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https://www.readbyqxmd.com/read/28549861/the-ethanol-extract-of-leonurus-sibiricus-l-induces-antioxidant-antinociceptive-and-topical-anti-inflammatory-effects
#1
Alan Santos Oliveira, Luana Mendonça Cercato, Marília Trindade de Santana Souza, Allan John de Oliveira Melo, Bruno Dos Santos Lima, Marcelo Cavalcante Duarte, Adriano Antunes de Souza Araujo, Ana Mara de Oliveira E Silva, Enilton Aparecido Camargo
ETHNOPHARMACOLOGICAL RELEVANCE: Leonurus sibiricus L. (Lamiaceae), popularly known as motherwort, or "erva-de-macaé" or "rubim" in Brazil, is a plant used for the treatment of inflammatory conditions, but few studies have evaluated this anti-inflammatory activity or other activities that may be relevant. AIM OF THE STUDY: This study was undertaken to investigate the antioxidant, antinociceptive and topical anti-inflammatory effects of the ethanol extract of L. sibiricus (EELs)...
May 23, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28547246/indications-for-opioid-antagonists
#2
REVIEW
O J Michael Coppes, Christine N Sang
PURPOSE OF REVIEW: As opioids have become more common in clinical practice for the treatment of both acute and chronic pain, so too has the need for a deeper understanding of the clinical applications of opioid antagonists. The purpose of this review is to present both the longstanding and potential new indications for the use of drugs that block the effects of opioid receptors. RECENT FINDINGS: There is a growing body of data demonstrating the modulation of pain by opioid antagonists...
June 2017: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/28547032/car8-dorsal-root-ganglion-expression-and-genetic-regulation-of-analgesic-responses-are-associated-with-a-cis-eqtl-in-mice
#3
Roy C Levitt, Gerald Y Zhuang, Yuan Kang, Diana M Erasso, Udita Upadhyay, Mehtap Ozdemir, Eugene S Fu, Konstantinos D Sarantopoulos, Shad B Smith, William Maixner, Luda Diatchenko, Eden R Martin, Tim Wiltshire
Carbonic anhydrase-8 (Car8 mouse gene symbol) is devoid of enzymatic activity, but instead functions as an allosteric inhibitor of inositol trisphosphate receptor-1 (ITPR1) to regulate this intracellular calcium release channel important in synaptic functions and neuronal excitability. Causative mutations in ITPR1 and carbonic anhydrase-8 in mice and humans are associated with certain subtypes of spinal cerebellar ataxia (SCA). SCA mice are genetically deficient in dorsal root ganglia (DRG) Car8 expression and display mechanical and thermal hypersensitivity and susceptibility to subacute and chronic inflammatory pain behaviors...
May 25, 2017: Mammalian Genome: Official Journal of the International Mammalian Genome Society
https://www.readbyqxmd.com/read/28543930/further-analysis-of-acute-antinociceptive-and-anti-inflammatory-actions-of-4-phenylselenyl-7-chloroquinoline-in-mice
#4
Vanessa D G Silva, Angélica S Reis, Mikaela Pinz, Caren A R da Fonseca, Luis Fernando B Duarte, Juliano A Roehrs, Diego Alves, Cristiane Luchese, Ethel A Wilhelm
A new quinoline containing selenium, 4-phenylselenyl-7-chloroquinoline (4-PSQ), was described and synthetized by our research group. Recently, we demonstrated the potential antinociceptive and anti-inflammatory of 4-PSQ. For this reason, the first objective of this study was to expand our previous findings by investigating the contribution of glutamatergic, serotonergic and nitrergic systems to the acute antinociceptive action of this compound. Pretreatment with 4-PSQ (0.01-25 mg/kg, p.o.) reduced the nociception induced by glutamate...
May 23, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28538816/antioxidant-effect-of-quinoline-derivatives-containing-or-not-selenium-relationship-with-antinociceptive-action-quinolines-are-antioxidant-and-antinociceptive
#5
Ethel A Wilhelm, Ana Teresinha Ferreira, Mikaela P Pinz, Angélica S Dos Reis, Ane G Vogt, Andre L Stein, Gilson Zeni, Cristiane Luchese
The present study investigated the antioxidant effect of a new class of quinoline derivatives (a-d) on assays in vitro. Lipid peroxidation, thiol peroxidase-like and free radical scavenging activities were determined to evaluate antioxidant activity of compounds. Thiol oxidase-like and δ-aminolevulinate dehydratase activities were performed as a toxicological parameter. A second objective of this study was to evaluate the in vivo antinociceptive effect of the compound with better antioxidant effect and without toxic effects in a model of nociception induced by formalin in mice...
May 22, 2017: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/28535789/a-multi-target-therapeutic-potential-of-prunus-domestica-gum-stabilized-nanoparticles-exhibited-prospective-anticancer-antibacterial-urease-inhibition-anti-inflammatory-and-analgesic-properties
#6
Nazar Ul Islam, Raza Amin, Muhammad Shahid, Muhammad Amin, Sumera Zaib, Jamshed Iqbal
BACKGROUND: Phytotherapeutics exhibit diverse pharmacological effects that are based on the combined action of a mixture of phytoconstituents. In this study, Prunus domestica gum-loaded, stabilized gold and silver nanoparticles (Au/Ag-NPs) were evaluated for their prospective anticancer, antibacterial, urease-inhibition, anti-inflammatory, and analgesic properties. METHODS: Au/Ag-NPs were biosynthesized and characterized with UV-Vis, FTIR, SEM, EDX, and XRD techniques...
May 23, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28524250/one-plant-many-uses-a-review-of-the-pharmacological-applications-of-morinda-citrifolia
#7
REVIEW
Mylena Andréa Oliveira Torres, Isadora de Fátima Braga Magalhães, Renata Mondêgo-Oliveira, Joicy Cortez de Sá, Alessandra Lima Rocha, Ana Lucia Abreu-Silva
Morinda citrifolia, also known as noni, is commonly used in popular medicine in Brazil. Many parts of the noni tree are utilized in such practices, including the roots, leaves and seeds. Through a search of online databases, the present article reviews 92 research studies on the biological actions of M. citrifolia. The paper will discuss the therapeutic effects of noni and its compounds in a variety of forms of presentation, focusing on studies that support its traditional use. A large and diverse number of properties were identified, which were divided into immunostimulatory, antitumor, antidiabetic, anti-obesity, antibacterial and anti-septic, antifungal, antiviral, leishmanicidal, antiinflammatory, antinociceptive and analgesic, antioxidant, neuroprotective, wound healing, antiallergic, antiangiogenic, antiemetic and anti-nausea, anti-gastric ulcer and oesophagitis, anthelmintic, antimutagenic, antipsychotic, anxiolytic, photoprotective, anti-wrinkle and periodontal tissue regeneration activities...
May 19, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28524111/synthesis-and-pharmacological-properties-of-novel-esters-based-on-monoterpenoids-and-glycine
#8
Mariia Nesterkina, Iryna Kravchenko
Esters based on mono- and bicyclic terpenoids with glycine have been synthesized via Steglich esterification and characterized by ¹H-NMR, IR, and mass spectral studies. Their analgesic and anti-inflammatory activities were investigated after transdermal delivery on models of formalin, capsaicin, and AITC-induced pain, respectively. Glycine esters of menthol and borneol exhibited higher antinociceptive action, whereas eugenol derivative significantly suppressed the development of the inflammatory process. The mechanism of competitive binding between terpenoid esters and TRPA1/TRPV1 agonists was proposed explaining significant analgesic effect of synthesized derivatives...
May 18, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28521385/-ziziphus-oxyphylla-ethnobotanical-ethnopharmacological-and-phytochemical-review
#9
REVIEW
Rizwan Ahmad, Niyaz Ahmad, Atta Abbas Naqvi
ETHNOPHARMACOLOGICAL RELEVANCE: Ziziphus oxyphylla (ZO) is distributed mainly in tropic and warm temperate regions in the world. Pakistan owns six (06) indigenous species of genus Ziziphus out of which ZO is widely used for traditional treatment of different ailments such as diabetes, jaundice and liver diseases. AIM OF THE STUDY: The present review aims to provide in-depth and comprehensive literature overview, regarding botanical, chemical and biological characteristics of the plant alongwith phytochemical isolation and mechanistic studies to support its folklore and traditional uses...
May 14, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28514833/antinociceptive-effect-of-%C3%AE-bisabolol-in-nanocapsules
#10
Gisele Façanha Diógenes Teixeira, Antonio Eufrásio Vieira-Neto, Flávio Nogueira da Costa, Angelo Roncalli Alves E Silva, Adriana Rolim Campos
This study aimed to develop and to evaluate the antinociceptive effect of a drug delivery system containing (-)-α-bisabolol (BISA). Nanocapsules containing BISA (BISA-NC) were prepared using acetylated galatomannan. Particle size distribution was determined by atomic force microscopy, zeta potential measurement and photon correlation spectroscopy. Corneal nociception was induced by topical application of 5M NaCl and the nociceptive behavior was characterized by eye wiping in mice. Molecular docking was conducted on the TRPV1 channel...
May 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28512601/anti-nociceptive-and-anti-inflammatory-potentials-of-vernoniaamygdalina-leaf-extract-via-reductions-of-leucocyte-migration-and-lipid-peroxidation
#11
Samuel Adetunji Onasanwo, Oyetola Tolulope Oyebanjo, Abayomi Mayowa Ajayi, Mujeedat Adebukola Olubori
BACKGROUND: Vernonia amygdalina is well known as a medicinal plant in folk medicine as antidiabetic, anthelmintic, antimalarial, laxative/purgative, and expectorant among others. AIM: This study was conducted to investigate the antinociceptive and anti-inflammatory effects of V. amygdalina. MATERIALS AND METHODS: Methanol extract of V. amygdalina leaf (MEVA) was evaluated for antinociceptive effect and possible mechanisms of action in the presence of naloxone (1 mg/kg), atropine (2 mg/kg), and prazosin (1 mg/kg) using acetic acid writhing test in mice...
April 2017: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/28510066/the-delta-opioid-receptor-in-pain-control
#12
Khaled Abdallah, Louis Gendron
Nowadays, the delta opioid receptor (DOPr) represents a promising target for the treatment of chronic pain and emotional disorders. Despite the fact that they produce limited antinociceptive effects in healthy animals and in most acute pain models, DOPr agonists have shown efficacy in various chronic pain models. In this chapter, we review the progresses that have been made over the last decades in understanding the role played by DOPr in the control of pain. More specifically, the distribution of DOPr within the central nervous system and along pain pathways is presented...
May 17, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28509855/the-hypnotic-anxiolytic-and-antinociceptive-profile-of-a-novel-%C3%A2%C2%B5-opioid-agonist
#13
Guilherme Carneiro Montes, Bianca Nascimento Monteiro da Silva, Bismarck Rezende, Roberto Takashi Sudo, Vitor Francisco Ferreira, Fernando de Carvalho da Silva, Angelo da Cunha Pinto, Bárbara Vasconcellos da Silva, Gisele Zapata-Sudo
5'-4-Alkyl/aryl-1H-1,2,3-triazole derivatives PILAB 1-12 were synthesized and a pharmacological screening of these derivatives was performed to identify a possible effect on the Central Nervous System (CNS) and to explore the associated mechanisms of action. The mice received a peritoneal injection (100 µmol/kg) of each of the 12 PILAB derivatives 10 min prior to the injection of pentobarbital and the mean hypnosis times were recorded. The mean hypnosis time increased for the mice treated with PILAB 8, which was prevented when mice were administered CTOP, a µ-opioid antagonist...
May 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28508197/antinociceptive-effect-of-the-agonist-of-5-ht1a-receptors-buspirone-in-the-model-of-abdominal-pain-in-dogs
#14
O A Lyubashina, I I Busygina, S S Panteleev, A D Nozdrachev
We have demonstrated that activation of 5-HT1A receptors with buspirone promotes visceral analgesia in awake dogs. The administration of 0.035 mg/kg (i.m.) of the drug caused depression of viscero-motor (contraction of the abdominal muscles) and pressor (increase in the heart rate) responses to noxious distension of the large intestine. An increase in the dose to 0.07 and 0.14 mg/kg did not enhance the antinociceptive effect of buspirone but triggered basal tachycardia. The obtained results provide evidence of the inhibitory role of 5-HT1A receptors in modulating visceral pain sensitivity and the possibility of an exciting effect of their activation on the cardiovascular system...
March 2017: Doklady Biological Sciences: Proceedings of the Academy of Sciences of the USSR, Biological Sciences Sections
https://www.readbyqxmd.com/read/28508174/preclinical-comparison-of-mechanistically-different-antiseizure-antinociceptive-and-or-antidepressant-drugs-in-a-battery-of-rodent-models-of-nociceptive-and-neuropathic-pain
#15
Misty D Smith, Jose H Woodhead, Laura J Handy, Timothy H Pruess, Fabiola Vanegas, Erin Grussendorf, Joel Grussendorf, Karen White, Karolina K Bulaj, Reisa K Krumin, Megan Hunt, Karen S Wilcox
The series of experiments herein evaluated prototype drugs representing different mechanisms of antiseizure, antinociceptive or antidepressant action in a battery of preclinical pain models in adult male CF#1 mice (formalin, writhing, and tail flick) and Sprague Dawley rats partial sciatic nerve ligation (PSNL). In the formalin assay, phenytoin (PHT, 6 mg/kg), sodium valproate (VPA, 300 mg/kg), amitriptyline (AMI, 7.5 and 15 mg/kg), gabapentin (GBP, 30 and 70 mg/kg), tiagabine (TGB, 5 and 15 mg/kg), and acetominophen (APAP, 250 and 500 mg/kg) reduced both phases of the formalin response to ≤ 25% of vehicle-treated mice...
May 15, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28507784/geraniin-attenuates-naloxone-precipitated-morphine-withdrawal-and-morphine-induced-tolerance-in-mice
#16
Ella Anle Kasanga, Eric Boakye-Gyasi, Robert Peter Biney, James Oppong Kyekyeku, Christian Agyare, Eric Woode
BACKGROUND AND AIM: Potentially life-threatening and unpleasant side effects associated with some analgesics have fueled the drive for the search for more analgesics with better side effect profiles. Geraniin, the most dominant secondary metabolite in the aqueous extract of the aerial parts of Phyllanthus muellerianus, has been shown to possess antinociceptive properties mediated partly by opioidergic mechanisms. The purpose of this study is to determine whether geraniin exhibits tolerance and if it is able to ameliorate withdrawal signs in naloxone-precipitated morphine withdrawal...
April 2017: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/28502978/the-opioid-receptor-triple-agonist-dpi-125-produces-analgesia-with-less-respiratory-depression-and-reduced-abuse-liability
#17
Shou-Pu Yi, Qing-Hong Kong, Yu-Lei Li, Chen-Ling Pan, Jie Yu, Ben-Qiang Cui, Ying-Fei Wang, Guan-Lin Wang, Pei-Lan Zhou, Li-Li Wang, Ze-Hui Gong, Rui-Bin Su, Yue-Hai Shen, Gang Yu, Kwen-Jen Chang
Opioid analgesics remain the first choice for the treatment of moderate to severe pain, but they are also notorious for their respiratory depression and addictive effects. This study focused on the pharmacology of a novel opioid receptor mixed agonist DPI-125 and attempted to elucidate the relationship between the δ-, μ- and κ-receptor potency ratio and respiratory depression and abuse liability. Five diarylmethylpiperazine compounds (DPI-125, DPI-3290, DPI-130, KUST202 and KUST13T02) were selected for this study...
May 15, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28502907/neuropathic-and-inflammatory-antinociceptive-effects-and-electrocortical-changes-produced-by-salvia-divinorum-in-rats
#18
Karina Simón-Arceo, Ma Eva González-Trujano, Ulises Coffeen, Rodrigo Fernández-Mas, Francisco Mercado, Angélica Almanza, Bernardo Contreras, Orlando Jaimes, Francisco Pellicer
ETHNOPHARMACOLOGICAL RELEVANCE: Salvia divinorum Epling et Játiva-M (SD, Lamiaceae) is a medicinal plant traditionally used in hallucinogenic ethnopharmacological practices and for its analgesic and antinflammatory properties. Its active compounds include diterpenes known as salvinorins which act as potent κ opioid receptor agonists. AIM OF THE STUDY: Given its effects in acute animal models of pain, as well as its antinflammatory attributes, we decided to investigate the analgesic effects of an SD extract in neuropathic (sciatic loose nerve ligature) and inflammatory (intra plantar carrageenan) pain models in rats...
May 11, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28502631/a-brain-targeted-ampakine-compound-protects-against-opioid-induced-respiratory-depression
#19
Wei Dai, Dian Xiao, Xiang Gao, Xin-Bo Zhou, Tong-Yu Fang, Zheng Yong, Rui-Bin Su
The use of opioid drugs for pain relief can induce life-threatening respiratory depression. Although naloxone effectively counteracts opioid-induced respiratory depression, it diminishes the efficacy of analgesia. Our studies indicate that ampakines, in particular, a brain-targeted compound XD-8-17C, are able to reverse respiratory depression without affecting analgesia at relatively low doses. Mice and rats were subcutaneously or intravenously injected with the opioid agonist TH-030418 to induce moderate or severe respiratory depression...
May 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28502630/new-opioid-receptor-antagonist-naltrexone-14-o-sulfate-synthesis-and-pharmacology
#20
Ferenc Zádor, Kornél Király, András Váradi, Mihály Balogh, Ágnes Fehér, Dóra Kocsis, Anna I Erdei, Erzsébet Lackó, Zoltán S Zádori, Sándor Hosztafi, Béla Noszál, Pál Riba, Sándor Benyhe, Susanna Fürst, Mahmoud Al-Khrasani
Opioid antagonists, naloxone and naltrexone have long been used in clinical practice and research. In addition to their low selectivity, they easily pass through the blood-brain barrier. Quaternization of the amine group in these molecules, (e.g. methylnaltrexone) results in negligible CNS penetration. In addition, zwitterionic compounds have been reported to have limited CNS access. The current study, for the first time gives report on the synthesis and the in vitro [competition binding, G-protein activation, isolated mouse vas deferens (MVD) and mouse colon assay] pharmacology of the zwitterionic compound, naltrexone-14-O-sulfate...
May 11, 2017: European Journal of Pharmacology
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