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Antinociception

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https://www.readbyqxmd.com/read/28935564/antinociception-induced-by-a-novel-%C3%AE-2a-adrenergic-receptor-agonist-in-rodents-acute-and-chronic-pain-models
#1
Roberto Takashi Sudo, Rachel Vieiralves do Amaral, Carlos Eduardo da Silva Monteiro, Ivan da Rocha Pitta, Maria do Carmo Lima, Guilherme Carneiro Montes, Douglas Gordon Ririe, Kenichiro Hayashida, Gisele Zapata-Sudo
The mechanisms and antinociceptive effects of a novel α2A adrenoceptor agonist, 3-(2-chloro-6-fluorobenzil)-imidazolinide-2,4-dione (PT-31) were investigated using animal models of acute and chronic pain. The effects of PT-31 on pain responses were examined using hot plate and formalin tests in mice and spinal nerve ligation (SNL)-induced hyperalgesia in rats. The effects of antagonists acting on α adrenoceptor were assessed to investigate the interaction of these pathways upon PT-31 induced antinociception...
September 18, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28934547/multifunctional-hybrid-compounds-derived-from-2-2-5-dioxopyrrolidin-1-yl-3-methoxypropanamides-with-anticonvulsant-and-antinociceptive-properties
#2
Michał Abram, Mirosław Zagaja, Szczepan Mogilski, Marta Andres-Mach, Gniewomir Latacz, Sebastian Baś, Jarogniew J Łuszczki, Katarzyna Kieć-Kononowicz, Krzysztof Kamiński
The focused set of new pyrrolidine-2,5-diones as potential broad-spectrum hybrid anticonvulsants was described. These derivatives integrate on the common structural scaffold the chemical fragments of well-known antiepileptic drugs such as ethosuximide, levetiracetam, and lacosamide. Such hybrids demonstrated effectiveness in two of the most widely used animal seizure models, namely, the maximal electroshock (MES) test and the psychomotor 6 Hz (32 mA) seizure model. Compound 33 showed the highest anticonvulsant activity in these models (ED50 MES = 79...
September 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28930716/antinociceptive-effect-of-ghrelin-in-a-rat-model-of-irritable-bowel-syndrome-involves-trpv1-opioid-systems
#3
Yuqing Mao, Zhengyang Li, Kan Chen, Huafang Yu, Shaoren Zhang, Miao Jiang, Yuanhua Ma, Chunli Liang, Hongyan Liu, Huanqing Li, Qian Hua, Hao Zhou, Yonghong Sun, Xiaoming Fan
BACKGROUND/AIMS: Irritable bowel syndrome (IBS), defined as recurrent abdominal pain and changes in bowel habits, seriously affects quality of life and ability to work. Ghrelin is a brain-gut hormone, which has been reported to show antinociceptive effects in peripheral pain. We investigated the effect of ghrelin on visceral hypersensitivity and pain in a rat model of IBS. METHODS: Maternal deprivation (MD) was used to provide a stress-induced model of IBS in Wistar rats...
September 20, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28928658/anti-inflammatory-antinociceptive-and-antioxidant-activities-of-methanol-and-aqueous-extracts-of-anacyclus-pyrethrum-roots
#4
Houria Manouze, Otmane Bouchatta, A Chemseddoha Gadhi, Mohammed Bennis, Zahra Sokar, Saadia Ba-M'hamed
Anacyclus pyrethrum (L.) is a plant widely used in Moroccan traditional medicine to treat inflammatory and painful diseases. The objective of the present study was to evaluate the antinociceptive, anti-inflammatory and antioxidant activities of aqueous and methanol extracts of Anacyclus pyrethrum roots (AEAPR and MEAPR). The anti-inflammatory effect of AEAPR and MEAPR was determined in xylene-induced ear edema and Complete Freund's Adjuvant (CFA)-induced paw edema. The antinociceptive activity of AEAPR and MEAPR (125, 250, and 500 mg/kg) administered by gavage was examined in mice by using acetic acid-induced writhing, hot plate, and formalin tests, and the mechanical allodynia were assessed in CFA-induced paw edema...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28928655/effects-of-simvastatin-beyond-dyslipidemia-exploring-its-antinociceptive-action-in-an-animal-model-of-complex-regional-pain-syndrome-type-i
#5
Graziela Vieira, Juliana Cavalli, Elaine C D Gonçalves, Tainara R Gonçalves, Larissa R Laurindo, Maíra Cola, Rafael C Dutra
Simvastatin is a lipid-lowering agent that blocks the production of cholesterol through inhibition of 3-hydroxy-methyl-glutaryl coenzyme A (HMG-CoA) reductase. In addition, recent evidence has suggested its anti-inflammatory and antinociceptive actions during inflammatory and pain disorders. Herein, we investigated the effects of simvastatin in an animal model of complex regional pain syndrome-type I, and its underlying mechanisms. Chronic post-ischemia pain (CPIP) was induced by ischemia and reperfusion (IR) injury of the left hind paw...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28924009/site-specific-regulation-of-p2x7-receptor-function-in-microglia-gates-morphine-analgesic-tolerance
#6
Heather Leduc-Pessah, Nicholas L Weilinger, Churmy Y Fan, Nicole E Burma, Roger J Thompson, Tuan Trang
Tolerance to the analgesic effects of opioids is a major problem in chronic pain management. Microglia are implicated in opioid tolerance, but the core mechanisms regulating their response to opioids remain obscure. By selectively ablating microglia in the spinal cord using a saporin-conjugated antibody to Mac1, we demonstrate a causal role for microglia in the development, but not maintenance, of morphine tolerance in male rats. Increased P2X7 receptor (P2X7R) activity is a cardinal feature of microglial activation, and in this study we found that morphine potentiates P2X7R-mediated Ca(2+) responses in resident spinal microglia acutely isolated from morphine tolerant rats...
September 18, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28921601/is-2-hydroxypropyl-%C3%AE-cyclodextrin-a-suitable-carrier-for-central-administration-of-%C3%AE-9-tetrahydrocannabinol-preclinical-evidence
#7
R Agabio, F Sanna, C Lobina, M Monduzzi, V Nairi, F Cugia, S Mameli, G M Pisanu, G L Gessa, M R Melis
Preclinical Research Δ(9) -Tetrahydrocannabinol (THC) is a hydrophobic compound that has a potent antinociceptive effect in animals after intrathecal (IT) or intracerebroventricular (ICV) administration. The lack of a suitable solvent precludes its IT administration in humans. 2-Hydroxypropyl-β-cyclodextrin (HPβCD) increases the water solubility of hydrophobic drugs and is approved for IT administration in humans. To investigate whether HPβCD might be a suitable carrier for ICV administration of THC in rats, two formulations containing THC complexed with HPβCD (30 and 135 μg of THC per animal) and vehicle were administered to Wistar rats...
September 18, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28915966/use-of-anthropogenic-nitrogen-fertilizers-in-agriculture-is-associated-with-per-capita-ethanol-consumption
#8
Keith Fluegge, Kyle Fluegge
It has previously been demonstrated that emissions of the agricultural pollutant, nitrous oxide (N2O), may be a confounder to the relationship between herbicide use and psychiatric impairments, including ADHD. This report attempts to extend this hypothesis by testing whether annual use of anthropogenic nitrogen-based fertilizers in U.S. agriculture (thought to be the most reliable indicator of environmental N2O emissions) is associated with per capita ethanol consumption patterns, a behavior often comorbid with ADHD...
September 2017: Medical Hypotheses
https://www.readbyqxmd.com/read/28914627/antinociceptive-effects-of-jwh015-in-female-and-male-rats
#9
Rebecca M Craft, Nicholas Z Greene, Alexa A Wakley
Despite greater chronic pain prevalence in females compared with males, and the analgesic potential of cannabinoid receptor type 2 (CB2) agonists, CB2 agonists have rarely been tested in females. The aim of the present study was to compare the antinociceptive effects of a CB2-preferring agonist, (2-methyl-1-propyl-1H-indol-3-yl)-1-naphthalenylmethanone (JWH015), in female and male rats against acute pain and persistent inflammatory pain. JWH015 (5-20 mg/kg, intraperitoneally) produced dose-dependent and time-dependent increases in latency to respond on the tail withdrawal and paw pressure tests that did not differ statistically between the sexes...
September 13, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28903179/antinociceptive-anti-inflammatory-and-anxiolytic-like-effects-of-the-ethanolic-extract-fractions-and-hibalactone-isolated-from-hydrocotyle-umbellata-l-acari%C3%A3-oba-araliaceae
#10
Thiago Levi Silva Oliveira, Sandra Ribeiro de Morais, Stone de Sá, Matheus Gabriel de Oliveira, Iziara Ferreira Florentino, Dayane Moreira da Silva, Verônica Vale Carvalho, Vinícius Barreto da Silva, Boniek Gontijo Vaz, José Ricardo Sabino, Elson Alves Costa, José Realino de Paula
Hydrocotyle umbellata Linn. (Araliaceae) is specie used in the treatment of inflammatory diseases. Crude extract (E-HU) was prepared from H. umbellata subterraneous parts and fractionated by liquid-liquid partition, resulting hexane fraction (HF-HU), dichloromethane fraction (DF-HU), ethyl acetate fraction (EAF-HU) and aqueous fraction (AF-HU). The hibalactone (HU-1) was isolated from the DF-HU and its structure was elucidated by (1)H NMR and (13)C NMR Spectroscopy, mass spectrometry and crystallographic x-ray analysis...
September 9, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28902707/impact-of-human-ca8-on-thermal-antinociception-in-relation-to-morphine-equivalence-in-mice
#11
Eugene S Fu, Diana M Erasso, Gerald Z Zhuang, Udita Upadhyay, Mehtap Ozdemir, Timothy Wiltshire, Konstantinos D Sarantopoulos, Shad B Smith, William Maixner, Eden R Martin, Roy C Levitt
Recently, we showed that murine dorsal root ganglion (DRG) Car8 expression is a cis-regulated eQTL that determines analgesic responses. In this report, we show that transduction through sciatic nerve injection of DRG with human wild-type carbonic anhydrase-8 using adeno-associated virus viral particles (AAV8-V5-CA8WT) produces analgesia in naive male C57BL/6J mice and antihyperalgesia after carrageenan treatment. A peak mean increase of about 4 s in thermal hindpaw withdrawal latency equaled increases in thermal withdrawal latency produced by 10 mg/kg intraperitoneal morphine in these mice...
September 11, 2017: Neuroreport
https://www.readbyqxmd.com/read/28902684/estrogens-synthesized-and-acting-within-a-spinal-oligomer-suppress-spinal-endomorphin-2-antinociception-ebb-and-flow-over-the-rat-reproductive-cycle
#12
Nai-Jiang Liu, Vijaya Murugaiyan, Emiliya M Storman, Stephen A Schnell, Martin W Wessendorf, Alan R Gintzler
The magnitude of antinociception elicited by intrathecal endomorphin 2 (EM2), an endogenous mu-opioid receptor (MOR) ligand, varies across the rat estrous cycle. We now report that phasic changes in analgesic responsiveness to spinal EM2 result from plastic interactions within a novel membrane-bound oligomer containing estrogen receptors (mERs), aromatase (aka estrogen synthase), metabotropic glutamate receptor 1 (mGluR1), and MOR. During diestrus, spinal mERs, activated by locally synthesized estrogens, act with mGluR1 to suppress spinal EM2/MOR antinociception...
June 21, 2017: Pain
https://www.readbyqxmd.com/read/28902622/functional-interaction-between-n-methyl-d-aspartate-receptor-and-ascorbic-acid-during-neuropathic-pain-induced-by-chronic-constriction-injury-of-the-sciatic-nerve
#13
Sepideh Saffarpour, Farinaz Nasirinezhad
BACKGROUND: Neuropathic pain is a chronic pain condition, which is resistant to therapy. Ascorbate was released because of the activation of glutaminergic neurons. Due to the important role of N-methyl-D-aspartate (NMDA) receptors in the pathophysiology of neuropathic pain, this study investigated the analgesic efficacy of ascorbic acid (AA) in neuropathic pain condition and the role of NMDA receptors in this effect. METHODS: For this purpose, adult male rats were randomly allocated to experimental groups (n=8 in each group)...
September 13, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/28901776/liposomal-delivery-of-diacylglycerol-lipase-beta-inhibitors-to-macrophages-dramatically-enhances-selectivity-and-efficacy-in-vivo
#14
Myungsun Shin, Helena W Snyder, Giulia Donvito, Lesley D Schurman, Todd E Fox, Aron H Lichtman, Mark Kester, Ku-Lung Hsu
Diacylglycerol lipase-beta (DAGLβ) hydrolyzes arachidonic acid (AA)-containing diacylglycerols to produce bioactive lipids including endocannabinoids and AA-derived eicosanoids involved in regulation of inflammatory signaling. Previously, we demonstrated that DAGLβ inactivation using the triazole urea inhibitor KT109 blocked macrophage inflammatory signaling and reversed allodynic responses of mice in inflammatory and neuropathic pain models. Here, we tested whether we could exploit the phagocytic capacity of macrophages to localize delivery of DAGLβ inhibitors to these cells in vivo using liposome encapsulated KT109...
September 13, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28901555/dyspnea-catastrophizing-and-neural-activations-during-the-anticipation-and-perception-of-dyspnea
#15
M Cornelia Stoeckel, Roland W Esser, Matthias Gamer, Christian Büchel, Andreas von Leupoldt
Dyspnea is an aversive symptom in various diseases. High levels of negative affectivity are typically associated with increased dyspnea and changes in its neural processing. Recently, more dyspnea-specific forms of negative affectivity such as dyspnea catastrophizing were suggested to contribute to increased perception of dyspnea beyond effects of rather unspecific negative affectivity such as general anxiety levels. The involved neural mechanisms have not yet been explored. Therefore, the present retrospective analysis examined the associations of dyspnea catastrophizing with neural activations during the anticipation and perception of dyspnea...
September 13, 2017: Psychophysiology
https://www.readbyqxmd.com/read/28901432/effects-of-coadministration-of-low-dose-cannabinoid-type-2-receptor-agonist-and-morphine-on-vanilloid-receptor-1-expression-in-a-rat-model-of-cancer-pain
#16
Mingyue Zhang, Meng Chi, Huichao Zou, Songyu Tian, Zhaodi Zhang, Guonian Wang
Morphine is widely used as an analgesic to treat moderate to severe pain, but chronic morphine use is associated with development of tolerance and dependence, which limits its analgesic efficacy. Our previous research has showed that nonanalgetic dose of a cannabinoid type 2 (CB2) receptor agonist reduced morphine tolerance in cancer pain. A previous study showed the colocalization of CB2 and transient receptor potential vanilloid 1 (TRPV1) in human and rat dorsal root ganglia (DRG) sensory neurons. Whether coadministration of a CB2 receptor agonist and morphine could reduce TRPV1 expression in morphine‑induced antinociception and tolerance in cancer pain is unclear...
September 13, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28899779/eupatilin-with-ppar%C3%AE-agonistic-effects-inhibits-tnf%C3%AE-induced-mmp-signaling-in-hacat-cells
#17
Yujung Jung, Jin-Chul Kim, Yongsoo Choi, Sullim Lee, Ki Sung Kang, Yong Kee Kim, Su-Nam Kim
Eupatilin (5,7-dihydroxy-3,4,6-trimethoxyflavone) is a flavonoid compound exhibiting several beneficial biological activities, including neuroprotection, anti-cancer, antinociception, chondroprotection, anti-oxidation, and anti-inflammation. Our previous study demonstrated that eupatilin specifically activates peroxisome proliferator-activated receptor alpha (PPARα) through direct binding. The PPAR subfamily includes ligand-dependent transcription factors that consist of three isotypes: PPARα, PPARβ/δ, and PPARγ...
September 9, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28895719/radical-s-adenosylmethionine-enzymes-involved-in-ripp-biosynthesis
#18
Nilkamal Mahanta, Graham A Hudson, Douglas A Mitchell
Ribosomally synthesized and post-translationally modified peptides (RiPPs) display a diverse range of structures and continue to expand as a natural product class. Accordingly, RiPPs exhibit a wide array of bioactivities, acting as broad and narrow spectrum growth suppressors, antidiabetics, and antinociception and anticancer agents. Because of these properties, and the complex repertoire of post-translational modifications (PTMs) that give rise to these molecules, RiPP biosynthesis has been intensely studied...
September 22, 2017: Biochemistry
https://www.readbyqxmd.com/read/28894363/ketoprofen-loaded-polymer-carriers-in-bigel-formulation-an-approach-to-enhancing-drug-photostability-in-topical-application-forms
#19
Velichka Andonova, Petya Peneva, George S Georgiev, Vencislava T Toncheva, Elisaveta Apostolova, Zhivko Peychev, Stela Dimitrova, Mariana Katsarova, Nadia Petrova, Margarita Kassarova
The purpose of the study was to investigate the stability and biopharmaceutical characteristics of ketoprofen, loaded in polymeric carriers, which were included into a bigel in a semisolid dosage form. The polymer carriers with in situ-included ketoprofen were obtained by emulsifier-free emulsion polymerization of the monomers in aqueous medium or a solution of the polymers used. The morphological characteristics of the carriers, the in vitro release and the photochemical stability of ketoprofen were evaluated...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28893589/leptin-status-alters-buprenorphine-induced-antinociception-in-obese-mice-with-dysfunctional-leptin-receptors
#20
Zachary Glovak, Sara Mihalko, Helen A Baghdoyan, Ralph Lydic
Buprenorphine is an opiate used for pain management and to treat opiate addiction. The cytokine leptin can modulate nociception, but the extent to which buprenorphine-induced antinociception varies as a function of leptin signaling has not been characterized. Four congenic mouse lines with phenotypes that include differences in body weight and leptin status were used to test the hypothesis that the antinociceptive effects of buprenorphine vary as function of sex and leptin signaling. Each mouse line was comprised of males (n=12) and females (n=12) for a total of 96 animals...
September 8, 2017: Neuroscience Letters
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