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https://www.readbyqxmd.com/read/29160600/current-evidence-of-cannabinoid-based-analgesia-obtained-in-preclinical-and-human-experimental-settings
#1
REVIEW
J Lötsch, I Weyer-Menkhoff, I Tegeder
Cannabinoids have a long record of recreational and medical use and become increasingly approved for pain therapy. This development is based on preclinical and human experimental research summarized in this review. Cannabinoid CB1 receptors are widely expressed throughout the nociceptive system. Their activation by endogenous or exogenous cannabinoids modulates the release of neurotransmitters. This is reflected in antinociceptive effects of cannabinoids in preclinical models of inflammatory, cancer and neuropathic pain, and by nociceptive hypersensitivity of cannabinoid receptor-deficient mice...
November 21, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/29159717/analgesic-anti-inflammatory-and-anticancer-activities-of-combretin-a-and-combretin-b-isolated-from-combretum-fragrans-f-hoffm-combretaceae-leaves
#2
Marius Mbiantcha, Jabeen Almas, Amadou Dawe, Aisha Faheem, Zafar Sidra
Previous pharmacological and phytochemical studies showed that, Combretum fragrans F. HOFFM (Combretaceae) is a Cameroonian medicinal plant possessing numerous therapeutic virtues and rich in various active secondary metabolites. In this study, we investigate in vivo anti-nociceptive and anti-inflammatory activity and, in vitro anticancer, anti-TNFα, ROS and NO-inhibitory activities of Combretum A and Combretin B, two triterpenes cycloartane-type isolated from the leaves of Combretum fragrans. The effect on ROS, TNF-α and NO production, anticancer activity and cytotoxicity assay were done using chemiluminescence technique, ELISA kit, colorimetric method, MCF-7 cells and MTT assay, respectively...
November 20, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/29156533/serotonin-induces-peripheral-antinociception-via-the-opioidergic-system
#3
Danielle Aguiar Diniz, Júlia Alvarenga Petrocchi, Larissa Caldeira Navarro, Tâmara Cristina Souza, Marina Gomes Miranda E Castor, Igor Dimitri Gama Duarte, Thiago Roberto Lima Romero
PURPOSE: Studies conducted since 1969 have shown that the release of serotonin (5-HT) in the dorsal horn of the spinal cord contributes to opioid analgesia. In the present study, the participation of the opioidergic system in antinociceptive effect serotonin at the peripheral level was examined. METHODS: The paw pressure test was used with mice (Swiss, males from 35 g) which had increased pain sensitivity by intraplantar injection of PGE2 (2 μg). Serotonin (250 ng), administered locally to the right paw of animals, produces antinociception in this model...
November 15, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29155084/anti-inflammatory-antinociceptive-and-antioxidant-properties-of-schinopsis-brasiliensis-bark
#4
Clisiane Carla de Souza Santos, Carolina Carvalho Guilhon, Daniela Sales Alviano Moreno, Celuta Sales Alviano, Charles Dos Santos Estevam, Arie Fitzgerald Brank, Patricia Dias Fernandes
ETHNOPHARMACOLOGICAL RELEVANCE: Schinopsis brasiliensis is a native plant from Brazil, popularly used in folk medicine to relieve pain and treat inflammation. This study evaluated the antinociceptive and anti-inflammatory activities and antioxidant properties of the hydroethanol extract (HEE) and ethyl acetate fraction (EAF) obtained from S. brasiliensis bark. MATERIALS AND METHODS: The HEE and EAF of S. brasiliensis bark (10, 30 and 100mg/kg, p.o.) were evaluated using models of analgaesia (formalin-induced licking and hot -plate models) or inflammation (licking response by formalin-induced and carrageenan-induced cell migration into the subcutaneous air pouch)...
November 15, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29149605/bias-factor-and-therapeutic-window-correlate-to-predict-safer-opioid-analgesics
#5
Cullen L Schmid, Nicole M Kennedy, Nicolette C Ross, Kimberly M Lovell, Zhizhou Yue, Jenny Morgenweck, Michael D Cameron, Thomas D Bannister, Laura M Bohn
Biased agonism has been proposed as a means to separate desirable and adverse drug responses downstream of G protein-coupled receptor (GPCR) targets. Herein, we describe structural features of a series of mu-opioid-receptor (MOR)-selective agonists that preferentially activate receptors to couple to G proteins or to recruit βarrestin proteins. By comparing relative bias for MOR-mediated signaling in each pathway, we demonstrate a strong correlation between the respiratory suppression/antinociception therapeutic window in a series of compounds spanning a wide range of signaling bias...
November 16, 2017: Cell
https://www.readbyqxmd.com/read/29149031/anti-inflammatory-and-antinociceptive-effects-of-ethyl-acetate-fraction-of-an-edible-red-macroalgae-sarcodia-ceylanica
#6
Chieh-Chih Shih, Hwong-Ru Hwang, Chi-I Chang, Huei-Meei Su, Pei-Chin Chen, Hsiao-Mei Kuo, Pei-Jyuan Li, Hui-Min David Wang, Kuan-Hao Tsui, Yu-Chi Lin, Shi-Ying Huang, Zhi-Hong Wen
Research so far has only shown that edible red macroalgae, Sarcodia ceylanica has the ability to eliminate free radicals and anti-diabetic, anti-bacterial properties. This study was conducted both in vitro and in vivo on the ethyl acetate extract (PD1) of farmed red macroalgae in order to explore its anti-inflammatory properties. In order to study the in vitro anti-inflammatory effects of PD1, we used lipopolysaccharide (LPS) to induce inflammatory responses in murine macrophages. For evaluating the potential in vivo anti-inflammatory and antinociceptive effects of PD1, we used carrageenan-induced rat paw edema to produce inflammatory pain...
November 17, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29146238/ccr5-mediates-hiv-1-tat-induced-neuroinflammation-and-influences-morphine-tolerance-dependence-and-reward
#7
Maciej Gonek, Virginia D McLane, David L Stevens, Kumiko Lippold, Hamid I Akbarali, Pamela E Knapp, William L Dewey, Kurt F Hauser, Jason J Paris
The HIV-1 regulatory protein, trans-activator of transcription (Tat), interacts with opioids to potentiate neuroinflammation and neurodegeneration within the CNS. These effects may involve the C-C chemokine receptor type 5 (CCR5); however, the behavioral contribution of CCR5 on Tat/opioid interactions is not known. Using a transgenic murine model that expresses HIV-1 Tat protein in a GFAP-regulated, doxycycline-inducible manner, we assessed morphine tolerance, dependence, and reward. To assess the influence of CCR5 on these effects, mice were pretreated with oral vehicle or the CCR5 antagonist, maraviroc, prior to morphine administration...
November 13, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/29145067/role-of-thalamic-ventral-posterolateral-nucleus-histamine-h2-and-opiate-receptors-in-modulation-of-formalin-induced-muscle-pain-in-rats
#8
Hamid Ghasemi, Esmaeal Tamaddonfard, Farhad Soltanalinejad
BACKGROUND: Histamine and opiate systems contribute to supraspinal processing of pain. In the present study, we investigated the effects of microinjection of histamine and agonists and antagonists of histamine H2 and opiate receptors into the thalamic ventral posterolateral nucleus on muscle pain in rats. METHODS: The thalamic ventral posterolateral nuclei were bilaterally implanted with two guide cannulas. Muscle pain was induced by intramuscular injection of a diluted formalin solution (2...
May 8, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29143802/the-inhibitory-effects-of-cobalt-protoporphyrin-ix-and-cannabinoid-2-receptor-agonists-in-type-2-diabetic-mice
#9
Christina McDonnell, Sergi Leánez, Olga Pol
The activation of the transcription factor Nrf2 inhibits neuropathy and modulates the activity of delta-opioid receptors (DOR) in type 2 diabetic mice but the impact of Nrf2/HO-1 pathway on the antinociceptive actions of cannabinoid 2 receptors (CB2R) has not been assessed. Using male mice BKS.Cg-m+/+Leprdb/J (db/db) we investigated if treatment with cobalt protoporphyrin IX (CoPP), an HO-1 inductor, inhibited mechanical allodynia, hyperglycemia and obesity associated to type 2 diabetes. The antinociceptive effects of JWH-015 and JWH-133 (CB2R agonists) administered with and without CoPP or sulforaphane (SFN), a Nrf2 transcription factor activator, have been also evaluated...
October 28, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29143334/pk-pd-modeling-of-flunixin-meglumine-in-a-kaolin-induced-inflammation-model-in-piglets
#10
O L Levionnois, T K Fosse, B Ranheim
Flunixin is marketed in several countries for analgesia in adult swine but little is known about its efficacy in piglets. Thirty-two piglets (6-8 days old) were randomized to receive placebo saline (n = 11, group CONTROL) or flunixin meglumine intravenously at 2.2 (n = 11, group MEDIUM) or 4.4 (n = 10, group HIGH) mg/kg, 10 hr after subcutaneous injection of kaolin in the left metacarpal area. A hand-held algometer was used to determine each piglet's mechanical nociceptive threshold (MNT) from both front feet up to 50 hr after treatment (cut-off value of 24...
November 16, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29142391/acacia-catechu-ethanolic-seed-extract-triggers-apoptosis-of-scc-25-cells
#11
Thangavelu Lakshmi, Devaraj Ezhilarasan, Upendra Nagaich, Rajagopal Vijayaragavan
Background: Acacia catechu Willd (Fabaceae), commonly known as catechu, cachou, and black cutch, has been studied for its hepatoprotective, antipyretic, antidiarrheal, hypoglycemic, anti-inflammatory, immunomodulatory, antinociceptive, antimicrobial, free radical scavenging, and antioxidant activities. Objective: We evaluated the cytotoxic activity of ethanol extract of A. catechu seed (ACS) against SCC-25 human oral squamous carcinoma cell line. Methods: Cytotoxic effect of ACS extract was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, using concentrations of 0...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29141251/opioid-receptors-contribute-to-antinociceptive-effect-of-tianeptine-on-colorectal-distension-induced-visceral-pain-in-rats
#12
S Sırrı Bilge, Fatih İlkaya, Özge Darakcı, Engin Çiftcioğlu, Ayhan Bozkurt
Tianeptine is a clinically effective atypical antidepressant with distinct neurochemical properties. In this study, we aimed to investigate the contribution of opioid receptors in the antinociceptive effect of tianeptine on visceral pain in awake rats and to differentiate the subtype and the localization (central and/or peripheral) of these opioid receptors involved in this antinociception. Visceromotor response to noxious colorectal distension (CRD) was quantified with electromyographic recordings, obtained from previously implanted electrodes into the external oblique musculature of rats under anesthesia, before and after tianeptine administration...
November 15, 2017: Pharmacology
https://www.readbyqxmd.com/read/29138109/mesopontine-neurons-implicated-in-anesthetic-loss-of-consciousness-have-either-ascending-or-descending-axonal-projections-but-not-both
#13
Adi Miriam Goldenberg, Anne Minert, Yelena Fishman, Gilly Wolf, Marshall Devor
The MPTA (mesopontine tegmental anesthesia area) is a key node in a network of axonal pathways that collectively engage the key components of general anesthesia: immobility and atonia, analgesia, amnesia and loss-of-consciousness. In this study we have applied double retrograde tracing to analyze MPTA connectivity, with a focus on axon collateralization. Prior tracer studies have shown that collectively, MPTA neurons send descending projections to spinal and medullary brain targets associated with atonia and analgesia as well as ascending projections to forebrain structures associated with amnesia and arousal...
November 11, 2017: Neuroscience
https://www.readbyqxmd.com/read/29136953/antidiarrheal-effects-of-water-soluble-proteins-from-plumeria-pudica-latex-in-mice
#14
Lucas de Araújo Bastos Santana, Diego Passos Aragão, Thiago de Souza Lopes Araújo, Nayara Alves de Sousa, Luan Kelves Miranda de Souza, Lucas Eduardo Silva Oliveira, Anna Carolina Toledo da Cunha Pereira, Gustavo Portela Ferreira, Naylla Veras de Moraes Oliveira, Bruna da Silva Souza, Francisca Beatriz Melo Sousa, Márcio Viana Ramos, Cleverson Diniz Teixeira de Freitas, Jand-Venes Rolim Medeiros, Jefferson Soares de Oliveira
The water-soluble protein fraction obtained from Plumeria pudica (LPPp) latex has previously been demonstrated to have anti-inflammatory and antinociceptive effects. In the present study, LPPp was tested for activity against diarrhea induced by castor oil, prostaglandin E2 (PGE2) or cholera toxin. Different doses of LPPp (10, 20 or 40mg/kg) significantly inhibited the percentage of diarrheal stools (31.18%, 42.97% and 59.70%, respectively) induced by castor oil. This event was followed by significant reduction of both intestinal fluid accumulation (31...
November 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29136763/amorphous-solid-dispersions-of-hecogenin-acetate-using-different-polymers-for-enhancement-of-solubility-and-improvement-of-anti-hyperalgesic-effect-in-neuropathic-pain-model-in-mice
#15
Carlos Demócedes Luís de França Almeida Moreira, Jonas Gabriel de Oliveira Pinheiro, Walter Ferreira da Silva-Júnior, Euzébio Guimarães Barbosa, Zênia Maria Maciel Lavra, Erick Willyame Menezes Pereira, Marília Matos Resende, Eduardo Pereira de Azevedo, Lucindo José Quintans-Júnior, Adriano Antunes de Souza Araújo, Jullyana de Souza Siqueira Quintans, Ádley Antonini Neves de Lima
Hecogenin acetate (HA) is an acetylated sapogenin that has shown potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors. However, HA exhibits poor aqueous solubility, which may limit its application. This study aims to develop amorphous solid dispersions (ASD) using five hydrophilic polymers, to characterize them and to evaluate their antihyperalgesic activity. Physicochemical characterization was performed by X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and Fourier Transformed Infrared (FTIR) spectroscopy...
November 6, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29134730/role-of-central-versus-peripheral-opioid-system-in-antinociceptive-and-anti-inflammatory-effect-of-botulinum-toxin-type-a-in-trigeminal-region
#16
V Drinovac Vlah, B Filipović, L Bach-Rojecky, Z Lacković
BACKGROUND: Although botulinum toxin type A (BT-A) is approved for chronic migraine treatment, its site and mechanism of action are still elusive. Recently our group discovered that suppression of CGRP release from dural nerve endings might account for antimigraine action of pericranially injected BT-A. We demonstrated that central antinociceptive effect of BT-A in sciatic region involves endogenous opioid system as well. Here we investigated possible interaction of BT-A with endogenous opioid system within the trigeminal region...
November 13, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/29132133/endomorphins-promising-endogenous-opioid-peptides-for-the-development-of-novel-analgesics
#17
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/29130348/tryptophan-containing-non-cationizable-opioid-peptides-a-new-chemotype-with-unusual-structure-and-in-vivo-activity
#18
Rossella De Marco, Luca Gentilucci
Recently, a new family of opioid peptides containing tryptophan came to the spotlight for the absence of the fundamental protonable tyramine 'message' pharmacophore. Structure-activity relationship investigations led to diverse compounds, characterized by different selectivity profiles and agonist or antagonist effects. Substitution at the indole of Trp clearly impacted peripheral/central antinociceptivity. These peculiarities prompted to gather all the compounds in a new class, and to coin the definition 'Tryptophan-Containing Non-Cationizable Opioid Peptides', in short 'TryCoNCOPs'...
November 13, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29130346/chemical-composition-and-evaluation-of-antinociceptive-activity-of-the-essential-oil-of-stevia-serrata-cav-from-guatemala
#19
Daniel Luiz Reis Simas, Max Samuel Mérida-Reyes, Manuel Alejandro Muñoz-Wug, Millena Santos Cordeiro, Thais Biondino Sardella Giorno, Edwin Adolfo Taracena, Bessie Evelyn Oliva-Hernández, José Vicente Martínez-Arévalo, Patricia Dias Fernandes, Juan Francisco Pérez-Sabino, Antonio Jorge Ribeiro da Silva
The composition and the antinociceptive activity of the essential oil of Stevia serrata Cav. from a population located in the west highlands of Guatemala were evaluated. A yield of 0.2% (w/w) of essential oil was obtained by hydrodistillation of the dried aerial parts of the plant. The essential oil analysed by GC-FID and GC-MS showed a high content of sesquiterpenoids, with chamazulene (60.1%) as the major component and 91.5% of the essential oil composition was identified. To evaluate antinociceptive activity in mice, the essential oil of S...
November 13, 2017: Natural Product Research
https://www.readbyqxmd.com/read/29127424/involvement-of-galanin-and-galanin-receptor-1-in-nociceptive-modulation-in-the-central-nucleus-of-amygdala-in-normal-and-neuropathic-rats
#20
Shi-Yang Li, Mei-Ling Huo, Xu-Yang Wu, Yu-Qing Huang, Lei Wang, Xin Zhang, Yan-Mei Jiang, Meng-Lin Zhang, Lin-Lin Wang, Long-Chuan Yu
The present study was performed to explore the role of galanin and galanin receptor 1 (GalR 1) in nociceptive modulation in the central nucleus of amygdala (CeA) in normal rats and rats with neuropathy, and the involvement of GalR 1 and PKC was also investigated. The hindpaw withdrawal latencies (HWLs) to thermal and mechanical stimulations were increased in a dose-dependent manner after intra-CeA injection of galanin in both normal rats and rats with neuropathy. The increased HWLs were significantly attenuated by intra-CeA injection of galanin receptor antagonist M40, indicating an involvement of galanin receptor in nociceptive modulation in CeA...
November 10, 2017: Scientific Reports
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