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Antinociception

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https://www.readbyqxmd.com/read/28447789/exploring-the-role-of-n-6-substituents-in-potent-dual-acting-5-c-ethyl-tetrazolyl-adenosine-derivatives-synthesis-binding-functional-assays-and-antinociceptive-effects-in-mice
#1
Riccardo Petrelli, Mirko Scortichini, Sonja Kachler, Serena Boccella, Carmen Cerchia, Ilaria Torquati, Fabio Del Bello, Daniela Salvemini, Ettore Novellino, Livio Luongo, Sabatino Maione, Kenneth A Jacobson, Antonio Lavecchia, Karl-Norbert Klotz, Loredana Cappellacci
Structural determinants of affinity of N(6)-substituted-5'-C-(ethyl-tetrazol-2-yl)-adenosine and 2-chloro-adenosine derivatives at adenosine receptor (AR) subtypes were studied with binding and molecular modeling. Small N(6)-cycloalkyl and 3-halo-benzyl groups furnished potent dual acting A1AR agonists and A3AR antagonists. 4 was the most potent dual acting human (h) A1AR agonist (Ki = 0.45 nM) and A3AR antagonist (Ki = 0.31 nM) and highly selective versus A2A; 11 and 26 were most potent at both h and rat (r) A3AR...
April 27, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28446950/analgesic-effect-of-17%C3%AE-estradiol-on-nucleus-paragigantocellularis-lateralis-of-male-rats-mediated-via-gabaa-receptors
#2
Roghaieh Khakpay, Maryam Azaddar, Fatemeh Khakpay, Homeira Hatami Nemati
INTRODUCTION: Beside its autonomic functions, the nucleus paragigantocellularis lateralis (LPGi) is involved in the descending pain modulation. 17β-Estradiol is a neuroactive steroid found in several brain areas such as LPGi. Intra-LPGi microinjection of 17β-estradiol can elicit the analgesic responses. 17β-Estradiol modulates nociception by binding to estrogenic receptors as well as allosteric interaction with other membrane-bound receptors like GABAA receptors. This study aimed to examine the role of GABAA receptors in the pain modulating effect of intra-LPGi injection of 17β-estradiol...
January 2017: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/28446883/in-vitro-and-in-vivo-profile-of-ppl-101-and-ppl-103-mixed-opioid-partial-agonist-analgesics-with-low-abuse-potential
#3
Taline V Khroyan, Andrea Cippitelli, Nicholas Toll, John A Lawson, William Crossman, Willma E Polgar, Lawrence Toll
Opiates are still the most effective and widely used treatments for acute and chronic pain. However, the problems associated with morphine and other standard opioid analgesics severely limit their effectiveness in the clinic. PPL-101 and PPL-103 derived from morphine and morphinan ring systems contain a chiral N-substituent, which confers it with a unique combination of high-binding affinities and partial agonist activities at mu, delta, and kappa opioid receptors, leading to unique in vivo pharmacology compared to other conventional opioids...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28446831/antinociceptive-and-antioxidant-activities-of-the-methanolic-extract-of-telfairia-occidentalis-seeds
#4
Olukemi Adetutu Osukoya, Daniel Adegbenro, Sunday A Onikanni, Oluwafemi A Ojo, Amos Onasanya
CONTEXT: The seeds of Telfairia occidentalis have been known to possess different biological properties and are used in traditional medicine in Africa and Asia to treat many ailments. The plant is particularly noted traditionally for its healing properties and is usually consumed in the form of herbal decoctions/concoctions as a blood tonic, to treat sudden attacks of convulsions, pain, malaria and anaemia. AIMS: In the present study, various phytochemical and pharmacological studies were done on the methanolic extract of the seeds of Telfairia occidentalis to evaluate its antioxidant and antinociceptive properties to substantiate its traditional use...
October 2016: Ancient Science of Life
https://www.readbyqxmd.com/read/28445853/cannabidiol-%C3%AE-9-tetrahydrocannabinol-interactions-on-acute-pain-and-locomotor-activity
#5
Stevie C Britch, Jenny L Wiley, Zhihao Yu, Brian H Clowers, Rebecca M Craft
BACKGROUND: Previous studies suggest that cannabidiol (CBD) may potentiate or antagonize Δ(9)-tetrahydrocannabinol's (THC) effects. The current study examined sex differences in CBD modulation of THC-induced antinociception, hypolocomotion, and metabolism. METHODS: In Experiment 1, CBD (0, 10 or 30mg/kg) was administered 15min before THC (0, 1.8, 3.2, 5.6 or 10mg/kg), and rats were tested for antinociception and locomotion 15-360min post-THC injection. In Experiments 2 and 3, CBD (30mg/kg) was administered 13h or 15min before THC (1...
April 15, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28445495/pharmacokinetic-and-pharmacodynamic-modelling-after-subcutaneous-intravenous-and-buccal-administration-of-a-high-concentration-formulation-of-buprenorphine-in-conscious-cats
#6
Graeme M Doodnaught, Beatriz P Monteiro, Javier Benito, Daniel Edge, Francis Beaudry, Ludovic Pelligand, Paulo Steagall
BACKGROUND: The aim of this study was to describe the joint pharmacokinetic-pharmacodynamic model and evaluate thermal antinociception of a high-concentration formulation of buprenorphine (Simbadol™) in cats. METHODS: Six healthy cats (4.9 ± 0.7 kg) were included in a prospective, randomized, blinded, crossover study. Simbadol™ (1.8 mg mL-1) was administered by the subcutaneous (SC; 0.24 mg kg-1), intravenous (IV; 0.12 mg kg-1) or buccal (OTM; 0.12 mg kg-1) route of administration and thermal thresholds (TT) were compared with a saline group (SAL)...
2017: PloS One
https://www.readbyqxmd.com/read/28442945/pulse-train-stimulation-of-primary-somatosensory-cortex-blocks-pain-perception-in-tail-clip-test
#7
Soohyun Lee, Eunjin Hwang, Dongmyeong Lee, Jee Hyun Choi
Human studies of brain stimulation have demonstrated modulatory effects on the perception of pain. However, whether the primary somatosensory cortical activity is associated with antinociceptive responses remains unknown. Therefore, we examined the antinociceptive effects of neuronal activity evoked by optogenetic stimulation of primary somatosensory cortex. Optogenetic transgenic mice were subjected to continuous or pulse-train optogenetic stimulation of the primary somatosensory cortex at frequencies of 15, 30, and 40 Hz, during a tail clip test...
April 2017: Experimental Neurobiology
https://www.readbyqxmd.com/read/28442584/apparent-cb1-receptor-rimonabant-affinity-estimates-combination-with-thc-and-synthetic-cannabinoids-in-the-mouse-in-vivo-triad-model
#8
Travis W Grim, Anthony J Morales, Brian F Thomas, Jenny L Wiley, Gregory W Endres, Sidney S Negus, Aron H Lichtman
Synthetic cannabinoids (SCs) represent an emerging class of abused drugs associated with psychiatric complications and other substantial health risks. These ligands are largely sold over the internet for human consumption presumably because of their high cannabinoid 1 receptor (CB1R) affinity and potency in eliciting similar pharmacological effects as Δ9-tetrahydrocannabinol (THC), while circumventing laws illegalizing this plant. Factors potentially contributing to the increased prevalence of SC abuse and related hospitalizations, such as increased CB1R efficacy and non-CB1R targets, highlight the need for quantitative pharmacological analyses to determine receptor mediation of the pharmacological effects of cannabinoids...
April 25, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28442580/ethanol-reversal-of-tolerance-to-the-antinociceptive-effects-of-oxycodone-and-hydrocodone
#9
Joanna C Jacob, Justin L Poklis, Hamid I Akbarali, Graeme Henderson, William L Dewey
This study compared the development of tolerance and its reversal by ethanol of two orally-bioavailable prescription opioids, oxycodone and hydrocodone, to that of morphine. Oxycodone (s.c) was significantly more potent in the mouse tail withdrawal assay than either morphine or hydrocodone. Oxycodone was also significantly more potent in this assay than hydrocodone when administered orally. Tolerance was seen following chronic subcutaneous administration of each of the three drugs and by the chronic administration of oral oxycodone, but not following the chronic oral administration of hydrocodone...
April 25, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28440889/a-glucagon-like-peptide-1-analog-liraglutide-improves-visceral-sensation-and-gut-permeability-in-rats
#10
Tsukasa Nozu, Saori Miyagishi, Shima Kumei, Rintaro Nozu, Kaoru Takakusaki, Toshikatsu Okumura
BACKGROUND AND AIM: A glucagon-like peptide-1 (GLP-1) analog, liraglutide, has been reported to block inflammatory somatic pain. We hypothesized that liraglutide attenuates lipopolysaccharide (LPS)- and repeated water avoidance stress (WAS)-induced visceral hypersensitivity and tested the hypothesis in rats. METHODS: The threshold of the visceromotor response (VMR) induced by colonic balloon distention was measured to assess visceral sensation. Colonic permeability was determined in vivo by quantifying the absorbed Evans blue spectrophotometrically, which was instilled in the proximal colon for 15 min...
April 25, 2017: Journal of Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28437805/anti-inflammatory-antipyretic-and-antinociceptive-effects-of-a-cressa-cretica-aqueous-extract
#11
Heba Mohammed Ibrahim Abdallah, Abdelsamed Ibrahim Elshamy, Abd El-Nasser Gaber El Gendy, Ahmed Mohamed Abd El-Gawad, Elsayed Abouelfotowh Omer, Marinella De Leo, Luisa Pistelli
Cressa cretica is a widely grown halophytic plant traditionally used for the treatment of different ailments. Previous investigations reported its biological activity on a wide spectrum of diseases. In this study, in vivo antinociceptive, anti-inflammatory, and antipyretic activities of C. cretica aqueous extract whole plant were evaluated. In addition, the total polyphenol content, the total flavonoid content, and the chemical characterization of the extract were performed. C. cretica showed writhing inhibition in acetic acid-induced peripheral nociception of 43 and 48 % at doses of 50 and 100 mg/kg, respectively...
April 24, 2017: Planta Medica
https://www.readbyqxmd.com/read/28436532/bis-phenylimidazoselenazolyl-diselenide-elicits-antinociceptive-effect-by-modulating-myeloperoxidase-activity-nox-and-nfkb-levels-in-the-collagen-induced-arthritis-mouse-model
#12
Pietro M Chagas, Bruna C W Fulco, Marcel H M Sari, Juliano A Roehrs, Cristina W Nogueira
Bis(phenylimidazoselenazolyl) diselenide (BPIS) is an organoselenium with acute antinociceptive and antioxidant properties. OBJECTIVES: The aim of this study was to investigate BPIS effect on a collagen-induced arthritis (CIA) model in mice. METHODS: Protocol of exposure consisted in arthritis induction by chicken collagen type II on day 0 with booster injection on day 21. On day 60 after collagen injection, incidence of mechanic allodynia (Von Frey test) or thermal hyperalgesia (hot plate test) was evaluated...
April 24, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28432424/variations-of-isovaline-structure-related-to-activity-in-the-formalin-foot-assay-in-mice
#13
Timothy Fung, Yahya I Asiri, Richard Wall, Stephan K W Schwarz, Ernest Puil, Bernard A MacLeod
Current centrally acting analgesics such as opioids are associated with adverse effects that limit their use and threaten patient safety. Isovaline is a novel prototype analgesic that produces peripheral antinociception in several pain models with little or no effect on the central nervous system. The aim of this study was to establish a preliminary structure-activity relationship for isovaline derivatives by assaying efficacy in the formalin foot assay and central adverse effect profile in mice. Selected compounds were tested using the formalin foot assay to determine efficacy in reducing formalin-induced behaviors...
April 21, 2017: Amino Acids
https://www.readbyqxmd.com/read/28420580/comparative-pharmacodynamic-analysis-of-imidazoline-compounds-using-rat-model-of-ocular-mydriasis-with-a-test-of-quantitative-structure-activity-relationships
#14
Joanna Raczak-Gutknecht, Antoni Nasal, Teresa Frąckowiak, Anita Kornicka, Franciszek Sączewski, Renata Wawrzyniak, Łukasz Kubik, Roman Kaliszan
Imidazol(in)e derivatives, having the chemical structure similar to clonidine, exert diverse pharmacological activities connected with their interactions with alpha2-adrenergic receptors, e.g. hypotension, bradycardia, sedation as well as antinociceptive, anxiolytic, antiarrhythmic, muscle relaxant and mydriatic effects. The mechanism of pupillary dilation observed after systemic administration of imidazol(in)es to rats, mice and cats depends on the stimulation of postsynaptic alpha2-adrenoceptors within the brain...
April 6, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28419516/systemic-and-local-anti-nociceptive-effects-of-simvastatin-in-the-rat-formalin-assay-role-of-peroxisome-proliferator-activated-receptor-%C3%AE-and-nitric-oxide
#15
Mohammad Taghi Mansouri, Bahareh Naghizadeh, Behnam Ghorbanzadeh, Soheila Alboghobeish
This study aimed to determine the potential systemic and local anti-nociceptive effects of simvastatin (SIM) and the possible role of peroxisome proliferator-activated receptor gamma (PPARγ) and nitric oxide (NO) pathways using a formalin assay in rats. After allocation, rats were intraplantarly (i.pl.) treated with formalin solution (2.5%) and the flinching behaviors were recorded for 5 min (phase 1) and 15-60 min (phase 2). SIM was given intraperitoneally (i.p.) and i.pl. 30 and 20 min before test, respectively...
April 17, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28416993/antinociceptive-effect-of-intrathecal-sec-o-glucosylhamaudol-on-the-formalin-induced-pain-in-rats
#16
Sang Hun Kim, Hwa Song Jong, Myung Ha Yoon, Seon Hee Oh, Ki Tae Jung
BACKGROUND: The root of Peucedanum japonicum Thunb., a perennial herb found in Japan, the Philippines, China, and Korea, is used as an analgesic. In a previous study, sec-O-glucosylhamaudol (SOG) showed an analgesic effect. This study was performed to examine the antinociceptive effect of intrathecal SOG in the formalin test. METHODS: Male Sprague-Dawley rats were implanted with an intrathecal catheter. Rats were randomly treated with a vehicle and SOG (10 µg, 30 µg, 60 µg, and 100 µg) before formalin injection...
April 2017: Korean Journal of Pain
https://www.readbyqxmd.com/read/28412475/potential-anti-inflammatory-effect-of-lqfm-021-in-carrageenan-induced-inflammation-the-role-of-nitric-oxide
#17
Iziara F Florentino, Daiany P B Silva, Dayane M Silva, Carina Sofia Cardoso, André L E Moreira, Clayton L Borges, Célia M de A Soares, Pablinny M Galdino, Luciano M Lião, Paulo C Ghedini, Ricardo Menegatti, Elson A Costa
The pyrazole compound LQFM-021 exhibits vasorelaxant, antinociceptive and anti-inflammatory activities. Furthermore, it has low toxicity, indicating that this compound may be considered to be a good prototype for the development of new analgesic/anti-inflammatory drugs. Therefore, the aim of this study was to investigate the potential anti-inflammatory activity of LQFM-021 using a model of carrageenan-induced inflammation as well as the mechanism of action and role of nitric oxide in this effect. Acute treatments with LQFM-021 (30 and 60 mg/kg p...
April 12, 2017: Nitric Oxide: Biology and Chemistry
https://www.readbyqxmd.com/read/28412371/the-anti-inflammatory-effect-of-tramadol-in-the-temporomandibular-joint-of-rats
#18
Simone Monaliza S Lamana, Marcelo H Napimoga, Ana Paula Camatta Nascimento, Fabiana F Freitas, Daniele R de Araujo, Mariana S Quinteiro, Cristina G Macedo, Carlos L Fogaça, Juliana T Clemente-Napimoga
Tramadol is a centrally acting analgesic drug able to prevent nociceptor sensitization when administered into the temporomandibular joint (TMJ) of rats. The mechanism underlying the peripheral anti-inflammatory effect of tramadol remains unknown. This study demonstrated that intra-TMJ injection of tramadol (500µg/TMJ) was able to inhibit the nociceptive response induced by 1.5% formalin or 1.5% capsaicin, suggesting that tramadol has an antinociceptive effect, acting directly on the primary nociceptive neurons activating the nitric oxide/cyclic guanosine monophosphate signaling pathway...
April 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28411257/relief-of-pain-depressed-behavior-in-rats-by-activation-of-d1-like-dopamine-receptors
#19
Matthew F Lazenka, Kelen C Freitas, Sydney Henck, S Stevens Negus
Clinically significant pain often includes depression of both behavior and mesolimbic dopamine signaling. Indirect and/or direct dopamine receptor agonists may alleviate pain-related behavioral depression. To test this hypothesis, the present study compared effects of indirect and direct dopamine agonists in a preclinical assay of pain-depressed operant responding. Male Sprague-Dawley rats with chronic indwelling microelectrodes in the medial forebrain bundle were trained in an intracranial self-stimulation (ICSS) procedure to press a lever for pulses of electrical brain stimulation...
April 14, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28391533/the-validation-of-calophyllum-brasiliense-guanandi-uses-in-brazilian-traditional-medicine-as-analgesic-by-in-vivo-antinociceptive-evaluation-and-its-chemical-analysis
#20
Luiz Carlos Klein-Júnior, Daniele Zambiasi, Giovana Rocha Salgado, Franco Delle Monache, Valdir Cechinel Filho, Fátima de Campos Buzzi
Calophyllum brasiliense is used as anti-inflammatory and analgesic in Brazilian traditional medicine. Thus, the main purpose of this study is to evaluate the antinociceptive effect of the chloroform fraction of C. brasiliense (CFCB) roots and to investigate its main mechanism of action. The antinociceptive effect of CFCB was evaluated in mice using acetic acid-induced writhing, formalin-induced paw licking, and hot-plate tests and capsaicin- and glutamate-induced nociception. Brasiliensic acid and 1,2-dimethoxyxanthone were isolated and evaluated in writhing test...
April 8, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
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