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https://www.readbyqxmd.com/read/29155916/a-novel-strategy-to-address-unmeasured-confounding-when-comparing-opioid-agonist-therapies-in-pregnancy
#1
Lara S Lemon
Opioid addiction in pregnancy is a growing concern that has recently received a lot of attention. When comparing recommended opioid agonist therapies, many currently published studies guiding practice may be impacted by unmeasured confounding by indication. Populations of women who receive methadone are generally different from those treated with buprenorphine. Women treated with methadone frequently have more severe and uncontrolled addiction compared with buprenorphine treated patients; however, these factors are typically unmeasured or unavailable in large observational data sets...
November 16, 2017: American Journal of Epidemiology
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
#2
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/29152051/%C3%AF-space-screening-of-dermorphin-based-tetrapeptides-through-use-of-constrained-arylazepinone-and-quinolinone-scaffolds
#3
Olivier Van der Poorten, Robin Van Den Hauwe, Emilie Eiselt, Cecilia Betti, Karel Guillemyn, Nga N Chung, François Hallé, Frédéric Bihel, Peter W Schiller, Dirk Tourwé, Philippe Sarret, Louis Gendron, Steven Ballet
Herein, the synthesis of novel conformationally constrained amino acids, 4-amino-8-bromo-2-benzazepin-3-one (8-Br-Aba), 3-amino-3,4-dihydroquinolin-2-one, and regioisomeric 4-amino-naphthoazepinones (1- and 2-Ana), is described. Introduction of these constricted scaffolds into the N-terminal tetrapeptide of dermorphin (i.e., H-Tyr-d-Ala-Phe-Gly-NH2) induced significant shifts in binding affinity, selectivity, and in vitro activity at the μ- and δ-opioid receptors (MOP and DOP, respectively). A reported constrained μ-/δ-opioid lead tetrapeptide H-Dmt-d-Arg-Aba-Gly-NH2 was modified through application of various constrained building blocks to identify optimal spatial orientations in view of activity at the opioid receptors...
November 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29150865/enhanced-mu-opioid-receptor-dependent-opioidergic-modulation-of-striatal-cholinergic-transmission-in-dyt1-dystonia
#4
Giulia Ponterio, Annalisa Tassone, Giuseppe Sciamanna, Valentina Vanni, Maria Meringolo, Massimo Santoro, Nicola Biagio Mercuri, Paola Bonsi, Antonio Pisani
BACKGROUND: Mu opioid receptor activation modulates acetylcholine release in the dorsal striatum, an area deeply involved in motor function, habit formation, and reinforcement learning as well as in the pathophysiology of different movement disorders, such as dystonia. Although the role of opioids in drug reward and addiction is well established, their involvement in motor dysfunction remains largely unexplored. METHODS: We used a multidisciplinary approach to investigate the responses to mu activation in 2 mouse models of DYT1 dystonia (Tor1a(+/Δgag) mice, Tor1a(+/-) torsinA null mice, and their respective wild-types)...
November 18, 2017: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/29149148/current-impact-and-application-of-abuse-deterrent-opioid-formulations-in-clinical-practice
#5
Ya-Han Lee, Daniel L Brown, Hsiang-Yin Chen
BACKGROUND: Abuse-deterrent formulations (ADFs) represent one novel strategy for curbing the potential of opioid abuse. OBJECTIVE: We aim to compare and contrast the characteristics and applications of current abuse-deterrent opioid products in clinical practice. METHODS: Literature searches were conducted in databases (Pubmed Medline, International Pharmaceutical Abstracts, Google Scholar) and official reports. Relevant data were screened and organized into: 1) epidemiology of opioid abuse, 2) mitigation strategies for reducing opioid abuse, 3) development of ADFs, and 4) clinical experience with these formulations...
November 2017: Pain Physician
https://www.readbyqxmd.com/read/29147138/an-update-on-prucalopride-in-the-treatment-of-chronic-constipation
#6
REVIEW
Anam Omer, Eamonn M M Quigley
Chronic constipation (CC) is a highly prevalent and often under-appreciated gastrointestinal disorder associated with significant impairment in quality of life. Symptoms of constipation are typically present for a number of years prior to a patient seeking help. Lifestyle modifications followed by, or coupled with, over-the-counter laxatives represent the initial treatment option; however, relief for many is limited and dissatisfaction rates for these approaches remain high. Over recent years, therefore, considerable effort has been exerted on the development of novel pharmacological approaches...
November 2017: Therapeutic Advances in Gastroenterology
https://www.readbyqxmd.com/read/29146290/sustained-opioid-antagonism-modulates-striatal-sensitivity-to-baby-schema-in-opioid-use-disorder
#7
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/29144441/g-protein-coupled-receptors-targeted-by-analgesic-venom-peptides
#8
REVIEW
James T Daniel, Richard J Clark
Chronic pain is a complex and debilitating condition associated with a large personal and socioeconomic burden. Current pharmacological approaches to treating chronic pain such as opioids, antidepressants and anticonvulsants exhibit limited efficacy in many patients and are associated with dose-limiting side effects that hinder their clinical use. Therefore, improved strategies for the pharmacological treatment of pathological pain are urgently needed. G-protein coupled receptors (GPCRs) are ubiquitously expressed on the surface of cells and act to transduce extracellular signals and regulate physiological processes...
November 16, 2017: Toxins
https://www.readbyqxmd.com/read/29143400/pharmacokinetics-of-concentrated-naloxone-nasal-spray-for-opioid-overdose-reversal-phase-i-healthy-volunteer-study
#9
Rebecca McDonald, Ulrike Lorch, Jo Woodward, Björn Bosse, Helen Dooner, Gill Mundin, Kevin Smith, John Strang
BACKGROUND AND AIMS: Take-home naloxone can prevent death from heroin/opioid overdose, but pre-provision is difficult because naloxone is usually given by injection. Non-injectable alternatives, including naloxone nasal sprays, are currently being developed. To be effective, the intranasal (i.n.) spray dose must be adequate but not excessive, and early absorption must be comparable to intramuscular (i.m.) injection. We report on the pharmacokinetics (PK) of a specially produced concentrated novel nasal spray...
November 16, 2017: Addiction
https://www.readbyqxmd.com/read/29142219/electroacupuncture-attenuates-induction-of-inflammatory-pain-by-regulating-opioid-and-adenosine-pathways-in-mice
#10
Hsien-Yin Liao, Ching-Liang Hsieh, Chun-Ping Huang, Yi-Wen Lin
Although inflammatory pain is a common clinical condition, its mechanisms are still unclear. Electroacupuncture (EA), a well-known method of pain management, may reduce inflammatory pain by regulating neurons, astrocytes, and inflammatory signaling pathways. Injections of complete Freund's adjuvant (CFA), which can initiate cell-mediated inflammatory pain, resulted in significant hyperalgesia, which was subsequently prevented by EA. In CFA-injected mice, a dramatic increase was observed in the expression of the following proteins in the dorsal root ganglion and spinal cord dorsal horn: the astrocytic marker GFAP, S100B, RAGE, pPKCε, COX-2, pERK, and pNFκB...
November 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29138268/n-acyl-amino-acids-elmiric-acids-endogenous-signaling-molecules-with-therapeutic-potential
#11
Sumner Burstein
The subject of N-acyl amino acid conjugates has been rapidly growing in recent years, especially with regard to their analgesic and anti-inflammatory actions. The field is comprised of a large family of lipid signaling molecules whose importance is only now being fully realized. The most widely studied member is N-arachidonoyl glycine (NAGly), which differs structurally from the endocannabinoid anandamide (N-arachidonoyl ethanolamide) by a single oxygen atom and the two are metabolically related. Topics that are covered in this mini review are: biosynthetic pathways for N-acyl amino acids, receptors for N-acyl amino acids, physiological actions of N-acyl amino acids, pharmacological effects of N-acyl amino acids and molecular mechanisms believed to be responsible for their effects...
November 14, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29135018/chronic-prurigo-of-nodular-type-a-review
#12
Claudia Zeidler, Athanasios Tsianakas, Manuel Pereira, Hartmut Ständer, Gil Yosipovitch, Sonja Ständer
Prurigo nodularis (PN) is a subtype of chronic prurigo presenting single to multiple symmetrically distributed, hyperkeratotic and intensively itching papules and nodules. PN evolves along with chronic pruritus in the context of diverse dermatological, systemic, neurological or psychiatric conditions. Permanent scratching is possibly a major trigger of PN, although its exact pathophysiology remains unclear. Current state-of-the-art therapy for PN consists of topical steroids, capsaicin, calcineurin inhibitors, ultraviolet (UV) therapy, systemic administration of gabapentinoids, μ-opioid receptor antagonists, antidepressants or immunosuppressants...
August 23, 2017: Acta Dermato-venereologica
https://www.readbyqxmd.com/read/29133887/a-complementary-scale-of-biased-agonism-for-agonists-with-differing-maximal-responses
#13
Javier Burgueño, Marta Pujol, Xavier Monroy, David Roche, Maria Jose Varela, Manuel Merlos, Jesús Giraldo
Compelling data in the literature from the recent years leave no doubt about the pluridimensional nature of G protein-coupled receptor function and the fact that some ligands can couple with different efficacies to the multiple pathways that a receptor can signal through, a phenomenon most commonly known as functional selectivity or biased agonism. Nowadays, transduction coefficients (log(τ/KA)), based on the Black and Leff operational model of agonism, are widely used to calculate bias. Nevertheless, combining both affinity and efficacy in a single parameter can result in compounds showing a defined calculated bias of one pathway over other though displaying varying experimental bias preferences...
November 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29132133/endomorphins-promising-endogenous-opioid-peptides-for-the-development-of-novel-analgesics
#14
Zheng-Hui Gu, Bo Wang, Zhen-Zhen Kou, Yang Bai, Tao Chen, Yu-Lin Dong, Hui Li, Yun-Qing Li
Endomorphin-1 (EM1) and endomorphin-2 (EM2) are two endogenous ligands that belong to the opioid peptide family and have the highest affinity and selectivity for the µ-opioid receptor (MOR). The neuroanatomical distribution, ultrastructural features and neural circuitry of EM-containing neuronal structures have been morphologically demonstrated. In addition, the modulation effects of the EMs in different areas reflect their potential endogenous roles in many major physiological processes, including their remarkable roles in the transmission and modulation of noxious information...
November 13, 2017: Neuro-Signals
https://www.readbyqxmd.com/read/29124744/usefulness-of-knockout-mice-to-clarify-the-role-of-the-opioid-system-in-chronic-pain
#15
REVIEW
Rafael Maldonado, Josep Eladi Baños, David Cabañero
Several lines of knockout mice deficient in the genes encoding each component of the endogenous opioid system have been used for decades to clarify the specific role of the different opioid receptors and peptide precursors in multiple physiopathological conditions. The use of these genetically modified mice has improved our knowledge of the specific involvement of each endogenous opioid component in nociceptive transmission during acute and chronic pain conditions. The present review summarizes the recent advances obtained using these genetic tools in understanding the role of the opioid system in the pathophysiological mechanisms underlying chronic pain...
November 10, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29121571/high-throughput-%C3%AE-spe-based-elution-coupled-with-uplc-ms-ms-for-determination-of-eluxadoline-in-plasma-sample-application-in-pharmacokinetic-characterization-of-plga-nanoparticle-formulations-in-rats
#16
Muzaffar Iqbal, Essam Ezzeldin, Khalid A Al-Rashood, Ramadan Al-Shdefat, Md Khalid Anwer
Eluxadoline is a novel μ- and κ-opioid receptor (OR) agonist and δ-OR antagonist, recently approved as a first line therapy for the treatment of irritable bowel syndrome. Due to abuse potential, poor bioavailability and high intersubject variability, a sensitive and reliable assay is prerequisite for its determination in biological samples. This work first time report the development and validation of UPLC-MS/MS assay for determination of eluxadoline in rat plasma sample using risperidone as an internal standard (IS)...
October 28, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29120924/potential-mechanisms-underlying-the-effect-of-bariatric-surgery-on-eating-behaviour
#17
Roxanna Zakeri, Rachel L Batterham
PURPOSE OF REVIEW: Reduced energy intake, resulting from favourable changes in eating behaviour, is the predominant driver of weight loss following bariatric surgery. Here we review the most recent studies examining the impact of Roux-en-Y gastric bypass (RYGB) and sleeve gastrectomy, the two most common bariatric procedures, upon eating behaviour and the suggested underlying biological mechanisms. RECENT FINDINGS: Following RYGB or sleeve gastrectomy, most people report subjective changes in appetite, taste and food preference, with decreased high-fat preference most commonly reported...
November 7, 2017: Current Opinion in Endocrinology, Diabetes, and Obesity
https://www.readbyqxmd.com/read/29115161/pharmacokinetics-of-tapentadol-in-laying-hens-and-its-residues-in-eggs-after-multiple-oral-dose-administration
#18
V De Vito, H Owen, M Marzoni, T Won Kim, A Poapolathep, M Giorgi
1. The aim of the study was to evaluate the pharmacokinetics of Tapentadol (TAP), a novel opioid analgesic, in laying hens after intravenous (IV) and oral (PO) administration and to quantify the concentrations of TAP residues in eggs. 2. Twenty healthy laying hens were divided into three groups: A (n=6), B (n=6) and C (n=8). The study was conducted in 2 phases. Groups A and B received TAP by IV and PO routes at the dose of 1 and 5 mg/kg, respectively. 3. No visible adverse effects were observed after administration of the drug...
November 8, 2017: British Poultry Science
https://www.readbyqxmd.com/read/29111148/effects-of-opioid-and-nonopioid-analgesics-on-canine-wheal-formation-and-cultured-human-mast-cell-degranulation
#19
Eric Schmidt-Rondon, Zhenping Wang, Shelle A Malkmus, Anna Di Nardo, Keith Hildebrand, Linda Page, Tony L Yaksh
Mast cell (MC) degranulation has been implicated in the side effect profile of a variety of clinically useful agents. Thus, after intrathecal delivery, formation of space-occupying, meningeally-derived masses may be related to local MC degranulation. We systematically characterized degranulating effects of opioid and nonopioid analgesics on cutaneous flares in the dog and in primary human MC (hMC) cultures. METHODS: Dogs were anesthetized with IV propofol and received intradermal (ID) injections (50μL)...
October 27, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29110363/synthesis-receptor-binding-studies-optical-spectroscopic-and-in-silico-structural-characterization-of-morphiceptin-analogs-with-cis-4-amino-l-proline-residues
#20
Anna Adamska-Bartłomiejczyk, Attila Borics, Csaba Tömböly, Szabolcs Dvorácskó, Marek Lisowski, Alicja Kluczyk, Grzegorz Wołczański, Justyna Piekielna-Ciesielska, Anna Janecka
Three novel morphiceptin analogs, in which Pro in position 2 and/or 4 was replaced by cis-4-aminoproline connected with the preceding amino acid through the primary amino group, were synthesized. The opioid receptor affinities, functional assay results, enzymatic degradation studies and experimental and in silico structural analysis of such analogs are presented. Copyright © 2017 European Peptide Society and John Wiley & Sons, Ltd.
November 7, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
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