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https://www.readbyqxmd.com/read/27915171/progress-in-the-development-of-%C3%AE-lactams-as-n-acylethanolamine-acid-amidase-naaa-inhibitors-synthesis-and-sar-study-of-new-potent-n-o-substituted-derivatives
#1
R Petracca, S Ponzano, S M Bertozzi, O Sasso, D Piomelli, T Bandiera, F Bertozzi
The anti-inflammatory effects resulting from raising the levels of palmitoylethanolamide (PEA), an endogenous bioactive lipid, led to envisage N-Acylethanolamine Acid Amidase (NAAA), the cysteine hydrolase mainly responsible for PEA degradation, as an attractive target for small molecule inhibitors. Previous work in our group identified serine-derived β-lactams as potent and systemically active inhibitors of NAAA activity. Aiming to expand the SAR study around this class of compounds, we investigated the effect of the substitution on the endocyclic nitrogen by designing and synthesizing a series of N-substituted β-lactams...
November 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27915078/analgesic-effect-of-coumarins-from-radix-angelicae-pubescentis-is-mediated-by-inflammatory-factors-and-trpv1-in-a-spared-nerve-injury-model-of-neuropathic-pain
#2
Ruili Li, Chao Zhao, Minna Yao, Ying Song, Yin Wu, Aidong Wen
ETHNOPHARMACOLOGICAL RELEVANCE: Coumarins from Radix angelicae pubescentis (CRAP) are a major active component that are isolated from dried roots of Angelica biserrata Yuan et Shan, which has been used clinically to cure headaches for a long period of time, and it is an effective treatment for pain. The aim of the present study was to investigate the analgesic effect of CRAP on a spared nerve injury (SNI) model of neuropathy. MATERIALS AND METHODS: Antinociceptive effects of CRAP were assessed in Sprague-Dawley male rats using a spared nerve injury model of neuropathic pain...
November 30, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27914470/symptom-profiles-and-inflammatory-markers-in-moderate-to-severe-copd
#3
Huong Q Nguyen, Jerald R Herting, Kenneth C Pike, Sina A Gharib, Gustavo Matute-Bello, Soo Borson, Ruth Kohen, Sandra G Adams, Vincent S Fan
BACKGROUND: Physical and psychological symptoms are the hallmark of patients' subjective perception of their illness. The purpose of this analysis was to determine if patients with COPD have distinctive symptom profiles and to examine the association of symptom profiles with systemic biomarkers of inflammation. METHODS: We conducted latent class analyses of three physical (dyspnea, fatigue, and pain) and two psychological symptoms (depression and anxiety) in 302 patients with moderate to severe COPD using baseline data from a longitudinal observational study of depression in COPD...
December 3, 2016: BMC Pulmonary Medicine
https://www.readbyqxmd.com/read/27914313/requests-for-cesarean-deliveries-the-politics-of-labor-pain-and-pain-relief-in-shanghai-china
#4
Eileen Wang
Cesarean section rates have risen dramatically in China within the past 25 years, particularly driven by non-medical factors and maternal requests. One major reason women request cesareans is the fear of labor pain, in a country where a minority of women are given any form of pain relief during labor. Drawing upon ethnographic fieldwork and in-depth interviews with 26 postpartum women and 8 providers at a Shanghai district hospital in June and July of 2015, this article elucidates how perceptions of labor pain and the environment of pain relief constructs the cesarean on maternal request...
November 24, 2016: Social Science & Medicine
https://www.readbyqxmd.com/read/27913981/the-challenges-of-anaesthesia-and-pain-relief-in-hip-fracture-care
#5
Rachel Cowan, Jun Hao Lim, Terence Ong, Ashok Kumar, Opinder Sahota
The care of the older person with hip fracture is complicated by their comorbid condition, limited physiological reserve, cognitive impairment and frailty. Two aspects of hip fracture management that have received considerable attention are how best to manage the pain associated with it and the ideal mode of anaesthesia. Existing literature has reported on the suboptimal treatment of pain in this orthogeriatric cohort. With recent advancements in medical care, a number of options have emerged as alternatives to conservative systemic analgesia...
December 3, 2016: Drugs & Aging
https://www.readbyqxmd.com/read/27913961/prediction-of-postoperative-clinical-recovery-of-drop-foot-attributable-to-lumbar-degenerative-diseases-via-a-bayesian-network
#6
Shota Takenaka, Hiroyuki Aono
BACKGROUND: Drop foot resulting from degenerative lumbar diseases can impair activities of daily living. Therefore, predictors of recovery of this symptom have been investigated using univariate or/and multivariate analyses. However, the conclusions have been somewhat controversial. Bayesian network models, which are graphic and intuitive to the clinician, may facilitate understanding of the prognosis of drop foot resulting from degenerative lumbar diseases. QUESTIONS/PURPOSES: (1) To show a layered correlation among predictors of recovery from drop foot resulting from degenerative lumbar diseases; and (2) to develop support tools for clinical decisions to treat drop foot resulting from lumbar degenerative diseases...
December 2, 2016: Clinical Orthopaedics and related Research
https://www.readbyqxmd.com/read/27913797/promoting-gait-recovery-and-limiting-neuropathic-pain-after-spinal-cord-injury-two-sides-of-the-same-coin
#7
Catherine Mercier, Meyke Roosink, Jason Bouffard, Laurent J Bouyer
Most persons living with a spinal cord injury experience neuropathic pain in the months following their lesion, at the moment where they receive intensive gait rehabilitation. Based on studies using animal models, it has been proposed that central sensitization in nociceptive pathways (maladaptive plasticity) and plasticity related to motor learning (adaptive plasticity) share common neural mechanisms and compete with each other. This article aims to address the discrepancy between the growing body of basic science literature supporting this hypothesis and the general belief in rehabilitation research that pain and gait rehabilitation represent two independent problems...
December 2, 2016: Neurorehabilitation and Neural Repair
https://www.readbyqxmd.com/read/27913581/a-proteomic-approach-to-analyse-the-aspirin-mediated-lysine-acetylome
#8
Michael H Tatham, Christian Cole, Paul Scullion, Ross Wilkie, Nicholas J Westwood, Lesley A Stark, Ronald T Hay
Aspirin, or acetylsalicylic acid is widely used to control pain, inflammation and fever. Important to this function is its ability to irreversibly acetylate cyclooxygenases at active site serines. Aspirin has the potential to acetylate other amino-acid side-chains, leading to the possibility that aspirin-mediated lysine acetylation could explain some of its as-yet unexplained drug actions or side-effects. Using isotopically labeled aspirin-d3, in combination with acetylated lysine purification and LC-MS/MS, we identified over 12000 sites of lysine acetylation from cultured human cells...
December 2, 2016: Molecular & Cellular Proteomics: MCP
https://www.readbyqxmd.com/read/27913310/targeted-disruption-of-the-orphan-receptor-gpr151-does-not-alter-pain-related-behaviour-despite-a-strong-induction-in-dorsal-root-ganglion-expression-in-a-model-of-neuropathic-pain
#9
Fiona E Holmes, Niall Kerr, Ying-Ju Chen, Penny Vanderplank, Craig A McArdle, David Wynick
BACKGROUND: Gpr151 is an orphan GPCR whose function is unknown. The restricted pattern of neuronal expression in the habenula, dorsal horn of the spinal cord and dorsal root ganglion plus homology with the galanin family of receptors imply a role in nociception. RESULTS: Real-time quantitative RT-PCR demonstrated a 49.9±2.9 fold highly significant (P<0.001) increase in Gpr151 mRNA expression in the dorsal root ganglion 7days after the spared nerve injury model of neuropathic pain...
November 29, 2016: Molecular and Cellular Neurosciences
https://www.readbyqxmd.com/read/27912939/dietary-supplementation-is-more-prevalent-among-adults-with-arthritis-in-the-united-states-population
#10
Patrick B Wilson
OBJECTIVES: Sparse data are available to describe the prevalence of dietary supplementation among individuals with arthritis. Using a nationally representative sample, this investigation assessed the prevalence of dietary supplement use among Americans self-reporting arthritis. SETTING AND DESIGN: Data from 4606 participants of the 2011-2012 National Health and Nutrition Examination Survey were analyzed, including from 1170 participants self-reporting arthritis...
December 2016: Complementary Therapies in Medicine
https://www.readbyqxmd.com/read/27912744/quality-of-life-after-stroke-in-pakistan
#11
Wardah Khalid, Shafquat Rozi, Tazeen Saeed Ali, Iqbal Azam, Michael T Mullen, Saleem Illyas, Qamar Un-Nisa, Nabila Soomro, Ayeesha Kamran Kamal
BACKGROUND: There is very little information about the quality of life (QOL) of stroke survivors in LMIC countries with underdeveloped non communicable health infrastructures, who bear two thirds of the global stroke burden. METHODOLOGY: We used a sequential mix methods approach. First, a quantitative analytical cross-sectional study was conducted on 700 participants, who constituted 350 stroke survivor and their caregiver dyads. QOL of stroke survivor was assessed via Stroke Specific Quality of Life Scale (SSQOLS) whereas QOL of caregivers was assessed through RAND-36...
December 3, 2016: BMC Neurology
https://www.readbyqxmd.com/read/27912032/pain-input-impairs-recovery-after-spinal-cord-injury-treatment-with-lidocaine
#12
Joel D Turtle, Misty M Strain, Miriam Aceves, Yung-Jen Huang, Joshua A Reynolds, Michelle A Hook, James W Grau
More than 90% of spinal cord injuries are caused by traumatic accidents and are often associated with other tissue damage (polytrauma) that can provide a source of continued pain input during recovery. In a clinically relevant spinal cord contusion injury model, prior work has shown that noxious stimulation at an intensity that engages pain (C) fibers soon after injury augments secondary injury and impairs functional recovery. Noxious input increases the expression of pro-inflammatory cytokines (interleukin 1β and 18), cellular signals associated with cell death (caspase 3 and 8), and physiological signs of hemorrhage...
December 2, 2016: Journal of Neurotrauma
https://www.readbyqxmd.com/read/27911782/egfr-signaling-is-critical-for-maintaining-the-superficial-layer-of-articular-cartilage-and-preventing-osteoarthritis-initiation
#13
Haoruo Jia, Xiaoyuan Ma, Wei Tong, Basak Doyran, Zeyang Sun, Luqiang Wang, Xianrong Zhang, Yilu Zhou, Farid Badar, Abhishek Chandra, X Lucas Lu, Yang Xia, Lin Han, Motomi Enomoto-Iwamoto, Ling Qin
Osteoarthritis (OA) is the most common joint disease, characterized by progressive destruction of the articular cartilage. The surface of joint cartilage is the first defensive and affected site of OA, but our knowledge of genesis and homeostasis of this superficial zone is scarce. EGFR signaling is important for tissue homeostasis. Immunostaining revealed that its activity is mostly dominant in the superficial layer of healthy cartilage but greatly diminished when OA initiates. To evaluate the role of EGFR signaling in the articular cartilage, we studied a cartilage-specific Egfr-deficient (CKO) mouse model (Col2-Cre EgfrWa5/flox)...
November 28, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27911382/a-simple-mechanical-procedure-to-create-limbal-stem-cell-deficiency-in-mouse
#14
Neda Afsharkhamseh, Elham Ghahari, Medi Eslani, Ali R Djalilian
Limbal stem cell deficiency (LSCD) is a state of malfunction or loss of limbal epithelial stem cells, after which the corneal epithelium is replaced with conjunctiva. Patients suffer from recurrent corneal defects, pain, inflammation, and loss of vision. Previously, a murine model of LSCD was described and compared to two other models. The goal was to produce a consistent mouse model of LSCD that both mimics the phenotype in humans and lasts long enough to make it possible to study the disease pathophysiology and to evaluate new treatments...
November 17, 2016: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/27911108/comparative-study-of-dual-pulsed-1-064-nm-q-switched-nd-yag-laser-and-single-pulsed-1-064-nm-q-switched-nd-yag-laser-by-using-zebrafish-model-and-prospective-split-face-analysis-of-facial-melasma
#15
Hee Won Jang, Seung Hyun Chun, Hae Chul Park, Hwa Jung Ryu, Il-Hwan Kim
BACKGROUND: Recently dual-pulsed low-fluence 1,064 nm Q-switched Nd:YAG (QSNY) laser has been developed for reducing complication during melasma treatment. OBJECTIVE: Comparison of the efficacy and safety between dual-pulsed mode and single-pulsed mode for the treatment of melasma. MATERIALS AND METHODS: In preclinical study, adult zebrafish were irradiated with dual-pulsed and single-pulsed mode. Changes of melanophore and cell death were assessed...
December 2, 2016: Journal of Cosmetic and Laser Therapy: Official Publication of the European Society for Laser Dermatology
https://www.readbyqxmd.com/read/27910899/glial-pannexin1-contributes-to-tactile-hypersensitivity-in-a-mouse-model-of-orofacial-pain
#16
Regina Hanstein, Menachem Hanani, Eliana Scemes, David C Spray
Drug studies in animal models have implicated pannexin1 (Panx1) in various types of pain, including trigeminal hypersensitivity, neuropathic pain and migraine. However, the tested drugs have limited specificity and efficacy so that direct evidence for Panx1 contribution to pain has been lacking. We here show that tactile hypersensitivity is markedly attenuated by deletion of Panx1 in a mouse model of chronic orofacial pain; in this model, trigeminal ganglion Panx1 expression and function are markedly enhanced...
December 2, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27910870/antinociceptive-profile-of-levo-tetrahydropalmatine-in-acute-and-chronic-pain-mice-models-role-of-spinal-sigma-1-receptor
#17
Dong-Wook Kang, Ji-Young Moon, Jae-Gyun Choi, Suk-Yun Kang, Yeonhee Ryu, Jin Bong Park, Jang-Hern Lee, Hyun-Woo Kim
We have recently reported that repeated systemic treatments of extract from Corydalis yanhusuo alleviate neuropathic pain and levo-tetrahydropalmatine (l-THP) is one of active components from Corydalis. We designed this study to investigate antinociceptive effect of l-THP in acute and chronic pain models and related mechanism within the spinal cord. We found that intraperitoneal pretreatment with l-THP significantly inhibited the second phase of formalin-induced pain behavior. In addition, intrathecal as well as intraperitoneal pretreatment with l-THP reduced the mechanical allodynia (MA) induced by direct activation of sigma-1 receptor (Sig-1)...
December 2, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27910150/randomised-clinical-trial-exploratory-phase-2-study-of-ono-2952-in-diarrhoea-predominant-irritable-bowel-syndrome
#18
W E Whitehead, K Duffy, J Sharpe, T Nabata, M Bruce
BACKGROUND: ONO-2952 is a novel and selective inhibitor of translocator protein 18 kDa that reduces stress-induced defecation and visceral hyperalgesia in rat models. AIM: To evaluate the efficacy and safety of ONO-2952 in females with irritable bowel syndrome with diarrhoea in an exploratory proof-of-concept study. METHODS: A randomised, double-blind, placebo-controlled study was conducted at 49 US centres. Two hundred subjects with irritable bowel syndrome with diarrhoea (Rome III criteria) were randomised to ONO-2952 20 mg, or 60 mg, or placebo...
January 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/27910097/chronic-migraine-an-update-on-physiology-imaging-and-the-mechanism-of-action-of-two-available-pharmacologic-therapies
#19
Sheena K Aurora, Mitchell F Brin
Several lines of research support the hypothesis that migraine is a spectrum of illness, with clinical symptoms that vary along a continuum from episodic migraine to chronic migraine. Physiologic changes may result in episodic migraine evolving into chronic migraine over months to years in susceptible individuals. With chronification, headache frequency increases, becoming more disabling and less responsive to therapy. Neurophysiologic and functional imaging research has reported that chronic migraine may be associated with severity-specific metabolic, functional, and structural abnormalities in the brainstem...
December 2, 2016: Headache
https://www.readbyqxmd.com/read/27909853/impact-of-irt-item-misfit-on-score-estimates-and-severity-classifications-an-examination-of-promis-depression-and-pain-interference-item-banks
#20
Yue Zhao
PURPOSE: In patient-reported outcome research that utilizes item response theory (IRT), using statistical significance tests to detect misfit is usually the focus of IRT model-data fit evaluations. However, such evaluations rarely address the impact/consequence of using misfitting items on the intended clinical applications. This study was designed to evaluate the impact of IRT item misfit on score estimates and severity classifications and to demonstrate a recommended process of model-fit evaluation...
December 1, 2016: Quality of Life Research
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