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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
https://www.readbyqxmd.com/read/28390968/inhibition-of-substance-p-induced-defensive-behavior-via-neurokinin-1-receptor-antagonism-in-the-central-and-medial-but-not-basolateral-nuclei-of-the-amygdala-in-male-wistar-rats
#8
G S Bassi, M C Carvalho, R C Almada, M L Brandão
RATIONALE: The production of unconditioned defensive behaviors has been related to the amygdala, a key component of the encephalic aversion system. Microinjection of the neuropeptide substance P (SP) in the amygdala elicits defensive behaviors via the activation of type 1 neurokinin (NK-1) receptors. However, no studies have investigated whether intra-amygdala SP/NK-1 mechanisms can elicit other types of defensive responses, such as antinociception and ultrasonic vocalizations (USVs)...
April 5, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28390647/brain-derived-neurotrophic-factor-in-the-mesolimbic-reward-circuitry-mediates-nociception-in-chronic-neuropathic-pain
#9
Hongxing Zhang, Yi-Ling Qian, Chen Li, Di Liu, Lei Wang, Xiao-Yi Wang, Mei-Jun Liu, He Liu, Song Zhang, Xiao-Yun Guo, Jun-Xia Yang, Hai-Lei Ding, Ja Wook Koo, Ezekiell Mouzon, Karl Deisseroth, Eric J Nestler, Venetia Zachariou, Ming-Hu Han, Jun-Li Cao
BACKGROUND: The mesolimbic reward system plays a critical role in modulating nociception; however, its underlying molecular, cellular, and neural circuitry mechanisms remain unknown. METHODS: Chronic constrictive injury (CCI) of the sciatic nerve was used to model neuropathic pain. Projection-specific in vitro recordings in mouse brain slices and in vivo recordings from anesthetized animals were used to measure firing of dopaminergic neurons in the ventral tegmental area (VTA)...
March 1, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28386698/comparison-of-some-behavioral-effects-of-d-and-l-methamphetamine-in-adult-male-rats
#10
Justin N Siemian, Zhaoxia Xue, Bruce E Blough, Jun-Xu Li
RATIONALE: Both l- and d-methamphetamine (l- and d-MA) are more potent to release norpepinephrine (NE) than dopamine, and the selectivity is greater for l-MA than d-MA. Little is known of the in vivo pharmacology of l-MA. OBJECTIVE: This study compared the effects of l-MA and d-MA in assays of nociception, behavioral disruption, and impulsivity. METHODS: Antinociceptive effects of d- and l-MA were examined in two pain assays: the warm water tail withdrawal test for acute nociception and the von Frey test in complete Freund's adjuvant (CFA)-treated rats for chronic inflammatory pain...
April 6, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28386033/comparative-antinociceptive-and-sedative-effects-of-epidural-romifidine-and-detomidine-in-buffalo-bubalus-bubalis
#11
M A Marzok, S A El-Khodery
In this study, comparative antinociceptive and sedative effects of epidural administration of romifidine and detomidine in buffalo were evaluated. Eighteen healthy adult buffalo, allocated randomly in three groups (two experimental and one control; n=6) received either 50 μg/kg of romifidine or detomidine diluted in sterile saline (0.9 per cent) to a final volume of 20 ml, or an equivalent volume of sterile saline epidurally. Antinociception, sedation and ataxia parameters were recorded immediately after drug administration...
April 6, 2017: Veterinary Record
https://www.readbyqxmd.com/read/28381108/-express-amp-activated-kinase-and-the-endogenous-endocannabinoid-system-might-contribute-to-antinociceptive-effects-of-prolonged-moderate-caloric-restriction-in-mice
#12
Tanya Sarah King-Himmelreich, Christine Verena Möser, Miriam Christina Wolters, Julia Schmetzer, Moritz Möller, Yannik Schreiber, Nerea Ferreirós, Gerd Geisslinger, Ellen Niederberger
No abstract text is available yet for this article.
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28379583/b-vitamins-potentiate-acute-morphine-antinociception-and-attenuate-the-development-of-tolerance-to-chronic-morphine-in-mice
#13
Xue-Ting Deng, Yuan Han, Wen-Tao Liu, Xue-Jun Song
Objectives. : Opiate analgesics are the most effective treatments for severe pain, but their clinical utility is often hampered by the development of analgesic tolerance. There are striking similarities between morphine actions and neuropathic pain. We have demonstrated that B vitamins can attenuate neuropathic pain after peripheral nerve injury, sensory neuron inflammation/compression, and transient spinal cord ischemia. Given this similarity, the present study investigated whether B vitamins might be able to modify the antinociceptive effect of morphine as well as morphine tolerance in mice...
March 31, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28378856/involvement-of-galanin-and-galanin-receptor-2-in-nociceptive-modulation-in-anterior-cingulate-cortex-of-normal-rats-and-rats-with-mononeuropathy
#14
Meng-Lin Zhang, Hong-Bo Wang, Feng-Hua Fu, Long-Chuan Yu
The present study was performed to explore the role of galanin and galanin receptor 2 in nociceptive modulation in anterior cingulate cortex (ACC) of normal rats and rats with mononeuropathy. Intra-ACC injection of galanin induced significant increases in hindpaw withdrawal latencies (HWLs) to thermal and mechanical stimulations in both normal rats and rats with mononeuropathy, the increased HWLs were attenuated significantly by intra-ACC injection of galanin receptor 2 antagonist M871, indicating an involvement of galanin receptor 2 in nociceptive modulation in ACC...
April 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28377055/original-endomorphin-1-analogues-exhibit-good-analgesic-effects-with-minimal-implications-for-human-sperm-motility
#15
Yiqing Wang, Xinyi Zhao, Xuelin Gao, Yongan Gan, Ying Liu, Xiaodong Zhao, Junping Hu, Xiaoling Ma, Yanjing Wu, Pengcheng Ma, Xiaolei Liang, Xuehong Zhang
To search a novel analgesic characterizes the effects on human sperm motility as minimal as possible. A new class of endomorphin-1 (EM-1) analogues was synthesized by combining successful chemical modifications including N-terminal guanidino modification, Phe(4) was chlorinated, replaced of l-Pro(2)-Trp(3) by d-Ala(2)-Gly(3) or d-Pro(2)-Gly(3) at position 2 and 3. Their bioactivities were measured by radioligand binding assay, metabolic stability, antinociception activity and sperm motility effects. In radioligand binding assays, analogue GAGP shown a μ-opioid receptor affinity about 17...
March 27, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28374409/antinociceptive-effect-of-natural-and-synthetic-alkamides-involves-trpv1-receptors
#16
Vianey de la Rosa-Lugo, Macdiel Acevedo-Quiroz, Myrna Déciga-Campos, María Yolanda Rios
OBJECTIVE: To establish the role of TRPV1 receptor in the antinociceptive effect of natural alkamides (i.e. affinin, longipinamide A, longipenamide A and longipenamide B) isolated from Heliopsis longipes (A. Gray) S.F. Blake and some related synthetic alkamides (i.e. N-isobutyl-feruloylamide and N-isobutyl-dihydroferuloylamide). METHODS: The orofacial formalin test was used to assess the antinociceptive activity of natural (1-30 μg, orofacial region) and synthetic alkamides (0...
April 4, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28374016/divergent-modulation-of-nociception-by-glutamatergic-and-gabaergic-neuronal-subpopulations-in-the-periaqueductal-gray
#17
Vijay K Samineni, Jose G Grajales-Reyes, Bryan A Copits, Daniel E O'Brien, Sarah L Trigg, Adrian M Gomez, Michael R Bruchas, Robert W Gereau
The ventrolateral periaqueductal gray (vlPAG) constitutes a major descending pain modulatory system and is a crucial site for opioid-induced analgesia. A number of previous studies have demonstrated that glutamate and GABA play critical opposing roles in nociceptive processing in the vlPAG. It has been suggested that glutamatergic neurotransmission exerts antinociceptive effects, whereas GABAergic neurotransmission exert pronociceptive effects on pain transmission, through descending pathways. The inability to exclusively manipulate subpopulations of neurons in the PAG has prevented direct testing of this hypothesis...
March 2017: ENeuro
https://www.readbyqxmd.com/read/28365824/gastroprotective-potential-of-methanolic-extract-and-dimethyl-cardamonin-from-campomanesia-reitziana-fruits-in-mice
#18
Carolina de Oliveira Cabral, Adriana Campos, Luisa Mota da Silva, Thaise Boeing, Sérgio Faloni de Andrade, Valdir Cechinel Filho, Luciane Ângela Nottar Nesello
This study evaluated the gastroprotective potential of methanolic extract from fruits of Campomanesia reitziana (MECR) and its isolated chalcone dimethyl cardamonin (DMC). The phenolic compound in the extract, and the free radical scavenging activity of MECR and DMC, were quantified. The gastroprotective activity of MECR (30-300 mg/kg, p.o) and DMC (1 and 3 mg/kg, p.o) was determined by ethanol/HCl-induced gastric ulcers in mice. Histological, histochemical, and biochemical analyses were performed in the ulcerated tissue...
April 1, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28363796/structure-constrained-endomorphin-analogs-display-differential-antinociceptive-mechanisms-in-mice-after-spinal-administration
#19
Yuan Wang, Jingjing Zhou, Xin Liu, Long Zhao, Zhaojuan Wang, Xianghui Zhang, Kezhou Wang, Linqing Wang, Rui Wang
We previously reported a series of novel endomorphin analogs with unnatural amino acid modifications. These analogs display good binding affinity and functional activity toward the μ opioid receptor (MOP). In the present study, we further investigated the spinal antinociceptive activity of these compounds. The analogs were potent in several nociceptive models. Opioid antagonists and antibodies against several endogenous opioid peptides were used to determine the mechanisms of action of these peptides. Intrathecal pretreatment with naloxone and β-funaltrexamine (β-FNA) effectively inhibited analog-induced analgesia, demonstrating that activity of the analogs is regulated primarily through MOP...
March 29, 2017: Peptides
https://www.readbyqxmd.com/read/28361827/comparative-antinociceptive-effect-of-arachidonylcyclopropylamide-a-cannabinoid-1-receptor-agonist-lignocaine-a-local-anaesthetic-agent-following-direct-intrawound-administration-in-rats
#20
Rahul Kumar, Pranav Prasoon, Mayank Gautam, Subrata Basu Ray
BACKGROUND & OBJECTIVES: Treatment of inflammatory pain with opioids is accompanied by unpleasant and, at times, life-threatening side effects.Cannabis produces antinociception as well as psychotropic effects. It was hypothesized that peripheral cannabinoid receptors outside the central nervous system could be selectively activated for relief of pain. This study was undertaken to measure the antinociceptive effect of type 1 cannabinoid receptor (CB1r) agonist arachidonylcyclopropylamide (ACPA) in a rat model of inflammatory pain after intrawound administration and the effects were compared with lignocaine...
November 2016: Indian Journal of Medical Research
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