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https://www.readbyqxmd.com/read/28626043/the-diverse-roles-of-arrestin-scaffolds-in-g-protein-coupled-receptor-signaling
#1
REVIEW
Yuri K Peterson, Louis M Luttrell
The visual/β-arrestins, a small family of proteins originally described for their role in the desensitization and intracellular trafficking of G protein-coupled receptors (GPCRs), have emerged as key regulators of multiple signaling pathways. Evolutionarily related to a larger group of regulatory scaffolds that share a common arrestin fold, the visual/β-arrestins acquired the capacity to detect and bind activated GPCRs on the plasma membrane, which enables them to control GPCR desensitization, internalization, and intracellular trafficking...
July 2017: Pharmacological Reviews
https://www.readbyqxmd.com/read/28625413/invisible-people-with-invisible-pain-a-commentary-on-even-my-sister-says-i-m-acting-like-a-crazy-to-get-a-check-race-gender-and-moral-boundary-work-in-women-s-claims-of-disabling-chronic-pain
#2
Joanna Kempner
This commentary to Pryma's (2017) article on women with fibromyalgia argues that intersectional approaches to health research can reveal not only how racialized institutions shape illness experience and medical care, but also how these institutions make some individuals visible, while rendering others invisible. Perhaps by adopting an intersectional approach to understanding health, we can start to unpack the multiple jeopardies faced by people of color in pain.
June 10, 2017: Social Science & Medicine
https://www.readbyqxmd.com/read/28623508/clinical-pharmacokinetic-characteristics-of-cebranopadol-a-novel-first-in-class-analgesic
#3
Elke Kleideiter, Chiara Piana, Shaonan Wang, Robert Nemeth, Michael Gautrois
BACKGROUND AND OBJECTIVES: Cebranopadol is a novel first-in-class analgesic acting as a nociceptin/orphanin FQ peptide and opioid peptide receptor agonist with central analgesic activity. It is currently in clinical development for the treatment of chronic pain conditions. This trial focuses on the clinical pharmacokinetic (PK) properties of cebranopadol after oral single- and multiple-dose administration. METHODS: The basic PK properties of cebranopadol were assessed by means of noncompartmental methods in six phase I clinical trials in healthy subjects and patients...
June 16, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28593417/laparoscopic-approach-for-the-treatment-of-chronic-groin-pain-after-inguinal-hernia-repair-laparoscopic-approach-for-inguinodynia
#4
Bruce Ramshaw, Vincent Vetrano, Mayuri Jagadish, Brandie Forman, Eric Heidel, Matthew Mancini
BACKGROUND: Traditional methods of clinical research may not be adequate to improve the value of care for patients with complex medical problems such as chronic pain after inguinal hernia repair. This problem is very complex with many potential factors contributing to the development of this complication. METHODS: We have implemented a clinical quality improvement (CQI) effort in an attempt to better measure and improve outcomes for patients suffering with chronic groin pain (inguinodynia) after inguinal hernia repair...
June 7, 2017: Surgical Endoscopy
https://www.readbyqxmd.com/read/28592614/the-cannabinoid-cb2-agonist-gw405833-suppresses-inflammatory-and-neuropathic-pain-through-a-cb1-mechanism-that-is-independent-of-cb2-receptors-in-mice
#5
Ai-Ling Li, Lawrence M Carey, Ken Mackie, Andrea G Hohmann
GW405833, widely accepted as a cannabinoid CB2 agonist, suppresses pathological pain in preclinical models without unwanted central side effects of CB1 agonists. However, recent in vitro studies suggest that GW405833 may also behave as a non-competitive CB1 antagonist, suggesting that its pharmacology is more complex than initially appreciated. Here, we further investigated the pharmacological specificity of in vivo antinociceptive actions of GW405833 in models of neuropathic (i.e. partial sciatic nerve ligation (PSNL) model) and inflammatory (i...
June 7, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28587921/cxcl1-cxcr2-signaling-in-pathological-pain-role-in-peripheral-and-central-sensitization
#6
REVIEW
Rangel L Silva, Alexandre H Lopes, Rafaela M Guimarães, Thiago M Cunha
Pathological pain conditions can be triggered after peripheral nerve injury and/or inflammation. It is associated with plasticity of nociceptive pathway in which pain is prolonged even after healing of the injured tissue. Generally combinations of analgesic drugs are not sufficient to achieve selective palliation from chronic pain, besides causing a greater number of side effects. In order to identify novel alternatives for more effective treatments, it is necessary to clarify the underlying mechanisms of pathological pain...
June 3, 2017: Neurobiology of Disease
https://www.readbyqxmd.com/read/28576672/watching-television-for-more-than-two-hours-increases-the-likelihood-of-reporting-poor-sleep-quality-among-brazilian-schoolteachers
#7
Sara Carolina Scremin de Souza, Marcela Zambrim Campanini, Selma Maffei de Andrade, Alberto Durán González, Juliana Moura de Melo, Arthur Eumann Mesas
Although time spent watching television and sleep problems have increased in the last few decades, it is unclear whether these conditions are associated in working adults after controlling for lifestyle, job characteristics and other individual aspects. The present study analyzed the association between time spent watching television and sleep quality among teachers from public schools in Londrina, Brazil. In this cross-sectional study, information from the Pittsburgh Sleep Quality Index (PSQI) and about time spent watching television was obtained during personal interviews...
May 30, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28576452/naldemedine-versus-placebo-for-opioid-induced-constipation-compose-1-and-compose-2-two-multicentre-phase-3-double-blind-randomised-parallel-group-trials
#8
Martin Hale, James Wild, Jyotsna Reddy, Tadaaki Yamada, Juan Camilo Arjona Ferreira
BACKGROUND: Opioid-induced constipation is a frequent side-effect of opioid treatment, and standard interventions have limited or inconsistent efficacy. This study assessed the efficacy and safety of naldemedine, a peripherally acting μ-opioid receptor antagonist, for the treatment of opioid-induced constipation in patients with chronic non-cancer pain. METHODS: We report two double-blind, randomised, placebo-controlled trials in adults with chronic non-cancer pain and opioid-induced constipation...
May 30, 2017: Lancet. Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/28571535/nonsteroidal-anti-inflammatory-drugs-exploiting-bivalent-coxib-tp-antagonists-for-the-control-of-cardiovascular-risk
#9
Silvia Carnevali, Carola Buccellati, Chiara Bolego, Massimo Bertinaria, Rovati G Enrico, Angelo Sala
BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) are some of the most widely prescribed or dispensed analgesics and antipyretics that act by inhibiting prostaglandins (PGs) and thromboxane synthesis. After the identification of a second isoform of COX, the pharmaceutical research focused on developing COX-2-selective drugs (COXIBs) considered as second generation NSAIDs that would retain the anti-inflammatory and analgesic activities of traditional NSAID without blunting the gastrointestinal cytoprotection sustained by COX1-derived products such as PGE2...
June 1, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28565998/gabab-receptors-mediated-tonic-inhibition-of-glutamate-release-from-a%C3%AE-fibers-in-rat-laminae-iii-iv-of-the-spinal-cord-dorsal-horn
#10
Chiara Salio, Adalberto Merighi, Rita Bardoni
Presynaptic GABAB receptors (GABABRs) are highly expressed in dorsal root ganglion neurons and spinal cord dorsal horn. GABABRs located in superficial dorsal horn play an important antinociceptive role, by acting at both pre- and postsynaptic sites. GABABRs expressed in deep dorsal horn could be involved in the processing of touch sensation and possibly in the generation of tactile allodynia in chronic pain. The objective of this study was to characterize the morphological and functional properties of GABABRs expressed on Aβ fibers projecting to lamina III/IV and to understand their role in modulating excitatory synaptic transmission...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28546769/treatment-of-chronic-low-back-pain-new-approaches-on-the-horizon
#11
REVIEW
Nebojsa Nick Knezevic, Shane Mandalia, Jennifer Raasch, Ivana Knezevic, Kenneth D Candido
Back pain is the second leading cause of disability among American adults and is currently treated either with conservative therapy or interventional pain procedures. However, the question that remains is whether we, as physicians, have adequate therapeutic options to offer to the patients who suffer from chronic low back pain but fail both conservative therapy and interventional pain procedures before they consider surgical options such as discectomy, disc arthroplasty, or spinal fusion. The purpose of this article is to review the potential novel therapies that are on the horizon for the treatment of chronic low back pain...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28546566/a-diastereoselective-synthesis-of-cebranopadol-a-novel-analgesic-showing-nop-mu-mixed-agonism
#12
Anna Fantinati, Sara Bianco, Remo Guerrini, Severo Salvadori, Salvatore Pacifico, Maria Camilla Cerlesi, Girolamo Calo, Claudio Trapella
A diastereoselective synthesis of the title compound as a single E diastereomer has been efficiently accomplished by assembling the featured pyrano-indole scaffold of the spiro[cyclohexane-dihydropyrano[3,4-b]-indole]-amine framework through an oxa-Pictet-Spengler reaction, promoted by a cheap and green Zeolite catalyst. Basic pharmacological experiments demonstrate that Cebranopadol acts as a mixed nociception/orphanin FQ (NOP) and mu (MOP) opioid receptor agonist useful for treatment of chronic pain.
May 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28536367/a-brief-review-of-the-pharmacology-of-amitriptyline-and-clinical-outcomes-in-treating-fibromyalgia
#13
REVIEW
Kim Lawson
Fibromyalgia is a complex chronic condition characterized by pain, physical fatigue, sleep disorder and cognitive impairment. Evidence-based guidelines recommend antidepressants as treatments of fibromyalgia where tricyclics are often considered to have the greatest efficacy, with amitriptyline often being a first-line treatment. Amitriptyline evokes a preferential reduction in pain and fatigue of fibromyalgia, and in the Fibromyalgia Impact Questionnaire (FIQ) score, which is a quality of life assessment. The multimodal profile of the mechanisms of action of amitriptyline include monoamine reuptake inhibition, receptor modulation and ion channel modulation...
May 17, 2017: Biomedicines
https://www.readbyqxmd.com/read/28529168/opioids-in-gastroenterology-treating-adverse-effects-and-creating-therapeutic-benefits
#14
Michael Camilleri, Anthony Lembo, David A Katzka
The use of opioid medications on both an acute and chronic basis is ubiquitous in the U.S. As opioid receptors densely populate the gastrointestinal tract, symptoms and side effects can be expected in these patients. In the esophagus, dysmotility may result manifesting with dysphagia and a syndrome indistinguishable from primary achalasia. In the stomach, a marked delay in gastric emptying may ensue with postprandial nausea and early satiety. Postoperatively, particularly with abdominal surgery, opioid induced ileus may ensue...
May 18, 2017: Clinical Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28527055/cluster-headache-present-and-future-therapy
#15
Massimo Leone, Alessandro Giustiniani, Alberto Proietti Cecchini
Cluster headache is characterized by severe, unilateral headache attacks of orbital, supraorbital or temporal pain lasting 15-180 min accompanied by ipsilateral lacrimation, rhinorrhea and other cranial autonomic manifestations. Cluster headache attacks need fast-acting abortive agents because the pain peaks very quickly; sumatriptan injection is the gold standard acute treatment. First-line preventative drugs include verapamil and carbolithium. Other drugs demonstrated effective in open trials include topiramate, valproic acid, gabapentin and others...
May 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28523574/medical-management-of-pain-in-chronic-pancreatitis
#16
REVIEW
Vikesh K Singh, Asbjørn M Drewes
The medical management of pain in chronic pancreatitis continues to pose significant challenges for clinicians caring for these patients. There are increasing data, suggesting that pain in chronic pancreatitis is largely due to peripheral and central sensitization that evolves, over time, as a result of nociceptive afferent associated with chronic inflammation and fibrosis of the pancreas. In many instances, patients rapidly progress to requiring opioid analgesics for the adequate treatment of pain despite the unequivocal risks associated with the long-term use of these drugs...
May 18, 2017: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/28508651/sugar-breathing-glycopolymersomes-for-regulating-glucose-level
#17
Yufen Xiao, Hui Sun, Jianzhong Du
Diabetes mellitus is a chronic, life-threatening illness that affects people of every age and ethnicity. It is a long-term pain for those who are affected and must regulate their blood glucose level by frequent subcutaneous injection of insulin every day. Herein, we propose a noninsulin and antidiabetic drug-free strategy for regulating blood glucose level by a nanosized "sugar sponge" which is a lectin-bound glycopolymersome capable of regulating glucose due to the dynamic recognition between the lectin and different carbohydrates...
June 7, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28483271/-mindful-neuropsychology-mindfulness-based-cognitive-remediation
#18
E Bulzacka, S Lavault, A Pelissolo, C Bagnis Isnard
OBJECTIVES: Mindfulness based interventions (MBI) have recently gained much interest in western medicine. MBSR paradigm is based on teaching participants to pay complete attention to the present experience and act nonjudgmentally towards stressful events. During this mental practice the meditator focuses his or her attention on the sensations of the body. While the distractions (mental images, thoughts, emotional or somatic states) arise the participant is taught to acknowledge discursive thoughts and cultivate the state of awareness without immediate reaction...
May 5, 2017: L'Encéphale
https://www.readbyqxmd.com/read/28463868/application-of-primary-care-guideline-for-chronic-low-back-pain-in-the-emergency-department
#19
Rebeca M Tacy, Sherry Donaworth, Kathleen Ballman
Chronic low back pain (CLBP) is a primary care condition that overflows into the emergency department (ED). No ED-specific practice guideline exists for the management of patients with CLBP in the ED setting. Back pain is a common chief complaint, with cases of CLBP making up to 50% of the patients seen with back pain in an urban, freestanding ED affiliated with a multicampus health system in the Midwest where 25% of patients live below the poverty line and 21.8% do not have primary care. Kolcaba's Theory of Comfort guides the implementation of an evidence-based practice application project...
April 2017: Advanced Emergency Nursing Journal
https://www.readbyqxmd.com/read/28460228/a-disposition-kinetic-study-of-tramadol-in-bile-duct-ligated-rats-in-perfused-rat-liver-model
#20
Zohre Esmaeili, Saeid Mohammadi, Alireza Nezami, Mohammad Reza Rouini, Yalda Hosseinzadeh Ardakani, Hoda Lavasani, Mahmoud Ghazi-Khansari
Tramadol hydrochloride is a centrally acting synthetic opioid analgesic drug and is used to treat chronic pain. In this study, the effects of Bile Duct Ligation (BDL) on the pharmacokinetics of tramadol in a liver recirculating perfusion system of male rats were used. Twenty-four Wistar male rats were randomly divided into four groups: control, sham and two weeks BDL and four weeks BDL. Serum levels of liver enzymes were measured before perfusion and the pharmacokinetics of tramadol was evaluated by using liver recirculating perfusion system...
July 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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