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https://www.readbyqxmd.com/read/28821921/anti-nociceptive-effect-of-stigmasterol-in-mouse-models-of-acute-and-chronic-pain
#1
Cristiani Isabel Banderó Walker, Sara Marchesan Oliveira, Raquel Tonello, Mateus Fortes Rossato, Evelyne da Silva Brum, Juliano Ferreira, Gabriela Trevisan
Stigmasterol is a common sterol found in plants, but the anti-nociceptive effect of this compound and its mechanism of action are not fully explored. Thus, in the present study, the anti-nociceptive effect of stigmasterol was investigated in acute and chronic models of pain and its mechanism of action. We used adult male albino Swiss mice (25-35 g) to observe the anti-nociceptive effect of stigmasterol in acetic-acid writhing test or in complete Freund's adjuvant injection, surgical incision in hind paw, or partial sciatic nerve ligation...
August 18, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28818835/src-dependent-phosphorylation-of-%C3%AE-opioid-receptor-at-tyr-336-modulates-opiate-withdrawal
#2
Lei Zhang, Cherkaouia Kibaly, Yu-Jun Wang, Chi Xu, Kyu Young Song, Patrick W McGarrah, Horace H Loh, Jing-Gen Liu, Ping-Yee Law
Opiate withdrawal/negative reinforcement has been implicated as one of the mechanisms for the progression from impulsive to compulsive drug use. Increase in the intracellular cAMP level and protein kinase A (PKA) activities within the neurocircuitry of addiction has been a leading hypothesis for opiate addiction. This increase requires the phosphorylation of μ-opioid receptor (MOR) at Tyr(336) by Src after prolonged opiate treatment in vitro Here, we report that the Src-mediated MOR phosphorylation at Tyr(336) is a prerequisite for opiate withdrawal in mice...
August 17, 2017: EMBO Molecular Medicine
https://www.readbyqxmd.com/read/28812595/compulsive-like-sufentanil-vapor-self-administration-in-the-rat
#3
Janaina Cm Vendruscolo, Brendan J Tunstall, Stephanie A Carmack, Brooke E Schmeichel, Emily G Lowery-Gionta, Maury Cole, Olivier George, Sophia Vandewater, Michael Taffe, George F Koob, Leandro F Vendruscolo
Opioid misuse is at historically high levels in the United States, with inhalation (ie, smoking, and vaping) being one of the most common routes of consumption. We developed and validated a novel preclinical model of opioid self-administration by inhalation that does not require surgery and reliably produces somatic and motivational signs of dependence. Rats were trained to perform an operant response (nosepoke) to receive 10 s of vaporized sufentanil, a potent opioid, in 2 h daily sessions. Rats readily and concentration-dependently self-administered vaporized sufentanil...
August 16, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28811779/effect-of-exercise-and-morphine-on-psychological-and-physical-dependencies-bdnf-and-trkb-gene-expression-in-rat-s-hippocampus
#4
Mojtaba Naghshvarian, Mohammad-Reza Zarrindast, Shahram Ejtemaei Mehr, Mohammad Mehdi Ommati, Seyedeh Fatemeh Sajjadi
OBJECTIVES: To compare the effect of exercise and morphine on abstinence syndrome and hippocampal gene expression in rat model. METHODS: Thirty adult male rats were exposed to voluntary wheel exercise (low, medium, high) for 28 days. The subjects entered Conditioned Place Preference (CPP) apparatus and experienced morphine (low, medium, high) CPP and followed by naloxone test. Correlation between exercise level, morphine injection, concurrent morphine administration and exercise with morphine CPP, BDNF and TrkB genes was determined...
May 2017: Pakistan Journal of Medical Sciences Quarterly
https://www.readbyqxmd.com/read/28807904/no-clinically-relevant-drug-drug-interactions-between-methadone-or-buprenorphine-naloxone-and-anti-viral-combination-glecaprevir-and-pibrentasvir
#5
Matthew Kosloski, Weihan Zhao, Armen Asatryan, Jens Kort, Pierre Geoffroy, Wei Liu
The combination of glecaprevir (formerly ABT-493), a nonstructural (NS) protein 3/4A protease inhibitor, and pibrentasvir (formerly ABT-530), a NS5A protein inhibitor, is being developed as treatment for HCV genotype 1-6 infection. The pharmacokinetics, pharmacodynamics, safety, and tolerability of methadone or buprenorphine/naloxone when coadministered with the glecaprevir and pibrentasvir combination in HCV-negative subjects on stable opioid maintenance therapy were investigated in a Phase 1, single-center, two-arm, multiple-dose, open-label sequential study...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28807672/pharmacological-characterization-of-novel-synthetic-opioids-nso-found-in-the-recreational-drug-marketplace
#6
REVIEW
Michael H Baumann, Susruta Majumdar, Valerie Le Rouzic, Amanda Hunkele, Rajendra Uprety, Xi Ping Huang, Jin Xu, Bryan L Roth, Ying-Xian Pan, Gavril W Pasternak
Novel synthetic opioids (NSO) are increasingly encountered in illicit heroin and counterfeit pain pills. Many NSO are resurrected from older biomedical literature or patent applications, so limited information is available about their biological effects. Here we examined the pharmacology of three structurally-distinct NSO found in the recreational drug market: N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylbutyramide (butyrylfentanyl), 3,4-dichloro-N-[(1R,2R)-2-(dimethylamino)cyclohexyl]-N-methylbenzamide (U-47700) and 1-cyclohexyl-4-(1,2-diphenylethyl)piperazine (MT-45)...
August 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28805471/prolonged-release-oxycodone-and-naloxone-treatment-counteracts-opioid-induced-constipation-in-patients-with-severe-pain-compared-to-previous-analgesic-treatment
#7
Gineke Koopmans-Klein, Joeri Van Op den Bosch, Yvonne van Megen, Hans Prenen, Frank Huygen, Isabelle Mancini
OBJECTIVE: Treatment with prolonged-release oxycodone/naloxone (PR OXN) has been shown to improve opioid induced constipation (OIC) in constipated patients. This publication reports on a real-life observational study investigating the efficacy of PR OXN with regard to bowel function in patients switching to PR OXN from WHO-step 1, step 2 and step 3 opioids. METHODS: Patients with chronic pain experiencing insufficient pain relief and/or unacceptable side effects were switched to PR OXN and monitored in this observational study with respect to efficacy regarding bowel function and efficacy regarding pain relief in comparison with previous analgesic therapy...
August 14, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28794657/repeated-administration-of-mazindol-reduces-spontaneous-pain-related-behaviors-without-modifying-bone-density-and-microarchitecture-in-a-mouse-model-of-complete-freund-s-adjuvant-induced-knee-arthritis
#8
L E Robledo-González, A Martínez-Martínez, V M Vargas-Muñoz, R I Acosta-González, R Plancarte-Sánchez, M Anaya-Reyes, C Fernández Del Valle-Laisequilla, J G Reyes-García, J M Jiménez-Andrade
BACKGROUND: The role of dopaminergic system in the development of rheumatoid arthritis-related pain, a major symptom in this disease, has not been explored. Therefore, the anti-nociceptive effect of mazindol, a dopamine uptake inhibitor, was evaluated in a model of complete Freund's adjuvant (CFA)-induced arthritis. Furthermore, as studies have shown that the dopaminergic system regulates bone metabolism, the effect of mazindol on bone mass and microarchitecture was determined. METHODS: Adult ICR male mice received intra-articular injections of either CFA or saline into the right knee joint every week...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28792650/oral-oxycodone-naloxone-for-pain-control-in-liver-cirrhosis-observational-study-in-patients-with-symptomatic-metastatic-hepatocellular-carcinoma
#9
Francesco Tovoli, Stefania De Lorenzo, Boaz Gedaliahu Samolsky Dekel, Fabio Piscaglia, Francesca Benevento, Giovanni Brandi, Luigi Bolondi
BACKGROUND & AIMS: Pain management in liver cirrhosis is a clinical challenge. Most analgesics are metabolized in the liver and cirrhosis may deeply alter their concentration, favoring the appearance of side effects. We aimed to assess the efficacy and safety of oral prolonged-release association of oxycodone/naloxone tablets (OXN) in the treatment of moderate/severe cancer pain in cirrhotic patients with metastatic hepatocellular carcinoma (HCC). METHODS: We enrolled n=32 HCC patients with moderate/severe cancer pain unresponsive to paracetamol alone or associated with codeine or tramadol...
August 9, 2017: Liver International: Official Journal of the International Association for the Study of the Liver
https://www.readbyqxmd.com/read/28780471/neuropathic-pain-attenuating-effects-of-perampanel-in-an-experimental-model-of-chronic-constriction-injury-in-rats
#10
Ravneet Kaur Khangura, Anjana Bali, Gunjanpreet Kaur, Nirmal Singh, Amteshwar Singh Jaggi
The present study explores the pain attenuating effect of perampanel, AMPA receptor antagonist, in chronic constriction injury-induced neuropathic pain. Chronic Constriction Injury was performed by putting four loose ligatures around the sciatic nerve. Pain was assessed by determining mechanical hyperalgesia, cold allodynia and heat hyperalgesia on 7th and 14th day post surgery. Perampanel (3mg and 6mg/kg, p.o.) was administered 30min before pain assessment test on 14th day post-surgery. CCI led to significant development of pain and peak symptoms were observed on 14th day...
August 3, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28772172/naloxone-use-among-overdose-prevention-trainees-in-new-york-city-a-longitudinal-cohort-study
#11
Anne Siegler, Zina Huxley-Reicher, Lara Maldjian, Robyn Jordan, Chloe Oliver, Andrea Jakubowski, Hillary V Kunins
BACKGROUND: Providing naloxone to laypersons who are likely to witness an opioid overdose is now a widespread public health response to the national opioid overdose epidemic. Estimating the proportion of individuals who use naloxone can define its potential impact to reduce overdose deaths at a population level. We determined the proportion of study participants who used naloxone within 12 months following training and factors associated with witnessing overdose and naloxone use. METHODS: We conducted a prospective, observational study of individuals completing overdose prevention training (OPT) between June and September 2013...
July 24, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28767537/addressing-stigma-in-medication-treatment-of-adolescents-with-opioid-use-disorder
#12
Sarah M Bagley, Scott E Hadland, Brittany L Carney, Richard Saitz
: In September 2016, the American Academic of Pediatrics released a policy statement that adolescents with opioid use disorder should be offered pharmacotherapy with buprenorphine/naloxone, methadone, or naltrexone. In our clinical practice, however, we have encountered the perception among patients, families, and clinicians alike that medications should be used as a last resort. That we should wait until things get worse is a discarded approach. As addiction specialists, it is imperative that we prevent and identify risky use and use disorders, then intervene early and offer timely, evidence-based treatment...
August 1, 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28763627/limb-remote-ischemic-per-conditioning-protects-heart-against-ischemia-reperfusion-injury-through-opioid-system-in-rats
#13
Li Zhang, Hui Guo, Fang Yuan, Zeng-Chao Hong, Yan-Ming Tian, Xiang-Jian Zhang, Yi Zhang
Remote ischemia per-conditioning (RPerC) has been demonstrated to have cardiac protection, but the underlying mechanism remains unclear. This study aimed to investigate the mechanism underlying cardiac protection of RPerC. Adult male Sprague-Dawley rats were used in this study. Cardiac ischemia/reperfusion (I/R) was induced by 30-min occlusion and 3-h reperfusion of left anterior descending coronary artery. RPerC were performed by 5-min occlusion of right femoral artery followed by 5-min reperfusion for three times during cardiac ischemia...
August 1, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28758123/peripheral-antinociception-induced-by-aripiprazole-is-mediated-by-the-opioid-system
#14
Renata Cristina Mendes Ferreira, Ana Flávia Almeida-Santos, Igor Dimitri Gama Duarte, Daniele C Aguiar, Fabricio A Moreira, Thiago Roberto Lima Romero
BACKGROUND: Aripiprazole is an antipsychotic drug used to treat schizophrenia and related disorders. Our previous study showed that this compound also induces antinociceptive effects. The present study aimed to assess the participation of the opioid system in this effect. METHODS: Male Swiss mice were submitted to paw pressure test and hyperalgesia was induced by intraplantar injection of prostaglandin E2 (PGE2, 2 μg). Aripiprazole was injected 10 min before the measurement...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28755985/peripheral-and-central-sites-of-action-for-anti-allodynic-activity-induced-by-the-bifunctional-opioid-npff-receptors-agonist-bn-9-in-inflammatory-pain-model
#15
Run Zhang, Biao Xu, Meng-Na Zhang, Ting Zhang, Zi-Long Wang, Geng Zhao, Guang-Hai Zhao, Ning Li, Quan Fang, Rui Wang
The activation of opioid and neuropeptide FF (NPFF) receptors plays important roles to modulate nociceptive signal in inflammatory pain states. Recently, BN-9 (Tyr-D.Ala-Gly-Phe-Gln-Pro-Gln-Arg-Phe-NH2) was pharmacologically characterized as a novel bifunctional agonist at both opioid and NPFF receptors. In the present study, the anti-allodynic activity and site(s) of action of BN-9 were assessed in a mouse model of carrageenan-induced inflammatory pain. In mice, BN-9 induced a dose-dependent anti-allodinic effect through opioid receptor at supraspinal or spinal level, and this effect was augmented by pretreatment with the NPFF receptor antagonist at the same level...
July 26, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28750553/the-analgesic-and-anti-inflammatory-activity-of-linum-usitatissimum-in-balb-c-mice
#16
Mahmoud Rafieian-Kopaei, Abdollah Shakiba, Mehrnoosh Sedighi, Mahmoud Bahmani
Linum usitatissimum L is traditionally used for relief of pain and inflammation. In this study, the analgesic and anti-inflammatory effects of this plant were evaluated. Xylene test was used for anti-inflammatory evaluation in which 48 mice were randomly designated into 6 groups of 8 each including: control, dexamethasone as positive control (15 mg/kg), and experimental groups (42, 85, 170, and 340 mg/kg, respectively). For analgesic evaluation, 192 mice were randomly designated into 4 sets of 6 groups of 8 mice, including control, morphine as positive control, morphine plus naloxone, experimental groups (200 and 500 mg/kg extract), and extract along with naloxone group, which received 500 mg/kg...
January 1, 2017: Journal of Evidence-based Complementary & Alternative Medicine
https://www.readbyqxmd.com/read/28750193/awareness-possession-and-use-of-take-home-naloxone-among-illicit-drug-users-vancouver-british-columbia-2014-2015
#17
Seonaid Nolan, Jane Buxton, Sabina Dobrer, Huiru Dong, Kanna Hayashi, M J Milloy, Thomas Kerr, Julio Montaner, Evan Wood
OBJECTIVES: Although take-home naloxone (THN) programs are integral in strategies to prevent overdose deaths among opioid users, the uptake of THN among people who use drugs (PWUD) (including non-opioid users) is unknown. The objectives of this study were to determine awareness, possession, and use of THN among PWUD in Vancouver, Canada, and identify barriers to adopting this strategy. METHODS: From December 1, 2014, to May 29, 2015, participants in 2 prospective cohort studies of PWUD in Vancouver completed a standardized questionnaire, which asked about awareness, possession, and use of THN; sociodemographic characteristics; and drug use patterns...
January 1, 2017: Public Health Reports
https://www.readbyqxmd.com/read/28745837/prosecretory-effect-of-loperamide-in-ileal-and-colonic-mucosae-of-mice-displaying-high-or-low-swim-stress-induced-analgesia-associated-with-high-and-low-endogenous-opioid-system-activity
#18
A Wasilewski, A Misicka, M Sacharczuk, J Fichna
BACKGROUND: Irritable bowel syndrome (IBS) is characterized by abdominal pain, bloating, and changes in bowel habit. The aim of this study was to characterize the effect of loperamide hydrochloride (LOP) and naloxone hydrochloride (NLX), an opioid agonist and antagonist, respectively, on electrolyte equilibrium in ileal and colonic mucosae and to estimate the possible influence of divergent activity of the endogenous opioid system (EOS) on IBS therapy. METHODS: Two mouse lines bidirectionally selected for high (HA) and low (LA) swim stress-induced analgesia associated with high and low EOS activity were used in this study...
July 26, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28745076/effects-of-ici204-448-naloxone-methiodide-and-levocetirizine-on-the-scratching-behavior-induced-by-a-%C3%AE%C2%BA-opioid-antagonist-nor-bni-in-icr-mice
#19
Tasuku Nakasone, Hirokazu Wakuda, Yumi Sugimoto, Chiaki Kamei
OBJECTIVE: In this study, we aimed to study the effects of ICI204,448, naloxone methiodide and levocetirizine on the scratching behavior induced by intradermal injection of a ?-opioid antagonist, nor-binaltorphimine (nor-BNI), into the rostral back of ICR mice were investigated. MATERIALS AND METHODS: Male ICR mice weighing 30?35 g were used. The number of scratching episodes were counted for 60 min after i.d. injection of nor-BNI. RESULTS: nor-BNI dose dependently increased in the number of scratching episodes in ICR mice...
July 26, 2017: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/28742624/impact-of-a-mandated-change-in-buprenorphine-formulation
#20
Ryan Graddy, Darius A Rastegar
OBJECTIVE: This study examines the impact of an insurance-mandated change in formulation of buprenorphine/naloxone (BNX) for patients with opioid use disorder treated in a primary care clinic. METHODS: A retrospective cohort study was conducted to determine the proportion of patients who were switched back to the previous BNX formulation and rates of aberrant urine drug tests for the 3 months before and 3 months after a mandated change in BNX from the sublingual film to the rapidly dissolving tablet (BNX-RDT)...
July 24, 2017: Journal of Addiction Medicine
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