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endogenous analgesia

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https://www.readbyqxmd.com/read/28341345/the-signaling-signature-of-the-neurotensin-type-1-receptor-with-endogenous-ligands
#1
Élie Besserer-Offroy, Rebecca L Brouillette, Sandrine Lavenus, Ulrike Froehlich, Andrea Brumwell, Alexandre Murza, Jean-Michel Longpré, Éric Marsault, Michel Grandbois, Philippe Sarret, Richard Leduc
The human neurotensin 1 receptor (hNTS1) is a G protein-coupled receptor involved in many physiological functions, including analgesia, hypothermia, and hypotension. To gain a better understanding of which signaling pathways or combination of pathways are linked to NTS1 activation and function, we investigated the ability of activated hNTS1, which was stably expressed by CHO-K1 cells, to directly engage G proteins, activate second messenger cascades and recruit β-arrestins. Using BRET-based biosensors, we found that neurotensin (NT), NT(8-13) and neuromedin N (NN) activated the Gαq-, Gαi1-, GαoA-, and Gα13-protein signaling pathways as well as the recruitment of β-arrestins 1 and 2...
March 22, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28339438/the-role-of-autonomic-function-in-exercise-induced-endogenous-analgesia-a-case-control-study-in-myalgic-encephalomyelitis-chronic-fatigue-syndrome-and-healthy-people
#2
Jessica Van Oosterwijck, Uros Marusic, Inge De Wandele, Lorna Paul, Mira Meeus, Greta Moorkens, Luc Lambrecht, Lieven Danneels, Jo Nijs
BACKGROUND: Patients with myalgic encephalomyelitis / chronic fatigue syndrome (ME/CFS) are unable to activate brain-orchestrated endogenous analgesia (or descending inhibition) in response to exercise. This physiological impairment is currently regarded as one factor explaining post-exertional malaise in these patients. Autonomic dysfunction is also a feature of ME/CFS. OBJECTIVES: This study aims to examine the role of the autonomic nervous system in exercise-induced analgesia in healthy people and those with ME/CFS, by studying the recovery of autonomic parameters following aerobic exercise and the relation to changes in self-reported pain intensity...
March 2017: Pain Physician
https://www.readbyqxmd.com/read/28337942/is-fetal-analgesia-necessary-during-prenatal-surgery
#3
C V Bellieni, S Vannuccini, F Petraglia
Fetal anesthesia is still matter of debate: some authors hypothesize that several intrauterine endogenous neuroinhibitors (ENIn) anesthetize the fetus, keeping it in a constant state of sleep, and making pharmacological fetal anaesthesia useless for fetal surgery. AIM: To retrieve evidences about fetal pain, fetal arousability and about the level of sedation induced by the ENIn, in order to assess the necessity of direct fetal anesthesia during prenatal fetal surgery. METHODS: We performed a careful literature review (1990-2016) on fetal arousability, and on the possibility that ENIn at the average fetal blood levels induce actual anesthesia...
March 24, 2017: Journal of Maternal-fetal & Neonatal Medicine
https://www.readbyqxmd.com/read/28322978/delta-opioid-receptor-antagonism-leads-to-excessive-ethanol-consumption-in-mice-with-enhanced-activity-of-the-endogenous-opioid-system
#4
Piotr Poznanski, Anna Lesniak, Michal Korostynski, Klaudia Szklarczyk, Marzena Lazarczyk, Piotr Religa, Magdalena Bujalska-Zadrozny, Bogdan Sadowski, Mariusz Sacharczuk
The opioid system modulates the central reinforcing effects of ethanol and participates in the etiology of addiction. However, the pharmacotherapy of ethanol dependence targeted on the opioid system is little effective and varies due to individual patients' sensitivity. In the present study, we used two mouse lines with high (HA) and low (LA) activity of the endogenous opioid system to analyze the effect of opioid receptor blockade on ethanol drinking behavior. We found that LA and HA lines characterized by divergent magnitudes of swim stress-induced analgesia also differ in ethanol intake and preference...
March 18, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28284950/naloxone-exacerbates-memory-impairments-and-depressive-like-behavior-after-mild-traumatic-brain-injury-mtbi-in-mice-with-upregulated-opioid-system-activity
#5
Anna Lesniak, Pawel Leszczynski, Magdalena Bujalska-Zadrozny, Chaim G Pick, Mariusz Sacharczuk
The neuroprotective role of the endogenous opioid system in the pathophysiological sequelae of brain injury remains largely ambiguous. Noteworthy, almost no data is available on how its genetically determined activity influences the outcome of mild traumatic brain injury. Thus, the aim of our study was to examine the effect of opioid receptor blockage on cognitive impairments produced by mild traumatic brain injury in mice selectively bred for high (HA) and low (LA) swim-stress induced analgesia that show innate divergence in opioid system activity...
March 8, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28279705/lower-placebo-responses-after-long-term-exposure-to-fibromyalgia-pain
#6
Eva Kosek, Annelie Rosen, Serena Carville, Ernest Choy, Richard H Gracely, Hanke Marcus, Frank Petzke, Martin Ingvar, Karin B Jensen
Knowledge about placebo mechanisms in patients with chronic pain is scarce. Fibromyalgia syndrome (FM) is associated with dysfunctions of central pain inhibition, and since placebo analgesia entails activation of endogenous pain inhibition, we hypothesized that long-term exposure to FM pain would negatively affect placebo responses. Here we examined the placebo-group (n=37, mean age 45 years) from a 12-week, randomized, double-blind, placebo-controlled trial investigating the effects of milnacipran or placebo...
March 6, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28235500/action-of-%C3%AE-endorphin-and-nonsteroidal-anti-inflammatory-drugs-and-the-possible-effects-of-nonsteroidal-anti-inflammatory-drugs-on-%C3%AE-endorphin
#7
REVIEW
Yuan-Hang Luan, Di Wang, Qi Yu, Xiao-Qing Chai
This study aimed to review research on the effects of nonsteroidal anti-inflammatory drugs (NSAIDs) on β-endorphin. NSAIDs are commonly used as anti-inflammatory and analgesic drugs. They are well known for inducing peripheral analgesia by inhibiting cyclooxygenase (COX). However, an increasing number of studies have shown that NSAIDs have an analgesic effect not only in the periphery but also at the center. It means that a central analgesic mechanism of the action of NSAIDs exists besides the peripheral mechanism, and the central mechanism likely involves β-endorphin...
February 2017: Journal of Clinical Anesthesia
https://www.readbyqxmd.com/read/28169487/endogenous-analgesic-effect-of-pregabalin-a-double-blind-and-randomized-controlled-trial
#8
S Sugimine, S Saito, T Araki, K Yamamoto, H Obata
BACKGROUND: Conditioned pain modulation (CPM) is widely used to measure endogenous analgesia, and a recent study indicated that drugs that act on endogenous analgesia are more effective in individuals with lower CPM. Recent animal studies have indicated that pregabalin activates endogenous analgesia by stimulating the descending pain inhibitory system. The present study examined whether the analgesic effect of pregabalin is greater in individuals with lower original endogenous analgesia using CPM...
February 7, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28166793/cytotoxic-t-cells-modulate-inflammation-and-endogenous-opioid-analgesia-in-chronic-arthritis
#9
Uta Baddack-Werncke, Melanie Busch-Dienstfertig, Sara González-Rodríguez, Santhosh Chandar Maddila, Jenny Grobe, Martin Lipp, Christoph Stein, Gerd Müller
BACKGROUND: This study examined the development of chronic pain, a cardinal symptom of rheumatoid arthritis (RA), in mice with antigen- and collagen-induced arthritis (ACIA). Since the role of CD8(+) T cells in arthritis is controversial, we investigated the consequences of CD8-depletion on arthritis development and opioid modulation of pain in this novel model of chronic autoimmune arthritis. METHODS: Disease severity in control and CD8-depleted animals was determined by histological assessment of knee-joint sections and measurement of autoantibody formation...
February 6, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28134928/blocking-microglial-pannexin-1-channels-alleviates-morphine-withdrawal-in-rodents
#10
Nicole E Burma, Robert P Bonin, Heather Leduc-Pessah, Corey Baimel, Zoe F Cairncross, Michael Mousseau, Jhenkruthi Vijaya Shankara, Patrick L Stemkowski, Dinara Baimoukhametova, Jaideep S Bains, Michael C Antle, Gerald W Zamponi, Catherine M Cahill, Stephanie L Borgland, Yves De Koninck, Tuan Trang
Opiates are essential for treating pain, but termination of opiate therapy can cause a debilitating withdrawal syndrome in chronic users. To alleviate or avoid the aversive symptoms of withdrawal, many of these individuals continue to use opiates. Withdrawal is therefore a key determinant of opiate use in dependent individuals, yet its underlying mechanisms are poorly understood and effective therapies are lacking. Here, we identify the pannexin-1 (Panx1) channel as a therapeutic target in opiate withdrawal...
March 2017: Nature Medicine
https://www.readbyqxmd.com/read/28096471/resolving-the-brainstem-contributions-to-attentional-analgesia
#11
Jonathan C W Brooks, Wendy-Elizabeth Davies, Anthony E Pickering
Previous human imaging studies manipulating attention or expectancy have identified the periaqueductal gray (PAG) as a key brainstem structure implicated in endogenous analgesia. However, animal studies indicate that PAG analgesia is mediated largely via caudal brainstem structures, such as the rostral ventromedial medulla (RVM) and locus coeruleus (LC). To identify their involvement in endogenous analgesia, we used brainstem optimized, whole-brain imaging to record responses to concurrent thermal stimulation (left forearm) and visual attention tasks of titrated difficulty in 20 healthy subjects...
March 1, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28077540/leukemia-inhibitory-factor-lif-potentiates-antinociception-activity-and-inhibits-tolerance-induction-of-opioids
#12
H J Tu, K H Kang, S Y Ho, H C Liou, H H Liou, C P Lin, W M Fu
BACKGROUND: The efficacy of opioids typically decreases after long-term use owing to the development of tolerance. Glial activation and the upregulation of proinflammatory cytokines are related to the induction of tolerance. We investigated the effect of leukemia inhibitory factor (LIF) on morphine analgesia and tolerance. METHODS: LIF concentrations in rat spinal cords were measured by polymerase chain reaction (PCR) and enzyme-linked immunosorbent assay (ELISA) after morphine administration...
October 2016: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/28074005/synergistic-regulation-of-serotonin-and-opioid-signaling-contributes-to-pain-insensitivity-in-nav1-7-knockout-mice
#13
Jörg Isensee, Leonhardt Krahé, Katharina Moeller, Vanessa Pereira, Jane E Sexton, Xiaohui Sun, Edward Emery, John N Wood, Tim Hucho
Genetic loss of the voltage-gated sodium channel Nav1.7 (Nav1.7(-/-)) results in lifelong insensitivity to pain in mice and humans. One underlying cause is an increase in the production of endogenous opioids in sensory neurons. We analyzed whether Nav1.7 deficiency altered nociceptive heterotrimeric guanine nucleotide-binding protein-coupled receptor (GPCR) signaling, such as initiated by GPCRs that respond to serotonin (pronociceptive) or opioids (antinociceptive), in sensory neurons. We found that the nociceptive neurons of Nav1...
January 10, 2017: Science Signaling
https://www.readbyqxmd.com/read/28049031/the-efficacy-of-dynorphin-fragments-at-the-%C3%AE%C2%BA-%C3%AE-and-%C3%AE-opioid-receptor-in-transfected-hek-cells-and-in-an-animal-model-of-unilateral-peripheral-inflammation
#14
M Morgan, A Heffernan, F Benhabib, S Wagner, A K Hewavitharana, P N Shaw, P J Cabot
Dynorphin 1-17 is an endogenous peptide that is released at sites of inflammation by leukocytes, binding preferentially to κ-opioid receptors (KOP) to mediate nociception. We have previously shown that dynorphin 1-17 is rapidly biotransformed to smaller peptide fragments in inflamed tissue homogenate. This study aimed to determine the efficacy and potency of selected dynorphin fragments produced in an inflamed environment at the KOP, μ and δ-opioid receptors (MOP and DOP respectively) and in a model of inflammatory pain...
March 2017: Peptides
https://www.readbyqxmd.com/read/28012859/endogenous-opiates-and-behavior-2015
#15
REVIEW
Richard J Bodnar
This paper is the thirty-eighth consecutive installment of the annual review of research concerning the endogenous opioid system. It summarizes papers published during 2015 that studied the behavioral effects of molecular, pharmacological and genetic manipulation of opioid peptides, opioid receptors, opioid agonists and opioid antagonists. The particular topics that continue to be covered include the molecular-biochemical effects and neurochemical localization studies of endogenous opioids and their receptors related to behavior, and the roles of these opioid peptides and receptors in pain and analgesia, stress and social status, tolerance and dependence, learning and memory, eating and drinking, drug abuse and alcohol, sexual activity and hormones, pregnancy, development and endocrinology, mental illness and mood, seizures and neurologic disorders, electrical-related activity and neurophysiology, general activity and locomotion, gastrointestinal, renal and hepatic functions, cardiovascular responses, respiration and thermoregulation, and immunological responses...
February 2017: Peptides
https://www.readbyqxmd.com/read/28010996/pharmacological-characterization-of-rat-vd-hemopressin-%C3%AE-an-%C3%AE-hemoglobin-derived-peptide-exhibiting-cannabinoid-agonist-like-effects-in-mice
#16
Ting Zheng, Ting Zhang, Run Zhang, Zi-Long Wang, Zheng-Lan Han, Ning Li, Xu-Hui Li, Meng-Na Zhang, Biao Xu, Xiong-Li Yang, Quan Fang, Rui Wang
Hemopressin and related peptides have shown to function as the endogenous ligands or the regulator of cannabinoid receptors. Moreover, hemopressin and its truncated peptides were also reported to produce a slight modulatory effect on opioid system. In the present work, based on the amino acid sequence analyses of hemoglobin subunit α, rat VD-hemopressin(α) [(r)VD-Hpα] was predicted as a cannabinoid peptide derived from rat α-hemoglobin. Furthermore, (r)VD-Hpα was synthesized and characterized in a series of in vitro and in vivo assays...
December 16, 2016: Neuropeptides
https://www.readbyqxmd.com/read/27977335/fatty-acid-amide-hydrolase-morphine-interaction-influences-ventilatory-response-to-hypercapnia-and-postoperative-opioid-outcomes-in-children
#17
Vidya Chidambaran, Valentina Pilipenko, Kristie Spruance, Raja Venkatasubramanian, Jing Niu, Tsuyoshi Fukuda, Tomoyuki Mizuno, Kejian Zhang, Kenneth Kaufman, Alexander A Vinks, Lisa J Martin, Senthilkumar Sadhasivam
AIM: Fatty acid amide hydrolase (FAAH) degrades anandamide, an endogenous cannabinoid. We hypothesized that FAAH variants will predict risk of morphine-related adverse outcomes due to opioid-endocannabinoid interactions. PATIENTS & METHODS: In 101 postsurgical adolescents receiving morphine analgesia, we prospectively studied ventilatory response to 5% CO2 (HCVR), respiratory depression (RD) and vomiting. Blood was collected for genotyping and morphine pharmacokinetics...
January 2017: Pharmacogenomics
https://www.readbyqxmd.com/read/27923161/antinociceptive-tolerance-to-nsaids-in-the-rat-formalin-test-is-mediated-by-the-opioid-mechanism
#18
Nana Tsiklauri, Ivliane Nozadze, Gulnaz Gurtskaia, Merab G Tsagareli
BACKGROUND: In the past decade it has been shown that tolerance develops to the antinociceptive effect of repeated systemic administration of commonly used non-steroidal anti-inflammatory drugs (NSAIDs) in acute pain models using rats. This is similar to the tolerance observed with opioid-induced analgesia. In the present study, we investigated the development of tolerance to the analgesic effects of NSAIDs diclofenac, ketorolac and xefocam in a chronic inflammatory pain model, the formalin test...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27898491/psychosocial-factors-predict-opioid-analgesia-through-endogenous-opioid-function
#19
John W Burns, Stephen Bruehl, Christopher R France, Erik Schuster, Daria Orlowska, Asokumar Buvanendran, Melissa Chont, Rajnish K Gupta
Use of opioid analgesics for management of chronic nonmalignant pain has become common, yet there are presently no well-validated predictors of optimal opioid analgesic efficacy. We examined whether psychosocial factors (eg, depressive symptoms) predicted changes in spontaneous low back pain after administration of opioid analgesics, and whether endogenous opioid (EO) function mediated these relationships. Participants with chronic low back pain but who were not chronic opioid users (N = 89) underwent assessment of low back pain intensity pre- and post-drug in 3 (counterbalanced) conditions: (1) placebo, (2) intravenous naloxone, and (3) intravenous morphine...
March 2017: Pain
https://www.readbyqxmd.com/read/27798132/gi-dreadd-expression-in-peripheral-nerves-produces-ligand-dependent-analgesia-as-well-as-ligand-independent-functional-changes-in-sensory-neurons
#20
Jami L Saloman, Nicole N Scheff, Lindsey M Snyder, Sarah E Ross, Brian M Davis, Michael S Gold
Designer receptors exclusively activated by designer drugs (DREADDs) are an advanced experimental tool that could potentially provide a novel approach to pain management. In particular, expression of an inhibitory (Gi-coupled) DREADD in nociceptors might enable ligand-dependent analgesia. To test this possibility, TRPV1-cre mice were used to restrict expression of Gi-DREADDs to predominantly C-fibers. Whereas baseline heat thresholds in both male and female mice expressing Gi-DREADD were normal, 1 mg/kg clozapine-N-oxide (CNO) produced a significant 3 h increase in heat threshold that returned to baseline by 5 h after injection...
October 19, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
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