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https://www.readbyqxmd.com/read/27910870/antinociceptive-profile-of-levo-tetrahydropalmatine-in-acute-and-chronic-pain-mice-models-role-of-spinal-sigma-1-receptor
#1
Dong-Wook Kang, Ji-Young Moon, Jae-Gyun Choi, Suk-Yun Kang, Yeonhee Ryu, Jin Bong Park, Jang-Hern Lee, Hyun-Woo Kim
We have recently reported that repeated systemic treatments of extract from Corydalis yanhusuo alleviate neuropathic pain and levo-tetrahydropalmatine (l-THP) is one of active components from Corydalis. We designed this study to investigate antinociceptive effect of l-THP in acute and chronic pain models and related mechanism within the spinal cord. We found that intraperitoneal pretreatment with l-THP significantly inhibited the second phase of formalin-induced pain behavior. In addition, intrathecal as well as intraperitoneal pretreatment with l-THP reduced the mechanical allodynia (MA) induced by direct activation of sigma-1 receptor (Sig-1)...
December 2, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27906750/role-of-orexin-2-and-cb1-receptors-within-the-periaqueductal-gray-matter-in-lateral-hypothalamic-induced-antinociception-in-rats
#2
Mohammad-Hossein Esmaeili, Zahra Reisi, Somayeh Ezzatpanah, Abbas Haghparast
Orexin plays an important role in pain modulation. Orexin-1 and orexin-2 receptors (Ox1r and Ox2r) are found at high density in the ventrolateral periaqueductal gray matter (vlPAG). Our previous study showed that chemical stimulation of the lateral hypothalamus with carbachol induces antinociception in the tail-flick test, a model of acute pain, and Ox1r-mediated antinociception in the vlPAG is modulated by the activity of vlPAG CB1 receptors. In the current study, TCS OX2 29, an Ox2r antagonist (5, 15, 50, 150, and 500 nmol/l), was microinjected into the vlPAG 5 min before the administration of carbachol (125 nmol/l)...
November 30, 2016: Behavioural Pharmacology
https://www.readbyqxmd.com/read/27903642/behavioral-characterization-of-kappa-opioid-receptor-agonist-spiradoline-and-cannabinoid-receptor-agonist-cp55940-mixtures-in-rats
#3
Vanessa Minervini, Sujata S Dahal, Charles France
Pain is a significant clinical problem and there is a need for more effective treatments with reduced adverse effects that currently limit the use of mu opioid receptor agonists. Synthetic kappa opioid receptor agonists have no abuse liability and well-documented antinociceptive effects; however, adverse effects (diuresis, dysphoria) preclude their use in the clinic. Combining kappa opioids with non-opioid drugs (cannabinoid receptor agonists) allows for smaller doses of each drug to produce antinociception...
November 30, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27900354/dataset-of-botulinum-toxin-a-influence-on-interleukins-under-neuropathy
#4
Magdalena Zychowska, Ewelina Rojewska, Wioletta Makuch, Siro Luvisetto, Flaminia Pavone, Sara Marinelli, Barbara Przewlocka, Joanna Mika
Our data show that botulinum toxin A (BoNT/A) didn't influence motor functions in naïve and CCI-exposed rats, but diminished the neuropathic pain-related behavior. The results indicate that BoNT/A administration diminished the spinal Iba-1 positive cells activation and, in parallel, downregulated IL-1beta. Moreover, we observed that in DRG the protein level of pronociceptive factors (IL-1beta and IL-18) decreased and antinociceptive (IL-10 and IL-1RA) factors increased. Additionally, our behavioral analysis shows that chronic minocycline treatment together with a single BoNT/A injection in CCI-exposed rats has beneficial analgesic effects (M...
December 2016: Data in Brief
https://www.readbyqxmd.com/read/27899527/biased-agonists-of-the-kappa-opioid-receptor-suppress-pain-and-itch-without-causing-sedation-or-dysphoria
#5
Tarsis F Brust, Jenny Morgenweck, Susy A Kim, Jamie H Rose, Jason L Locke, Cullen L Schmid, Lei Zhou, Edward L Stahl, Michael D Cameron, Sarah M Scarry, Jeffrey Aubé, Sara R Jones, Thomas J Martin, Laura M Bohn
Agonists targeting the kappa opioid receptor (KOR) have been promising therapeutic candidates because of their efficacy for treating intractable itch and relieving pain. Unlike typical opioid narcotics, KOR agonists do not produce euphoria or lead to respiratory suppression or overdose. However, they do produce dysphoria and sedation, side effects that have precluded their clinical development as therapeutics. KOR signaling can be fine-tuned to preferentially activate certain pathways over others, such that agonists can bias signaling so that the receptor signals through G proteins rather than other effectors such as βarrestin2...
November 29, 2016: Science Signaling
https://www.readbyqxmd.com/read/27899254/thalidomide-attenuates-the-development-and-expression-of-antinociceptive-tolerance-to-%C3%AE-opioid-agonist-morphine-through-l-arginine-inos-and-nitric-oxide-pathway
#6
Muhammad Imran Khan, Sattar Ostadhadi, Faiza Mumtaz, Majid Momeny, Farima Moghaddaskho, Mahsa Hassanipour, Shahram Ejtemaei-Mehr, Ahmad Reza Dehpour
Morphine is a μ-opioid analgesic drug which is used in the treatment and management of chronic pain. However, due to development of antinociceptive tolerance its clinical use is limited. Thalidomide is an old glutamic acid derivative which recently reemerged because of its potential to counteract a number of disorders including neurodegenerative disorders. The potential underlying mechanisms and effects of thalidomide on morphine-induced antinociceptive tolerance is still elusive. Hence, the present study was designed to explore the effect of thalidomide on the development and expression of morphine antinociceptive tolerance targeting l-arginine-nitric oxide (NO) pathway in mice and T98G human glioblastoma cell line...
November 26, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27899097/antinociception-of-petroleum-ether-fraction-derived-from-crude-methanol-extract-of-melastoma-malabathricum-leaves-and-its-possible-mechanisms-of-action-in-animal-models
#7
Z A Zakaria, E S Jaios, M H Omar, S Abd Rahman, S S A Hamid, S M Ching, L K Teh, M Z Salleh, S Deny, M Taher
BACKGROUND: Melastoma malabathricum L. (family Melastomaceae) has been traditionally used as remedies against various ailments including those related to pain. The methanol extract of M. malabathricum leaves has been proven to show antinociceptive activity. Thus, the present study aimed to determine the most effective fraction among the petroleum ether- (PEMM), ethyl acetate- (EAMM) and aqueous- (AQMM) fractions obtained through successive fractionation of crude, dried methanol extract of M...
November 29, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27890817/sec-butylpropylacetamide-spd-a-new-amide-derivative-of-valproic-acid-for-the-treatment-of-neuropathic-and-inflammatory-pain
#8
Dan Kaufmann, Peter J West, Misty D Smith, Boris Yagen, Meir Bialer, Marshall Devor, H Steve White, K C Brennan
Chronic pain is a multifactorial disease comprised of both inflammatory and neuropathic components that affect ∼20% of the world's population. sec-Butylpropylacetamide (SPD) is a novel amide analogue of valproic acid (VPA) previously shown to possess a broad spectrum of anticonvulsant activity. In this study we defined the pharmacokinetic parameters of SPD in rat and mouse, and then evaluated its antinociceptive potential in neuropathic and acute inflammatory pain models. In the sciatic nerve ligation (SNL) model of neuropathic pain, SPD was equipotent to gabapentin and more potent than its parent compound VPA...
November 24, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27890602/the-endocannabinoid-hydrolysis-inhibitor-sa-57-intrinsic-antinociceptive-effects-augmented-morphine-induced-antinociception-and-attenuated-heroin-seeking-behavior-in-mice
#9
Jenny L Wilkerson, Sudeshna Ghosh, Mohammed Mustafa, Rehab A Abdullah, Micah J Niphakis, Roberto Cabrera, Rafael L Maldonado, Benjamin F Cravatt, Aron H Lichtman
Although opioids are highly efficacious analgesics, their abuse potential and other untoward side effects diminish their therapeutic utility. The addition of non-opioid analgesics offers a promising strategy to reduce required antinociceptive opioid doses that concomitantly reduce opioid-related side effects. Inhibitors of the primary endocannabinoid catabolic enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) show opioid-sparing effects in preclinical models of pain. As simultaneous inhibition of these enzymes elicits enhanced antinociceptive effects compared with single enzyme inhibition, the present study tested whether the dual FAAH-MAGL inhibitor SA-57 [4-[2-(4-chlorophenyl)ethyl]-1-piperidinecarboxylic acid 2-(methylamino)-2-oxoethyl ester] produces morphine-sparing antinociceptive effects, without major side effects associated with either drug class...
November 24, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27886264/sigma-1-receptor-agonism-promotes-mechanical-allodynia-after-priming-the-nociceptive-system-with-capsaicin
#10
J M Entrena, C Sánchez-Fernández, F R Nieto, R González-Cano, S Yeste, E J Cobos, J M Baeyens
Sigma-1 receptor antagonists promote antinociception in several models of pain, but the effects of sigma-1 agonists on nociception (particularly when the nociceptive system is primed) are not so well characterized; therefore we evaluated the effects of sigma-1 agonists on pain under different experimental conditions. The systemic administration of the selective sigma-1 agonists (+)-pentazocine and PRE-084, as well as the nonselective sigma-1 agonist carbetapentane (used clinically as an antitussive drug), did not alter sensitivity to mechanical stimulation under baseline conditions...
November 25, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27872694/long-term-treatment-by-vitamin-b1-and-reduction-of-serum-proinflammatory-cytokines-hyperalgesia-and-paw-edema-in-adjuvant-induced-arthritis
#11
Jalal Zaringhalam, Akhtar Akbari, Alireza Zali, Homa Manaheji, Vida Nazemian, Mahdi Shadnoush, Somayeh Ezzatpanah
INTRODUCTION: Immune system is involved in the etiology and pathophysiology of inflammation and vitamins are important sources of substances inducing nonspecific immunomodulatory effects. Given the proinflammatory role of cytokines in the inflammation and pain induction, this study aimed to assess the effects of long-term administration of vitamin B1 on the proinflammatory cytokines, edema, and hyperalgesia during the acute and chronic phases of adjuvant-induced arthritis. METHODS: On the first day of study, inflammation was induced by intraplantar injection of complete Freund's adjuvant (CFA) in the hindpaws of rats...
October 2016: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/27872555/effect-of-intravenous-high-dose-vitamin-c-on-postoperative-pain-and-morphine-use-after-laparoscopic-colectomy-a-randomized-controlled-trial
#12
Younghoon Jeon, Jun Seok Park, Suyoung Moon, Jinseok Yeo
Background and Objective. Vitamin C has antioxidant, neuroprotective, and neuromodulating effects. Recently, it showed antinociceptive effect as a result of the antioxidant properties. Therefore, we designed this study to assess the effect of intravenous vitamin C on opiate consumption and pain in patients undergoing laparoscopic colectomy. Methods. A total of 100 patients were enrolled and allocated to receive 50 mg/kg vitamin C or placebo by intravenous infusion immediately after induction of anesthesia...
2016: Pain Research & Management: the Journal of the Canadian Pain Society
https://www.readbyqxmd.com/read/27871910/pharmacological-studies-on-the-nop-and-opioid-receptor-agonist-pwt2-dmt-1-n-ofq-1-13
#13
Maria Camilla Cerlesi, Huiping Ding, Mark F Bird, Norikazu Kiguchi, Federica Ferrari, Davide Malfacini, Anna Rizzi, Chiara Ruzza, David G Lambert, Mei-Chuan Ko, Girolamo Calo, Remo Guerrini
An innovative chemical strategy named peptide welding technology (PWT) has been developed for the facile synthesis of tetrabranched peptides. [Dmt(1)]N/OFQ(1-13)-NH2 acts as a universal agonist for nociceptin/orphanin FQ (N/OFQ) and classical opioid receptors. The present study investigated the pharmacological profile of the PWT derivative of [Dmt(1)]N/OFQ(1-13)NH2 (PWT2-[Dmt(1)]) in several assays in vitro and in vivo after spinal administration in monkeys subjected to the tail withdrawal assay. PWT2-[Dmt(1)] mimicked the effects of [Dmt(1)]N/OFQ(1-13)-NH2 displaying full agonist activity, similar affinity/potency and selectivity at human recombinant N/OFQ (NOP) and opioid receptors in receptor binding, stimulation of [(35)S]GTPγS binding, calcium mobilization in cells expressing chimeric G proteins, and BRET studies for measuring receptor/G-protein and receptor/β-arrestin 2 interaction...
November 19, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27867267/essential-oil-composition-antimicrobial-and-pharmacological-activities-of-lippia-sidoides-cham-verbenaceae-from-s%C3%A3-o-gon%C3%A3-alo-do-abaet%C3%A3-minas-gerais-brazil
#14
Sandra Ribeiro de Morais, Thiago Levi Silva Oliveira, Lanussy Porfiro de Oliveira, Leonice Manrique Faustino Tresvenzol, Edemilson Cardoso da Conceição, Maria Helena Rezende, Tatiana de Sousa Fiuza, Elson Alves Costa, Pedro Henrique Ferri, José Realino de Paula
BACKGROUND: Lippia sidoides (Verbenaceae) is used in Brazilian folk medicine as an antiseptic, and it is usually applied topically on skin, mucous membranes, mouth, and throat, or used for vaginal washings. OBJECTIVES: To analyze the chemical composition of the essential oil from L. sidoides collected in São Gonçalo do Abaeté, Minas Gerais and grown in Hidrolândia, Goiás; to evaluate the antimicrobial activity of the essential oil, crude ethanol extract, and hexane, dichloromethane, ethyl-acetate, and aqueous fractions (AFs); to study the antinociceptive, anti-inflammatory, and central nervous system activities of the crude ethanol extract...
October 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27865771/cholinergic-activation-affects-the-acute-and-chronic-antinociceptive-effects-of-morphine
#15
Kinga Gawel, Ewa Gibula-Bruzda, Marcin Dziedzic, Malgorzata Jenda-Wojtanowska, Marta Marszalek-Grabska, Jerzy Silberring, Jolanta H Kotlinska
Current studies indicate that the cholinergic and opioid systems interact to modulate pain. In the present work, we investigated the influence of the cholinesterase inhibitors, donepezil (0.5; 1 or 3mg/kg, i.p.) and rivastigmine (0.03; 0.5 or 1mg/kg, i.p.), on the acute antinociceptive effects of morphine (5mg/kg, i.p.) in the hot plate test in mice. Herein, both inhibitors were found to enhance and prolong the analgesic effects of morphine without affecting latencies themselves. In an extension of this work, we determined which cholinergic receptors subtype mediates the enhancement of analgesic effects of morphine, following inhibition of cholinesterases...
November 16, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27864110/antinociceptive-activity-and-mechanism-of-action-of-hydroalcoholic-extract-and-dichloromethane-fraction-of-amphilophium-crucigerum-seeds-in-mice
#16
Samira Dal Toé De Prá, Paula Ronsani Ferro, Alessandra Marcon Milioli, Flávia Karine Rigo, Orlando Justo Chipindo, Camila Camponogara, Rosana Casoti, Melânia Palermo Manfron, Sara Marchesan de Oliveira, Juliano Ferreira, Gabriela Trevisan
ETHNOPHARMACOLOGICAL RELEVANCE: The medicinal plant generally known as monkey's comb (Amphilophium crucigerum) has been popularly described for the treatment of neuropathic and inflammatory pain, specially seeds preparations. AIM OF THE STUDY: The goal of the present study was to evaluate the antinociceptive effect of the crude extract (Crd) and dichloromethane fraction (Dcm) of A. crucigerum seeds, and investigate the involvement of transient receptor potential vanilloid 1 (TRPV1) receptor in this effect...
November 15, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27862022/binge-ethanol-consumption-increases-inflammatory-pain-responses-and-mechanical-and-cold-sensitivity-tigecycline-treatment-efficacy-shows-sex-differences
#17
Susan E Bergeson, Henry Blanton, Joseph M Martinez, David C Curtis, Caitlyn Sherfey, Brandon Seegmiller, Patrick C Marquardt, Jessica A Groot, Clayton L Allison, Christian Bezboruah, Josée Guindon
BACKGROUND: Physicians have long reported that patients with chronic pain show higher tendencies for alcohol use disorder (AUD), and AUD patients appear to have higher pain sensitivities. The goal of this study was to test 2 hypotheses: (i) binge alcohol consumption increases inflammatory pain and mechanical and cold sensitivities; and (ii) tigecycline is an effective treatment for alcohol-mediated-increased pain behaviors and sensitivities. Both female and male mice were used to test the additional hypothesis that important sex differences in the ethanol (EtOH)-related traits would be seen...
December 2016: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/27855689/metformin-reduces-morphine-tolerance-by-inhibiting-microglial-mediated-neuroinflammation
#18
Yinbing Pan, Xiaodi Sun, Lai Jiang, Liang Hu, Hong Kong, Yuan Han, Cheng Qian, Chao Song, Yanning Qian, Wentao Liu
BACKGROUND: Tolerance seriously impedes the application of morphine in clinical medicine. Thus, it is necessary to investigate the exact mechanisms and efficient treatment. Microglial activation and neuroinflammation in the spinal cord are thought to play pivotal roles on the genesis and maintaining of morphine tolerance. Activation of adenosine monophosphate-activated kinase (AMPK) has been associated with the inhibition of inflammatory nociception. Metformin, a biguanide class of antidiabetic drugs and activator of AMPK, has a potential anti-inflammatory effect...
November 17, 2016: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/27847477/reverse-of-acute-and-chronic-morphine-tolerance-by-lithocholic-acid-via-down-regulating-ugt2b7
#19
Zizhao Yang, Li Li, Haihong Hu, Mingcheng Xu, Jingkai Gu, Zaijie Jim Wang, Lushan Yu, Su Zeng
Lithocholic acid (LCA) deposited in human livers always induces drastic pains which need analgesic drug, like morphine to release. Our research showed that LCA can effectively inhibit uridine 5'-diphospho-glucuronosyltransferase 2B7 (UGT2B7) in morphine tolerance-like human normal liver cells, HL-7702, then increase μ-opioid receptor (MOR) and calcium-calmodulin dependent protein kinase IIα (CaMKIIα) expression. In vivo assay, UGT2B7 was significantly repressed in the livers of acute or chronic morphine tolerance mice pretreated with LCA (10, 50, and 100 mg/kg, p...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27843474/electroacupuncture-pretreatment-at-gb20-exerts-antinociceptive-effects-via-peripheral-and-central-serotonin-mechanism-in-conscious-migraine-rats
#20
Lu Liu, Pei Pei, Luo-Peng Zhao, Zheng-Yang Qu, Yu-Pu Zhu, Lin-Peng Wang
Background. While electroacupuncture (EA) pretreatment in migraine has been found to attenuate pain and frequencies of attacks, the underlying mechanism of its antinociceptive effect remains poorly understood. Emerging evidence suggests that the serotonin system may be involved in migraine pathophysiology. Method. Forty male Sprague-Dawley rats were randomly assigned to Control, Model, EA, and sham acupuncture (SA) groups. HomeCageScan was used to measure the effects on spontaneous nociceptive behaviors. Radioimmunoassay and high-performance liquid chromatography were used to evaluate the expression of 5-hydroxytryptamine (HT) in the plasma and three-key structure of the descending pain modulatory system...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
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