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https://www.readbyqxmd.com/read/28723417/long-term-morphine-delivery-via-slow-release-morphine-pellets-or-osmotic-pumps-plasma-concentration-analgesia-and-naloxone-precipitated-withdrawal
#1
Virginia D McLane, Ivy Bergquist, James Cormier, Deborah J Barlow, Karen L Houseknecht, Edward J Bilsky, Ling Cao
AIMS: Slow-release morphine sulfate pellets and osmotic pumps are common routes of chronic morphine delivery in mouse models, but direct comparisons of these drug delivery systems are lacking. In this study, we assessed the efficacy of slow-release pellets versus osmotic pumps in delivering morphine to adult mice. MAIN METHODS: Male C57BL/6NCr mice (8weeksold) were implanted subcutaneously with slow-release pellets (25mg morphine sulfate) or osmotic pumps (64mg/mL, 1...
July 16, 2017: Life Sciences
https://www.readbyqxmd.com/read/28720466/antinociceptive-effects-of-huf-101-a-fluorinated-cannabidiol-derivative
#2
Nicole R Silva, Felipe V Gomes, Miriam D Fonseca, Raphael Mechoulam, Aviva Breuer, Thiago M Cunha, Francisco S Guimarães
Cannabidiol (CBD) is a phytocannabinoid with multiple pharmacological effects and several potential therapeutic properties. Its low oral bioavailability, however, can limit its clinical use. Preliminary results indicate that fluorination of the CBD molecule increases its pharmacological potency. Here, we investigated whether HUF-101 (3, 10, and 30mg/kg), a fluorinated CBD analogue, would induce antinociceptive effects. HUF-101 effects were compared to those induced by CBD (10, 30, and 90mg/kg) and the cannabinoid CB1/2 receptor agonist WIN55,212-2 (1, 3, and 5mg/kg)...
July 15, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28720004/antinociceptive-synergistic-interaction-between-achillea-millefolium-and-origanum-vulgare-l-extract-encapsulated-in-liposome-in-rat
#3
Farshad Hassanzadeh-Kiabi, Babak Negahdari
AIM: This study aims to evaluate the antinociceptive effect of combined Achillea millefolium and Origanum extract encapsulated in liposome. METHODS: The effect of Achillea millefolium and Origanum vulgare L. extract, and their liposome-incorporated form was assessed using 3% formalin test in rat. 12 male Wistar rats, 4 in each group, were used in this study, and increasing doses of Achillea millefolium (31.6, 100, 178, and 316 mg/kg) and Origanum vulgare L. extract (5...
July 18, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28719859/-curcumin-loaded-poly-d-l-lactide-co-glycolide-nanovesicles-induce-antinociceptive-effects-and-reduce-pronociceptive-cytokine-and-bdnf-release-in-spinal-cord-after-acute-administration-in-mice
#4
Stefano Pieretti, Amalendu P Ranjan, Amalia Di Giannuario, Anindita Mukerjee, Francesca Marzoli, Rita Di Giovannandrea, Jamboor K Vishwanatha
Given the poor bioavailability of curcumin, its antinociceptive effects are produced after chronic intravenous administration of high doses, while poly (d,l-lactide-co-glycolide)-loaded vesicles (PLGA) can improve drug delivery. This paper investigates the antinociceptive effects of curcumin-loaded PLGA nanovesicles (PLGA-CUR) administered via intravenous (i.v.) or intrathecal (i.t.) routes at low and high doses. The following models of pain were used: formalin test, zymosan-induced hyperalgesia and sciatic nerve ligation inducing neuropathic allodynia and hyperalgesia...
July 10, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28716934/sigma-1-receptors-control-immune-driven-peripheral-opioid-analgesia-during-inflammation-in-mice
#5
Miguel A Tejada, Angeles Montilla-García, Shane J Cronin, Domagoj Cikes, Cristina Sánchez-Fernández, Rafael González-Cano, M Carmen Ruiz-Cantero, Josef M Penninger, José M Vela, José M Baeyens, Enrique J Cobos
Sigma-1 antagonism potentiates the antinociceptive effects of opioid drugs, so sigma-1 receptors constitute a biological brake to opioid drug-induced analgesia. The pathophysiological role of this process is unknown. We aimed to investigate whether sigma-1 antagonism reduces inflammatory pain through the disinhibition of the endogenous opioidergic system in mice. The selective sigma-1 antagonists BD-1063 and S1RA abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute (3 h) inflammation...
July 17, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28715803/antinociceptive-effects-of-isosakuranetin-in-a-rat-model-of-peripheral-neuropathy
#6
Shushan Jia, Yong Zhang, Jingui Yu
Chronic pain remains a challenging clinical reality, yet currently available analgesics are insufficient to meet clinical needs. Increasing attention has been paid to bioactive compounds from natural plants, which may be efficacious against pain. This study examined the antinociceptive effects of isosakuranetin, a plant-derived transient receptor potential melastatin 3 blocker, in a rat model of peripheral neuropathy. Adult male Sprague-Dawley rats were first allowed to go through the chronic constriction injury surgery to develop neuropathic pain...
July 18, 2017: Pharmacology
https://www.readbyqxmd.com/read/28711635/a-new-pupillary-measure-to-assess-pain-a-prospective-study
#7
David J Charier, Daniel Zantour, Vincent Pichot, Florian Chouchou, Jean-Claude M Barthelemy, Frederic Roche, Serge B Molliex
Pupillary diameter (PD) varies under the influence of both the sympathetic and parasympathetic systems, increasing proportionally to pain intensity. Such variations however should not be confused with pupillary fluctuations, which refer to the fast and permanent PD fluctuations induced by the ongoing interplay between the sympathetic and parasympathetic systems, which we propose to measure using the Variation Coefficient of Pupillary Diameter (VCPD). This study aimed first at correlating both PD, PD increase during a contraction, and VCPD, with pain as rated with the Numerical Rating Scale (NRS) during obstetrical labor, and then at comparing such correlations with one another...
July 12, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28709955/neonatal-injury-results-in-sex-dependent-nociceptive-hypersensitivity-and-social-behavioral-deficits-during-adolescence-without-altering-morphine-response
#8
Nikita N Burke, Tuan Trang
Neonatal injury is associated with persistent changes in sensory function and altered nociceptive thresholds that give rise to aberrant pain sensitivity in later life. While these changes are well documented in adult rodents, little is known about the consequences of neonatal injury during adolescence. Since adolescence is a critical developmental period during which persistent pain conditions can arise, we examined the impact of neonatal injury on nociception, social behavior and response to morphine in adolescent Sprague Dawley rats...
July 11, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28704800/inclusion-complex-between-%C3%AE-cyclodextrin-and-hecogenin-acetate-produces-superior-analgesic-effect-in-animal-models-for-orofacial-pain
#9
Yasmim M B G Carvalho, Paula P Menezes, Bruna M H Sousa, Bruno S Lima, Igor A S Trindade, Mairim R Serafini, Erik W M Pereira, Marilia M Rezende, Jullyana S S Quintans, Lucindo J Quintans-Júnior, Celso V Nakamura, Edeildo F Silva-Júnior, Alessandre C Crispim, Thiago M Aquino, Adriano A S Araújo
Hecogenin acetate (HA) is a steroidal sapogenin-acetylated with pharmacological properties which have already been described in the literature such as, anti-inflammatory, anti-hyperalgesic and antinociceptive, but it has low solubility in aqueous media. Therefore, in an attempt to overcome this, we set out to create inclusion complexes between HA and b-cyclodextrin (b-CD) and evaluate the antinociceptive effects in the orofacial nociception in mice. The complexes were prepared using different methods in the molar ratios 1:1 and 1:2 and characterized physicochemically...
July 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28704145/adult-zebrafish-danio-rerio-an-alternative-behavioral-model-of-formalin-induced-nociception
#10
Francisco Ernani Alves Magalhães, Caio Átila Prata Bezerra de Sousa, Sacha Aubrey Alves Rodrigues Santos, Renata Barbosa Menezes, Francisco Lucas Alves Batista, Ângela Oliveira Abreu, Messias Vital de Oliveira, Luiz Francisco Wemmenson Gonçalves Moura, Ramon da Silva Raposo, Adriana Rolim Campos
The zebrafish (Danio rerio) has been proposed as a low-cost and simple alternative to the use of higher vertebrates in laboratory research on novel compounds with antinociceptive potential. In this study, we tested adult zebrafish (Danio rerio) as an alternative behavioral model of formalin-induced nociception. We evaluated the nociceptive effect of 0.1% formalin (3 or 5 μL; intramuscularly [i.m.]), applied into the tail or lips, on locomotor activity, using as parameter the number of times the fish crossed the lines between the quadrants of a glass Petri dish during the neurogenic stage (0-5 min) and the inflammatory stage (15-30 min)...
July 13, 2017: Zebrafish
https://www.readbyqxmd.com/read/28700700/the-induction-of-the-transcription-factor-nrf2-enhances-the-antinociceptive-effects-of-delta-opioid-receptors-in-diabetic-mice
#11
Christina McDonnell, Sergi Leánez, Olga Pol
The involvement of heme oxygenase 1 (HO-1) in the modulation of the antinociceptive effects of opioids in type 1 diabetes has been demonstrated but the role played by the transcription factor Nrf2 in the regulation of painful neuropathy and in the effects and expression of δ-opioid receptors (DOR) in type 2 diabetes, has not been studied. In male BKS.Cg-m+/+Leprdb/J (db/db) mice, the anti-allodynic effects produced by a Nrf2 transcription factor activator, sulforaphane (SFN) administered alone and combined with two DOR agonists, [d-Pen(2),d-Pen(5)]-Enkephalin (DPDPE) and (+)-4-[(αR)-α-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N diethylbenzamide (SNC-80), were evaluated...
2017: PloS One
https://www.readbyqxmd.com/read/28699722/antinociceptive-anti-inflammatory-and-antiarthritic-activities-of-bungarus-fasciatus-venom-in-experimental-animal-models
#12
Susmita Ghosh, Partha Pratim Saha, Subir C Dasgupta, Antony Gomes
Pain and inflammation are intimately associated with rheumatoid arthritis, a growing bone-joint related problem of the modern society. Though several therapeutic managements are available for arthritis, their side effects not only limit their use, but also advocate the quest for natural therapies. In this study, we explored the antinociceptive, anti-inflammatory and antiarthritic activities of Bungarus fasciatus venom (BFV) in experimental animal models. Rheumatoid arthritis was induced by Freund’s complete adjuvant (FCA) in male Wistar albino rats...
September 2016: Indian Journal of Experimental Biology
https://www.readbyqxmd.com/read/28699698/reduced-dosing-and-liability-in-methadone-maintenance-treatment-by-targeting-oestrogen-signal-for-morphine-addiction
#13
Yao-Chang Chiang, Ruey-Yun Wang, Chieh-Liang Huang, Shue-Hwa Chen, Wen-Jing Ho, Hsien-Yuan Lane, Ing-Kang Ho, Hwei-Ting Yang, Wen-Lung Ma
Methadone maintenance treatment (MMT) is the major tapering therapy for morphine addictive patients. There have gender differences reported in response to MMT. This study discovered that the estrogen-response element single nucleotide polymorphism (ERE-SNP; rs16974799, C/T) of cytochrome 2B6 gene (cyp2b6; methadone catabolic enzyme) responded differently to MMT dosing. Oestradiol was associated with high MMT dosing, high enantiomer (R- or S-) of 2-ethylidene-1,5-dimethyl-3,3-dipheny-pyrrolidine (EDDP; methadone metabolite) to methadone ratio and increased drug-seeking behaviour, implicating oestradiol-CYP-EDDP/methadone axis decreasing MMT efficacy...
July 12, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/28697954/antinociceptive-action-of-nop-and-opioid-receptor-agonists-in-the-mouse-orofacial-formalin-test
#14
A Rizzi, C Ruzza, S Bianco, C Trapella, G Calo'
Nociceptin/orphanin FQ (N/OFQ) modulates several biological functions, including pain transmission via selective activation of a specific receptor named NOP. The aim of this study was the investigation of the antinociceptive properties of NOP agonists and their interaction with opioids in the trigeminal territory. The orofacial formalin (OFF) test in mice was used to investigate the antinociceptive potential associated to the activation of NOP and opioid receptors. Mice subjected to OFF test displayed the typical biphasic nociceptive response and sensitivity to opioid and NSAID drugs...
July 8, 2017: Peptides
https://www.readbyqxmd.com/read/28691718/additive-and-antagonistic-antinociceptive-interactions-between-magnesium-sulfate-and-ketamine-in-the-rat-formalin-test
#15
Katarina Savić Vujović, Sonja Vučković, Dolika Vasović, Branislava Medić, Nick Knežević, Milica Prostran
Because ketamine and magnesium block NMDA receptor activation by distinct mechanisms of action, we hypothesized that in a model of inflammatory pain in rats the combination of ketamine and magnesium might be more effective than ketamine alone. Antinociceptive activity was assessed by the formalin test in male Wistar rats (200-250 g). Animals were injected with 100 μL of 2.5% formalin to the plantar surface of the right hind paw. Data were recorded as the total time spent in pain-related behavior after the injection of formalin or vehicle (0...
2017: Acta Neurobiologiae Experimentalis
https://www.readbyqxmd.com/read/28686967/the-anti-inflammatory-and-antinociceptive-activity-of-albumins-from-crotalaria-retusa-seeds
#16
Diego Passos Aragão, Bruna da Silva Souza, Tarcisio Vieira de Brito, Lucas de Araújo Bastos Santana, Renata Mariana de Paiva Silva, Ana Patrícia de Oliveira, Anna Carolina Toledo da Cunha Pereira, Gustavo Portela Ferreira, André Luiz Dos Reis Barbosa, Jefferson Soares de Oliveira
Seeds of Crotalaria retusa L. are used in popular medicine because of their pharmacological properties. The albumin fraction obtained from its seeds contains lectin, a protein known to have analgesic and anti-inflammatory properties. Thus, albumins extracted from C. retusa were investigated for their anti-inflammatory and antinociceptive effects. The intraperitoneal administration of different doses of albumins (5, 10 or 20mg/kg) significantly inhibited the mice paw edema induced by carrageenan (maximum inhibition rate of 80...
July 4, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28685673/physicochemical-and-pharmacological-characterization-of-permanently-charged-opioids
#17
Károly Mazák, Béla Noszál, Sándor Hosztafi
BACKGROUND: The main aim of synthesizing permanently charged opioids is to ensure they cannot enter the central nervous system. Such drugs can provide analgesic activity with reduced sedation and other central nervous system side effects. METHODS: We undertook a search of bibliographic databases for peer-reviewed research literature and also summarized our published results in this field. RESULTS: The present review focuses on the characterization of permanently charged opioids by various physicochemical methods, in vitro and in vivo tests...
July 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28684345/alterations-in-nociception-and-morphine-antinociception-in-mice-fed-a-high-fat-diet
#18
Caitlin M Nealon, Chandni Patel, Beth L Worley, Angela N Henderson-Redmond, Daniel J Morgan, Traci A Czyzyk
Currently, more than 78.6 million adults in the United States are obese. A majority of the patient population receiving treatment for pain symptoms is derived from this subpopulation. Environmental factors, including the increased availability of food high in fat and sugar, contribute to the continued rise in the rates of obesity. The focus of this study was to investigate whether long-term exposure to a high-fat, energy-dense diet enhances baseline thermal and inflammatory nociception while reducing sensitivity to morphine-induced antinociception...
July 3, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28680401/cannabidiol-is-a-potential-therapeutic-for-the-affective-motivational-dimension-of-incision-pain-in-rats
#19
Karina Genaro, Débora Fabris, Ana L F Arantes, Antônio W Zuardi, José A S Crippa, Wiliam A Prado
Background: Pain involves different brain regions and is critically determined by emotional processing. Among other areas, the rostral anterior cingulate cortex (rACC) is implicated in the processing of affective pain. Drugs that interfere with the endocannabinoid system are alternatives for the management of clinical pain. Cannabidiol (CBD), a phytocannabinoid found in Cannabis sativa, has been utilized in preclinical and clinical studies for the treatment of pain. Herein, we evaluate the effects of CBD, injected either systemically or locally into the rACC, on mechanical allodynia in a postoperative pain model and on the negative reinforcement produced by relief of spontaneous incision pain...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28676003/synthesis-structural-characterization-and-antinociceptive-activities-of-new-arylated-quinolines-via-suzuki-miyaura-cross-coupling-reaction
#20
Malik Aman Ullah, Muhammad Adeel, Muhammad N Tahir, Abdur Rauf, Muhammad Akram, Taibi Ben Hadda, Yahia N Mabkhot, Naveed Muhammad, Fehmida Naseer, Mohammad S Mubarak
Backgorund: The quinoline ring system is one of the most commonly encountered heterocycles in medicinal chemistry, due to the pharmaceutical and medicinal uses of derivatives containing this ring. These quinoline-based compounds have remarkable biological activity, as they are employed as antimalarial, antibacterial, antifungal, and antitumor agents. The quinoline nucleus can be synthesized by various traditional methods such as the Skraup reaction, Friedlaender synthesis, Combes quinoline synthesis, Larock quinoline synthesis, among others...
July 4, 2017: Medicinal Chemistry
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