/read/27014278/emerging-functions-of-natural-igm-and-its-fc-receptor-fcmr-in-immune-homeostasis
#14
REVIEW
Hongsheng Wang, John E Coligan, Herbert C Morse
Most natural IgM antibodies are encoded by germline Ig sequences and are produced in large quantities by both mice and humans in the absence of intentional immunization. Natural IgM are reactive with many conserved epitopes, including those shared by microorganisms and autoantigens. As a result, these antibodies play important roles in clearing intruding pathogens, as well as apoptotic/necrotic cells and otherwise damaged tissues. While natural IgM binds to target structures with low affinity due to a lack of significant selection by somatic hypermutation, its pentameric structure with 10 antigen-binding sites enables these antibodies to bind multivalent target antigens with high avidity...
2016: Frontiers in Immunology
https://www.readbyqxmd.com/read/26976581/truncated-mu-opioid-gpcr-variant-involvement-in-opioid-dependent-and-opioid-independent-pain-modulatory-systems-within-the-cns
#15
Gina F Marrone, Steven G Grinnell, Zhigang Lu, Grace C Rossi, Valerie Le Rouzic, Jin Xu, Susruta Majumdar, Ying-Xian Pan, Gavril W Pasternak
The clinical management of severe pain depends heavily on opioids acting through mu opioid receptors encoded by the Oprm1 gene, which undergoes extensive alternative splicing. In addition to generating a series of prototypic seven transmembrane domain (7TM) G protein-coupled receptors (GPCRs), Oprm1 also produces a set of truncated splice variants containing only six transmembrane domains (6TM) through which selected opioids such as IBNtxA (3'-iodobenzoyl-6β-naltrexamide) mediate a potent analgesia without many undesirable effects...
March 29, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/26956246/nociceptin-orphanin-fq-receptor-structure-signaling-ligands-functions-and-interactions-with-opioid-systems
#16
REVIEW
Lawrence Toll, Michael R Bruchas, Girolamo Calo', Brian M Cox, Nurulain T Zaveri
The NOP receptor (nociceptin/orphanin FQ opioid peptide receptor) is the most recently discovered member of the opioid receptor family and, together with its endogenous ligand, N/OFQ, make up the fourth members of the opioid receptor and opioid peptide family. Because of its more recent discovery, an understanding of the cellular and behavioral actions induced by NOP receptor activation are less well developed than for the other members of the opioid receptor family. All of these factors are important because NOP receptor activation has a clear modulatory role on mu opioid receptor-mediated actions and thereby affects opioid analgesia, tolerance development, and reward...
April 2016: Pharmacological Reviews
https://www.readbyqxmd.com/read/26735118/fos-like-immunoreactivity-in-tyrosine-hydroxylase-and-substance-p-like-immunoreactive-neurones-in-guinea-pig-brain-following-intracerebroventricular-injection-of-morphine-and-u50-488h
#17
G Bot, L A Chahl
Opioid drugs such as morphine have powerful reinforcing effects which lead to drug-seeking behaviour. Both dopamine- and substance P-containing neurones have been implicated in reward. In the present study twocolour immunohistochemistry was used to investigate whether Fos protein was induced in dopaminergic (tyrosine hydroxylase) and substance P-containing neurones of guinea-pig brain following intracerebroventricular administration of the predominantly mu-receptor agonist, morphine, and the kappa-receptor agonist, U50,488H, which have been reported to produce rewarding and aversive effects, respectively...
October 1998: Addiction Biology
https://www.readbyqxmd.com/read/26656274/changes-in-d1-but-not-d2-dopamine-or-mu-opioid-receptor-expression-in-limbic-and-motor-structures-after-lateral-hypothalamus-electrical-self-stimulation-a-quantitative-autoradiographic-study
#18
Maria J Simon, A Higuera-Matas, D Roura-Martinez, M Ucha, R Santos-Toscano, C Garcia-Lecumberri, E Ambrosio, A Puerto
Intracranial self-stimulation (ICSS) of the lateral hypothalamus (LH) is involved in the activation of neuroanatomical systems that are also associated with the processing of natural and other artificial rewarding stimuli. Specific components of this behavior (hedonic impact, learning, and motor behavior) may involve changes in different neurotransmitters, such as dopamine and opioids. In this study, quantitative autoradiography was used to examine changes in mu-opioid and D1/D2-dopamine receptor expression in various anatomical regions related to the motor and mesolimbic reward systems after intracranial self-stimulation of the LH...
January 2016: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/26591588/-the-influence-of-opioid-peptides-on-lipid-peroxidation-and-antioxidant-enzyme-activity-in-rats-after-swimming-stress
#19
A V Solin, Yu D Lyashev
It was established in experiments on rats, that injection of opioid peptides DAGO (a selective igonist of opioid mu-receptors), DSLET (a selective agonist of opioid delta-receptors) or dynorpiin A (1-13) (a selective agonist of opioid kappa-receptors) decreased the stress-induced activatin of lipid peroxidation in liver tissue and plasma. A selective agonist of opioid mu-receptors) AGO manifested the most expressed activity. The using of investigating peptides caused the increase of superoxiddismutase activity in liver tissue...
August 2015: Rossiĭskii Fiziologicheskiĭ Zhurnal Imeni I.M. Sechenova
https://www.readbyqxmd.com/read/26574020/the-new-kid-on-the-block-incorporating-buprenorphine-into-a-medical-toxicology-practice
#20
REVIEW
Timothy J Wiegand
Buprenorphine represents a safe and effective therapy for treating opioid dependence, alleviating craving and withdrawal symptoms in opioid-dependent patients. Buprenorphine has a "blocking" effect against the action of other opioids at the mu-receptor, preventing not only opioid-induced euphoria, but CNS and respiratory depressant effects as well. Buprenorphine was approved for the treatment of opioid dependence in 2002 after the passage of Drug Abuse Treatment Act 2000 (DATA 2000) which allowed clinicians to treat opioid-dependent patients with specifically named opioid agonist therapies in an office setting...
March 2016: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
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