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https://www.readbyqxmd.com/read/29333042/gas-chromatography-mass-spectrometry-profiling-in-methanolic-and-ethyl-acetate-root-and-stem-extract-of-corbichonia-decumbens-forssk-exell-from-thar-desert-of-rajasthan-india
#1
Sunita Arora, Manju Saini
Background: Corbichonia decumbens (Forssk.) Exell (Molluginaceae), recently has moved to Lophiocarpaceae as per angiospermic plant group (APG) III system, is an annual or short-lived, dwarf, glabrous subshrub, prefers to grow on rocky places and on sand-stones in dry, hot areas of Rajasthan. This is the potential plant with medicinal properties. Vegetative organs under study show antioxidant, anti-inflammatory, antiulcer, antimicrobial, and antinociception activity. Objective: This study was carried out to identify the phytoconstituents present in the methanolic and ethyl-acetate extract of root and stem of C...
December 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/29333034/antinociceptive-and-anti-inflammatory-effects-of-triterpenes-from-pluchea-quitoc-dc-aerial-parts
#2
Francisco Alcione Nobre da Silva, Sônia Maria de Farias Freire, Marilene Oliveira da Rocha Borges, Francisco Erivaldo Vidal Barros, Maria da de Sousa, Maria Nilce de Sousa Ribeiro, Giselle Maria Skelding Pinheiro Guilhon, Adolfo Henrique Müller, Antonio Carlos Romão Borges
Background: Pluchea quitoc DC. (Asteraceae), a medicinal plant known as "quitoco," "caculucage," "tabacarana" and "madre-cravo," is indicated for inflammatory conditions such as bronchitis, arthritis, and inflammation in the uterus and digestive system. Objective: This study evaluated the analgesic and anti-inflammatory activities of the triterpenes compounds obtained from P. quitoc aerial parts. Materials and Methods: The triterpenes compounds β-amyrin, taraxasterol and pseudo-taraxasterol in a mixture (T); β-amyrin, taraxasterol and pseudo-taraxasterol acetates in a mixture (Ta); β-amyrin, taraxasterol, pseudo-taraxasterol acetates in a mixture with β-amyrin, taraxasterol and pseudo-taraxasterol myristates (Tafe) were analyzed in the models of nociception and inflammation...
December 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/29332567/nociceptin-orphanin-fq-peptide-nop-receptor-modulators-an-update-in-structure-activity-relationships
#3
Carlo Mustazza, Stefano Pieretti, Francesca Marzoli
Nociceptin /Orphanin FQ Peptide" receptor (NOPr) is a G-protein-coupled receptor with the nociceptin/orphanin FQ peptide (N/OFQ) as endogenous agonist. It is expressed in the nervous system as well as in some non-neural tissues. Its activation has pronociceptive effect at the supraspinal level, whereas at the spinal level it produces nociceptive effects at low doses and antinociceptive effects at higher doses. NOPr is also involved in mood and blood pressure regulation, immunoregulation, airway constriction, feeding, urination, bowel motility, learning and memory...
January 10, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29331791/magnesium-sulfate-reduces-formalin-induced-orofacial-pain-in-rats-with-normal-magnesium-serum-levels
#4
Dragana P Srebro, Sonja M Vučković, Ivan S Dožić, Branko S Dožić, Katarina R Savić Vujović, Aleksandar P Milovanović, Branislav V Karadžić, Milica Š Prostran
BACKGROUND: In humans, orofacial pain has a high prevalence and is often difficult to treat. Magnesium is an essential element in biological a system which controls the activity of many ion channels, neurotransmitters and enzymes. Magnesium produces an antinociceptive effect in neuropathic pain, while in inflammatory pain results are not consistent. We examined the effects of magnesium sulfate using the rat orofacial formalin test, a model of trigeminal pain. METHODS: Male Wistar rats were injected with 1...
August 31, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29330156/application-of-receptor-theory-to-the-design-and-use-of-fixed-proportion-mu-opioid-agonist-and-antagonist-mixtures-in-rhesus-monkeys
#5
Jeremy C Cornelissen, Samuel Obeng, Kenner C Rice, Yan Zhang, S Stevens Negus, Matthew Banks
Receptor theory predicts that fixed-proportion mixtures of a competitive, reversible agonist (e.g. fentanyl) and antagonist (e.g. naltrexone) at a common receptor (e.g. mu opioid receptors; MOR) will result in antagonist proportion-dependent decreases in apparent efficacy of the mixtures and downward shifts in mixture dose-effect functions. The present study tested this hypothesis by evaluating behavioral effects of fixed-proportion fentanyl/naltrexone mixtures in a warm-water tail-withdrawal procedure in rhesus monkeys (n=4)...
January 12, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29327283/persea-americana-mill-crude-extract-exhibits-antinociceptive-effect-on-uvb-radiation-induced-skin-injury-in-mice
#6
Viviane C K N Deuschle, Indiara Brusco, Mariana Piana, Henrique Faccin, Leandro Machado de Carvalho, Sara Marchesan Oliveira, Carine Viana
Persea americana, popularly known as avocado, has been empirically used as analgesic and anti-inflammatory including in the skin disorder treatment. Species of the genus Persea also show a photoprotective effect against UVB radiation. We investigated the antinociceptive and anti-inflammatory effects from a topical formulation containing the P. americana leaf extract in a UVB irradiation-induced burn model in mice and performed a gel-formulation stability study. The antinociceptive and anti-inflammatory effect was evaluated through mechanical allodynia, paw oedema, and inflammatory cell infiltration...
January 11, 2018: Inflammopharmacology
https://www.readbyqxmd.com/read/29324503/%C3%AE-asarone-alleviated-chronic-constriction-injury-induced-neuropathic-pain-through-inhibition-of-spinal-endoplasmic-reticulum-stress-in-an-liver-x-receptor-dependent-manner
#7
Yulong Gui, Aiyuan Li, Jie Zhang, Guan Li, Xia Ruan, Qulian Guo, Wangyuan Zou
BACKGROUND: Neuropathic pain is an intractable and complex disease. Recent studies have shown a close relationship between endoplasmic reticulum (ER) stress and neuropathic pain. Here, we investigated the effect of α-asarone, an ER stress inhibitor, on chronic constriction injury (CCI)-induced neuropathic pain. METHODS: Two parts were included in this study. In part 1, rats were assigned to 7 groups: the sham group, the sham + α-asarone 20 mg/kg group, the CCI group, the CCI + vehicle group, the CCI + α-asarone 5 mg/kg group, the CCI + α-asarone 10 mg/kg group, and the CCI + α-asarone 20 mg/kg group...
January 9, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29322264/cerebral-gray-matter-volume-in-patients-with-chronic-migraine-correlations-with-clinical-features
#8
Gianluca Coppola, Barbara Petolicchio, Antonio Di Renzo, Emanuele Tinelli, Cherubino Di Lorenzo, Vincenzo Parisi, Mariano Serrao, Valentina Calistri, Stefano Tardioli, Gaia Cartocci, Anna Ambrosini, Francesca Caramia, Vittorio Di Piero, Francesco Pierelli
BACKGROUND: To date, few MRI studies have been performed in patients affected by chronic migraine (CM), especially in those without medication overuse. Here, we performed magnetic resonance imaging (MRI) voxel-based morphometry (VBM) analyses to investigate the gray matter (GM) volume of the whole brain in patients affected by CM. Our aim was to investigate whether fluctuations in the GM volumes were related to the clinical features of CM. METHODS: Twenty untreated patients with CM without a past medical history of medication overuse underwent 3-Tesla MRI scans and were compared to a group of 20 healthy controls (HCs)...
December 8, 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/29317149/phenylquinoline-transient-receptor-potential-vanilloid-1-antagonists-for-the-treatment-of-pain-discovery-of-1-2-phenylquinoline-4-carbonyl-n-4-trifluoromethyl-phenyl-pyrrolidine-3-carboxamide
#9
Chen Liao, Yan Liu, Chunxia Liu, Jiaqi Zhou, Huilan Li, Nasi Wang, Jieming Li, Taiyu Liu, Hesham Ghaleb, Wenlong Huang, Hai Qian
Reported herein is the design, synthesis, and pharmacologic characterization of a class of TRPV1 antagonists constructed on a phenylquinoline platform that evolved from Cinchophen lead. This design composes three sections: a phenylquinoline headgroup attached to an aliphatic carboxamides, which is tethered at a phenyl tail group. Optimization of this design led to the identification of 37, comprising a pyrrolidine linker and a trifluoromethyl-phenyl tail. In the TRPV1 functional assay, using cells expressed hTRPV1, 37 antagonized capsaicin-induced Ca2+ influx, with an IC50 value of 10...
December 30, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29315308/mac-sparing-effect-of-nitrous-oxide-in-sevoflurane-anesthetized-sheep-and-its-reversal-with-systemic-atipamezole-administration
#10
Lauren Duffee, Nicolò Columbano, Antonio Scanu, Valentino Melosu, Giovanni Mario Careddu, Giovanni Sotgiu, Bernd Driessen
INTRODUCTION: Nitrous oxide (N2O) is an anesthetic gas with antinociceptive properties and reduces the minimum alveolar concentration (MAC) for volatile anesthetic agents, potentially through mechanisms involving central alpha2-adrenoceptors. We hypothesized that 70% N2O in the inspired gas will significantly reduce the MAC of sevoflurane (MACSEVO) in sheep, and that this effect can be reversed by systemic atipamezole. MATERIALS AND METHODS: Animals were initially anesthetized with SEVO in oxygen (O2) and exposed to an electrical current as supramaximal noxious stimulus in order to determine MACSEVO (in duplicates)...
2018: PloS One
https://www.readbyqxmd.com/read/29314177/assessment-of-the-antinociceptive-and-ulcerogenic-activity-of-the-tapentadol-diclofenac-combination-in-rodents
#11
Juan R Zapata-Morales, Ángel J Alonso-Castro, Vinicio Granado-Soto, Sergio Sánchez-Enriquez, Mario A Isiordia-Espinoza
Preclinical Research & Development The objective of the present study was to evaluate the tapentadol-diclofenac combination in three dose-ratios in the mouse acetic acid-induced visceral pain and their ulcerogenic activity on the stomachal mucous. Dose-response curves were generated for tapentadol, diclofenac, and their combination in the acetic acid-induced writhing test in mice. Moreover, the stomachs of animals were surgically removal and gastrointestinal ulcerogenic action of the combination was assessed...
January 3, 2018: Drug Development Research
https://www.readbyqxmd.com/read/29311537/secreted-phospholipases-a%C3%A2-from-animal-venoms-in-pain-and-analgesia
#12
REVIEW
Vanessa O Zambelli, Gisele Picolo, Carlos A H Fernandes, Marcos R M Fontes, Yara Cury
Animal venoms comprise a complex mixture of components that affect several biological systems. Based on the high selectivity for their molecular targets, these components are also a rich source of potential therapeutic agents. Among the main components of animal venoms are the secreted phospholipases A₂ (sPLA₂s). These PLA₂ belong to distinct PLA₂s groups. For example, snake venom sPLA₂s from Elapidae and Viperidae families, the most important families when considering envenomation, belong, respectively, to the IA and IIA/IIB groups, whereas bee venom PLA₂ belongs to group III of sPLA₂s...
December 19, 2017: Toxins
https://www.readbyqxmd.com/read/29311110/long-lasting-in-vivo-effects-of-the-cannabinoid-cb1-antagonist-am6538
#13
Carol A Paronis, Girish R Chopda, Kiran Vemuri, Ani S Zakarian, Alexandros Makriyannis, Jack Bergman
AM6538 is a cannabinoid antagonist that binds CB1 receptors expressed in HEK-293 cells in a wash-resistant manner. The effects of AM6538 in live animals has not previously been established. We characterized the antagonist effects of AM6538 in male mice, using a warm-water tail-withdrawal assay, and in male squirrel monkeys trained to discriminate the CB1 agonist AM4054 from vehicle. The cannabinoid agonists WIN 55,212, Δ9-tetrahydrocannabinol (THC), and AM4054 all produced 100% maximum possible antinociceptive effects in mice following vehicle pretreatment...
January 8, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29310667/wwl70-protects-against-chronic-constriction-injury-induced-neuropathic-pain-in-mice-by-cannabinoid-receptor-independent-mechanisms
#14
Jie Wen, Melissa Jones, Mikiei Tanaka, Prabhuanand Selvaraj, Aviva J Symes, Brian Cox, Yumin Zhang
BACKGROUND: Targeting the endocannabinoid system has emerged as an effective strategy for the treatment of inflammatory and neurological diseases. Unlike the inhibition of the principal 2-arachidonyl glycerol (2-AG) hydrolytic enzyme monoacylglycerol lipase (MAGL), which leads to 2-AG overload and cannabinoid receptor desensitization, selective inhibition of the minor 2-AG hydrolytic enzyme alpha, beta-hydrolase domain 6 (ABHD6) can provide therapeutic benefits without producing cannabimimetic side effects...
January 8, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29304875/antinociceptive-tolerance-to-nsaids-in-the-anterior-cingulate-cortex-is-mediated-via-endogenous-opioid-mechanism
#15
Nana Tsiklauri, Natia Pirkulashvili, Ivliane Nozadze, Marina Nebieridze, Gulnaz Gurtskaia, Elene Abzianidze, Merab G Tsagareli
BACKGROUND: In the past decade several studies have reported that in some brain areas, particularly, in the midbrain periaqueductal gray matter, rostral ventro-medial medulla, central nucleus of amygdala, nucleus raphe magnus, and dorsal hippocampus, microinjections of non-steroidal anti-inflammatory drugs (NSAIDs) induce antinociception with distinct development of tolerance. Given this evidence, in this study we investigated the development of tolerance to the analgesic effects of NSAIDs diclofenac, ketorolac and xefocam microinjected into the rostral part of anterior cingulate cortex (ACC) in rats...
January 6, 2018: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29304162/adrenergic-receptors-inhibit-trpv1-activity-in-the-dorsal-root-ganglion-neurons-of-rats
#16
Yumi Matsushita, Miki Manabe, Naoki Kitamura, Izumi Shibuya
Transient receptor potential vanilloid type 1 (TRPV1) is a polymodal receptor channel that responds to multiple types of stimuli, such as heat, acid, mechanical pressure and some vanilloids. Capsaicin is the most commonly used vanilloid to stimulate TRPV1. TRPV1 channels are expressed in dorsal root ganglion neurons that extend to Aδ- and C-fibers and have a role in the transduction of noxious inputs to the skin into the electrical signals of the sensory nerve. Although noradrenergic nervous systems, including the descending antinociceptive system and the sympathetic nervous system, are known to modulate pain sensation, the functional association between TRPV1 and noradrenaline in primary sensory neurons has rarely been examined...
2018: PloS One
https://www.readbyqxmd.com/read/29303776/evaluation-of-morning-glory-jacquemontia-tamnifolia-l-griseb-leaves-for-antioxidant-antinociceptive-anticoagulant-and-cytotoxic-activities
#17
Mohammad Shahadat Hossain, A S M Ali Reza, Md Masudur Rahaman, Mst Samima Nasrin, Mohammed Rasib Uddin Rahat, Md Rabiul Islam, Md Josim Uddin, Md Atiar Rahman
BACKGROUND: The present study was planned to investigate the phytochemical, antioxidant, antinociceptive, anticoagulant and cytotoxic activities of the Jacquemontia tamnifolia (L.) Griseb leaf methanol extract (MExJT) in the laboratory using both in vitro and in vivo methods. METHODS: Phytochemical values, namely, total phenolic and flavonoid contents, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging effect and FeCl3 reducing power effects, were studied by established methods...
January 5, 2018: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/29299193/quetiapine-reverses-paclitaxel-induced-neuropathic-pain-in-mice-role-of-alpha2-adrenergic-receptors
#18
Alireza Abed, Mohammad Javad Khoshnoud, Mehdi Taghian, Mahbubeh Aliasgharzadeh, Azam Mesdaghinia
Objectives: Paclitaxel-induced peripheral neuropathy is a common adverse effect of cancer chemo -therapy. This neuropathy has a profound impact on quality of life and patient's survival. Preventing and treating paclitaxel-induced peripheral neuropathy is a major concern. First- and second-generation antipsychotics have shown analgesic effects both in humans and animals. Quetiapine is a novel atypical antipsychotic with low propensity to induce extrapyramidal or hyperprolactinemia side effects...
November 2017: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/29296562/the-potential-for-interaction-of-tolbutamide-with-pomegranate-juice-against-diabetic-induced-complications-in-rats
#19
Manodeep Chakraborty, Mohammed Gulzar Ahmed, Ananya Bhattacharjee
Background: Pomegranate can inhibit cytochrome P450 (CYP) 2C9 activity, which is largely responsible for the metabolism of sulfonylureas. The present study was undertaken to evaluate the pharmacokinetic and pharmacodynamic interaction of pomegranate and tolbutamide (TOL) against diabetic-induced complications. Methods: Diabetes was induced via administration of alloxan (150 mg/kg, intraperitoneally). Rats (n = 8) were treated with pomegranate juice (PJ) [3 mL/animal, per os (p...
December 2017: Integrative Medicine Research
https://www.readbyqxmd.com/read/29295695/anticancer-properties-of-essential-oils-an-overview
#20
Milene Aparecida Andrade, Mariana Aparecida Braga, Pedro Henrique Souza Cesar, Marcus Vinicius Cardoso Trento, Mariana Araujo Esposito, Lucilene Fernandes Silva
BACKGROUND: Essential oils are complex mixtures of low molecular weight compounds extracted from plants. Their main constituents are terpenes and phenylpropanoids, which are responsible for their biological and pharmaceutical properties, such as insecticidal, parasiticidal, antimicrobial, antioxidant, anti-inflammatory, analgesic, antinociceptive, anticarcinogenic, and antitumor properties. Cancer is a complex genetic disease considered as a serious public health problem worldwide, accounting for more than 8 million deaths annually...
January 1, 2018: Current Cancer Drug Targets
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