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https://www.readbyqxmd.com/read/29149605/bias-factor-and-therapeutic-window-correlate-to-predict-safer-opioid-analgesics
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
https://www.readbyqxmd.com/read/29115581/tramadol-attenuates-the-sensitivity-of-glioblastoma-to-temozolomide-through-the-suppression-of-cx43%C3%A2-mediated-gap-junction-intercellular-communication
#17
Lingzhi Wang, Yuexia Peng, Jianxin Peng, Min Shao, Li Ma, Zhuoli Zhu, Guocheng Zhong, Zhengyuan Xia, Huansen Huang
Analgesics and antineoplastic drugs are often used concurrently for cancer patients. Our previous study reported that gap junctions composed of connexin32 (Cx32) was implicated in the effect of analgesics on cisplatin cytotoxicity. However, the effect of analgesic on the most widely expressed connexin (Cx), connexin43 (Cx43), and whether such effect mediates the influence on chemotherapeutic efficiency remain unknown. By manipulation of Cx43 expression or gap junction function, we found that there were gap junction-dependent and independent effect of Cx43 on temozolomide (TMZ) sensitivity in U87 glioblastoma cells...
November 3, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/29115388/antinociceptive-effect-of-valeriana-fauriei-regulates-bdnf-signaling-in-an-animal-model-of-fibromyalgia
#18
Hwayoung Lee, Jiyun Im, Hansol Won, Jun Young Kim, Hyung-Ki Kim, Jun-Tack Kwon, Young Ock Kim, Sanghyun Lee, Ik-Hyun Cho, Sang Won Lee, Hak-Jae Kim
The genus Valeriana has been widely used in popular medicine for centuries, to treat sleep disorders, anxiety, epilepsy and insomnia. Recent studies have focused on the novel pharmacological effects of Valeriana fauriei Briq. (VF) species. Previous studies have attempted to determine the pharmacological functions of Valeriana in various human diseases, particularly with regards to its neuroprotective effects, and its ability to reduce pain and stress. The present study constructed an animal model of fibromyalgia (FM), which was induced by intermittent cold stress with slight modification...
October 20, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29114906/evaluation-of-three-chemical-immobilization-protocols-in-golden-headed-lion-tamarins-leontopithecus-chrysomelas-undergoing-vasectomy-surgery
#19
Mario A Ferraro, Camila V Molina, José L Catão-Dias, Maria C M Kierulff, Alcides Pissinatti, Marina G Bueno, Silvia R G Cortopassi
BACKGROUND: The golden-headed lion tamarin (Leontopithecus chrysomelas), originally endemic to Bahia, was introduced in Rio de Janeiro. The species is currently found in remaining forests within the region of original occupation of the golden lion tamarin (Leontopithecus rosalia), which may compromise the survival of the golden lion tamarin. Groups of golden-headed lion tamarins were captured and translocated to Bahia. However, the area chosen reached its limit and males underwent to vasectomy procedures...
November 8, 2017: Journal of Medical Primatology
https://www.readbyqxmd.com/read/29111112/anti-migraine-effect-of-%C3%A2-9-tetrahydrocannabinol-in-the-female-rat
#20
Ram Kandasamy, Cole T Dawson, Rebecca M Craft, Michael M Morgan
Current anti-migraine treatments have limited efficacy and many side effects. Although anecdotal evidence suggests that marijuana is useful for migraine, this hypothesis has not been tested in a controlled experiment. Thus, the present study tested whether administration of ∆(9)-tetrahydrocannabinol (THC) produces anti-migraine effects in the female rat. Microinjection of the TRPA1 agonist allyl isothiocyanate (AITC) onto the dura mater produced migraine-like pain for 3h as measured by depression of home cage wheel running...
October 28, 2017: European Journal of Pharmacology
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