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https://www.readbyqxmd.com/read/28806222/transient-receptor-potential-vanilloid-1-antagonists-prevent-anesthesia-induced-hypothermia-and-decrease-postincisional-opioid-dose-requirements-in-rodents
#1
Andras Garami, Mohab Ibrahim, Kerry Gilbraith, Rajesh Khanna, Eszter Pakai, Alexandra Miko, Erika Pinter, Andrej A Romanovsky, Frank Porreca, Amol M Patwardhan
BACKGROUND: Intraoperative hypothermia and postoperative pain control are two important clinical challenges in anesthesiology. Transient receptor potential vanilloid 1 has been implicated both in thermoregulation and pain. Transient receptor potential vanilloid 1 antagonists were not advanced as analgesics in humans in part due to a side effect of hyperthermia. This study tested the hypothesis that a single, preincision injection of a transient receptor potential vanilloid 1 antagonist could prevent anesthesia-induced hypothermia and decrease the opioid requirement for postsurgical hypersensitivity...
August 14, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28806211/the-opiorphin-analog-str-324-decreases-sensory-hypersensitivity-in-a-rat-model-of-neuropathic-pain
#2
Alain Van Elstraete, Philippe Sitbon, Leila Hamdi, Victor Juarez-Perez, Jean-Xavier Mazoit, Dan Benhamou, Catherine Rougeot
BACKGROUND: Neuropathic pain represents a therapeutic challenge, and treatments with increased efficacy and tolerability still need to be developed. Opiorphin protects endogenous enkephalins from degradation, potentiating enkephalin-dependent analgesia via the activation of opioid pathways. Enkephalins are natural ligands of opioid receptors, with strong affinity for δ-opioid receptors. Expression of functional δ-opioid receptors increases in sensory neurons after peripheral nerve injury in neuropathic pain models...
August 10, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28805972/in-vitro-pharmacological-characterization-of-a-novel-unbiased-nop-receptor-selective-nonpeptide-agonist-at-403
#3
Federica Ferrari, Davide Malfacini, Blair V Journigan, Mark F Bird, Claudio Trapella, Remo Guerrini, David G Lambert, Girolamo Calo', Nurulain T Zaveri
Nociceptin/orphanin FQ (N/OFQ) regulates several biological functions via selective activation of the N/OFQ receptor (NOP), a member of the opioid receptor family. We recently identified a new high affinity and highly selective NOP agonist AT-403. In this study, we characterized the functional profile of AT-403 and compared it to other known nonpeptide NOP agonists Ro 65-6570, Ro 2q, SCH-221510, MCOPPB, AT-202 and SCH-486757, using the following assays: GTPγ[(35) S] stimulated binding, calcium mobilization assay in cells-expressing human NOP or classical opioid receptors and chimeric G proteins, bioluminescence resonance energy transfer (BRET) based assay for studying NOP receptor interaction with G protein and arrestin, and the electrically stimulated mouse vas deferens bioassay...
August 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28802882/chronic-opioid-therapy-modifies-qst-changes-following-ketamine-infusion-in-chronic-pain-patients
#4
Dermot P Maher, Yi Zhang, Shihab Ahmed, Tina Doshi, Charlene Malarick, Kristin Stabach, Jianren Mao, Lucy Chen
The long-term effects of opioids on sensitization processes are believed to be mediated through the NDMA receptor. QST changes observed following a ketamine infusion have been previously described but the effect that chronic opioids will have is not known. The results of this prospective randomized factorial trial compared the thermal QST changes observed following a 0.05 mg/kg ketamine infusion or a saline placebo in chronic pain subjects who were either opioid-naïve or were chronically using opioids for chronic non-cancer pain are presented...
August 9, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28802836/neocortical-prodynorphin-expression-is-transiently-increased-with-learning-implications-for-time-and-learning-dependent-neocortical-kappa-opioid-receptor-activation
#5
Ryan Loh, Sean Collins, Roberto Galvez
There are several lines of evidence that indicate a prominent role for the opioid system in the acquisition and consolidation of learned associations. Specifically, kappa opioid receptor (KOR) modulation has been demonstrated to alter various behavioral tasks including whisker trace eyeblink conditioning (WTEB). WTEB is an associative conditioning paradigm in which a neutral conditioned stimulus (CS; Whisker stimulation) is paired following a short stimulus free trace interval with a salient unconditioned stimulus that elicits a blink response (US; Eye shock)...
August 9, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28798303/understanding-the-molecular-basis-of-agonist-antagonist-mechanism-of-human-mu-opioid-receptor-through-gaussian-accelerated-molecular-dynamics-method
#6
Yeng-Tseng Wang, Yang-Hsiang Chan
The most powerful analgesic and addictive properties of opiate alkaloids are mediated by the μ opioid receptor (MOR). The MOR has been extensively investigated as a drug target in the twentieth century, with numerous compounds of varying efficacy being identified. We employed molecular dynamics and Gaussian accelerated molecular dynamics techniques to identify the binding mechanisms of MORs to BU72 (agonist) and β-funaltrexamine (antagonist). Our approach theoretically suggests that the 34 residues (Lys209-Phe221 and Ile301-Cys321) of the MORs were the key regions enabling the two compounds to bind to the active site of the MORs...
August 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28797641/b2-kinin-receptors-in-the-dorsal-periaqueductal-gray-are-implicated-in-the-panicolytic-like-effect-of-opiorphin
#7
Caio César Sestile, Jhonatan Christian Maraschin, Marcel Pereira Rangel, Rosangela Getirana Santana, Hélio Zangrossi, Frederico Guilherme Graeff, Elisabeth Aparecida Audi
Reported results have shown that the pentapeptide opiorphin inhibits oligopeptidases that degrade brain neuropeptides, and has analgesic and antidepressant effects in experimental animals, without either tolerance or dependency after chronic administration. In a previous study we showed that opiorphin has a panicolytic-like effect in the dorsal periaqueductal gray (dPAG) electrical stimulation test (EST), mediated by the μ-opioid receptor (MOR). This study further analyzes the mechanism of opiorphin panicolytic action, using the EST and drug injection inside the dPAG...
August 7, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28796769/medication-related-patient-harm-in-new-zealand-hospitals
#8
Gillian Robb, Elizabeth Loe, Ashika Maharaj, Richard Hamblin, Mary E Seddon
AIM: The purpose of this study is to identify patterns of medication-related harm from a national perspective, and to use this information to inform decisions on where to focus medication safety efforts. This study updates a 2013 study using the same methodology. METHOD: District health boards (DHBs) still actively using either the Adverse Drug Event (ADE) Trigger Tool (TT) or the Global Trigger Tool (GTT), submitted two years of anonymised ADE data (1 July 2013-30 June 2015) to the Health Quality & Safety Commission (the Commission) using a standard template...
August 11, 2017: New Zealand Medical Journal
https://www.readbyqxmd.com/read/28796483/placement-of-hydroxy-moiety-on-pendant-of-peptidomimetic-scaffold-modulates-mu-and-kappa-opioid-receptor-efficacy
#9
Aubrie A Harland, Irina D Pogozheva, Nicholas W Griggs, Tyler J Trask, John R Traynor, Henry I Mosberg
In an effort to expand the structure-activity relationship (SAR) studies of a series of mixed-efficacy opioid ligands, peptidomimetics that incorporate methoxy and hydroxy groups around a benzyl or 2-methylindanyl pendant on a tetrahydroquinoline (THQ) core of the peptidomimetics were evaluated. Compounds containing a methoxy or hydroxy moiety in the o- or m- positions increased binding affinity to the kappa opioid receptor (KOR), whereas compounds containing methoxy or hydroxy groups in the p- position decreased KOR affinity and reduced or eliminated efficacy at the mu opioid receptor (MOR)...
August 10, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28795389/anti-nociceptive-effect-of-patchouli-alcohol-involving-attenuation-of-cyclooxygenase-2-and-modulation-of-mu-opioid-receptor
#10
Xuan Yu, Xin-Pei Wang, Xiao-Jin Yan, Jing-Fei Jiang, Fan Lei, Dong-Ming Xing, Yue-Ying Guo, Li-Jun Du
OBJECTIVE: To explore the anti-nociceptive effect of patchouli alcohol (PA), the essential oil isolated from Pogostemon cablin (Blanco) Bent, and determine the mechanism in molecular levels. METHODS: The acetic acid-induced writhing test and formalin-induced plantar injection test in mice were employed to confifirm the effect in vivo. Intracellular calcium ion was imaged to verify PA on mu-opioid receptor (MOR). Cyclooxygenase 2 (COX2) and MOR of mouse brain were expressed for determination of PA's target...
August 9, 2017: Chinese Journal of Integrative Medicine
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
#11
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/28790973/malignant-cerebellar-edema-subsequent-to-accidental-prescription-opioid-intoxication-in-children
#12
Daniel Duran, Robert D Messina, Lauren A Beslow, Julio D Montejo, Jason K Karimy, Charuta Gavankar Furey, Alison D Sheridan, Gordon Sze, Yanki Yarman, Michael L DiLuna, Kristopher T Kahle
We present two recent cases of toddlers who developed malignant cerebellar edema subsequent to accidental ingestion of prescription opioids. Both children presented acute neurological decline, hydrocephalus, and tonsillar herniation requiring emergent ventricular drain placement, suboccipital craniectomy, and partial cerebellectomy. Together with several other reports, these cases suggest the existence of an uncommon yet severe syndrome of acute opioid-induced malignant cerebellar edema. We hypothesize that the condition results from a combination of primary opioid receptor-mediated changes in neuronal metabolism that are exacerbated by secondary hypoxic insult...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28790193/assessing-the-value-of-the-zebrafish-conditioned-place-preference-model-for-predicting-human-abuse-potential
#13
Alistair James Brock, Susan M G Goody, Andrew N Mead, Ari Sudwarts, Matthew O Parker, Caroline H Brennan
Regulatory agencies recommend that centrally-active drugs are tested for abuse potential prior to approval. Standard preclinical assessments are conducted in rats or non-human primates (NHPs). This study evaluated the ability of the zebrafish conditioned place preference (CPP) model to predict human abuse outcomes. Twenty-seven compounds from a variety of pharmacological classes were tested in zebrafish CPP, categorized as positive or negative, and analysed using standard diagnostic tests of binary classification to determine the likelihood that zebrafish correctly predict robust positive signals in human subjective effects studies (+HSE) and/or DEA drug scheduling...
August 8, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28783942/codeine-precipitating-serotonin-syndrome-in-a-patient-in-therapy-with-antidepressant-and-triptan
#14
Giulia Milano, Werner Maria Natta, Alfredo Bello, Antonietta Martelli, Francesca Mattioli
The serotonin syndrome is a serioius medical condition due due to an intensive stimulation of setonin receptors. It is a rare, but severe, consequence of interaction between serotomimetic agents. This is a report of a 70-year-old woman steadily in therapy with venlafaxine and rizatriptan for migraine and major depressive syndrome. She was admitted to neurology unit for decreased light reflex with miotic pupils, global hyperreflexia, tremor, anxiety, ataxia and incoordination. The patient was diagnosed as a probable case of serotonin syndrome due to a pharmacological interaction between venlafaxine and rizatriptan trigged by opioid intake...
August 31, 2017: Clinical Psychopharmacology and Neuroscience: the Official Scientific Journal of the Korean College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28782637/synthesis-and-activity-of-opioid-peptidomimetics-with-%C3%AE-2-and-%C3%AE-3-amino-acids
#15
Katarzyna Gach-Janczak, Justyna Piekielna-Ciesielska, Anna Adamska-Bartłomiejczyk, Renata Perlikowska, Rafał Kruszyński, Alicja Kluczyk, Julia Krzywik, Jarosław Sukiennik, Maria Camilla Cerlesi, Girolamo Calo, Andrzej Wasilewski, Marta Zielińska, Anna Janecka
Morphiceptin (Tyr-Pro-Phe-Pro-NH2) is a selective ligand of the mu opioid receptor, an important target in pain regulation. In this study, morphiceptin was modified at positions 2 or 3 by introduction of β(2)- or β(3)-amino acids and additionally in position 1 by replacing Tyr by Dmt (2',6'-dimethyltyrosine), which resulted in obtaining enzymatically stable analogs with mixed opioid receptor affinity profiles. An analog of the sequence Dmt-D-Ala-(R)-β(2)-1-Nal-Pro-NH2 [Nal=3-(1-naphthyl)-alanine] showed very high activity at the mu and delta receptors in the calcium mobilization functional test but did not cross the artificial membrane imitating the blood-brain barrier...
August 3, 2017: Peptides
https://www.readbyqxmd.com/read/28781901/enkephalins-endogenous-analgesics-with-an-emerging-role-in-stress-resilience
#16
REVIEW
Mathilde S Henry, Louis Gendron, Marie-Eve Tremblay, Guy Drolet
Psychological stress is a state of mental or emotional strain or tension that results from adverse or demanding circumstances. Chronic stress is well known to induce anxiety disorders and major depression; it is also considered a risk factor for Alzheimer's disease. Stress resilience is a positive outcome that is associated with preserved cognition and healthy aging. Resilience presents psychological and biological characteristics intrinsic to an individual conferring protection against the development of psychopathologies in the face of adversity...
2017: Neural Plasticity
https://www.readbyqxmd.com/read/28781727/cross-state-dependent-learning-interaction-between-scopolamine-and-morphine-in-mice-the-role-of-dorsal-hippocampus
#17
Morteza Maleki, Majid Hassanpour-Ezatti, Majid Navaeian
INTRODUCTION: The current study aimed at investigating the existence of the cross state-dependent learning between morphine and scopolamine (SCO) in mice by passive avoidance method, pointing to the role of CA1 area. METHODS: The effects of pre-training SCO (0.75, 1.5, and 3 μg, Intra-CA1), or morphine (1, 3, and 6 mg/kg, intraperitoneal (i.p.) was evaluated on the retrieval of passive avoidance learning using step-down task in mice (n=10). Then, the effect of pretest administration of morphine (1...
May 2017: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/28780734/intra-accumbal-cannabinoid-agonist-attenuated-reinstatement-but-not-extinction-period-of-morphine-induced-conditioned-place-preference-evidence-for-different-characteristics-of-extinction-period-and-reinstatement
#18
Hossein Khaleghzadeh-Ahangar, Abbas Haghparast
The brain reward system consists of the ventral tegmental area that sends its dopaminergic projections to the forebrain, cortical areas, amygdala and largely to the nucleus accumbens (NAc). The present study aims were to investigate the effects of bilateral intra-accumbal microinjection of WIN55,212-2, a CB1 receptor agonist, on the duration of extinction period and reinstatement to morphine by the conditioned place preference (CPP) paradigm in the rat. Forty-six adult male albino Wistar rats received intra-accumbal WIN55,212-2 [p0...
August 5, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28780471/neuropathic-pain-attenuating-effects-of-perampanel-in-an-experimental-model-of-chronic-constriction-injury-in-rats
#19
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/28780411/increased-ethanol-drinking-in-humanized-mice-expressing-the-mu-opioid-receptor-a118g-polymorphism-are-mediated-through-sex-specific-mechanisms
#20
Angela N Henderson-Redmond, Tammy E Lowe, Xi B Tian, Daniel J Morgan
The A118G single nucleotide polymorphism (SNP) of the mu-opioid receptor gene (Oprm1) has been implicated in mediating the rewarding effects of alcohol. Clinical and preclinical studies suggest that the G allele may confer a genetic vulnerability to alcohol dependence, though it remains unknown whether these effects are sex-specific. We used male and female mice homozygous for the "humanized" 118AA or 118GG alleles to determine whether the A118G SNP potentiates ethanol consumption in a sex-specific manner in both the two-bottle choice and drinking-in-the-dark (DID) paradigms...
August 2, 2017: Brain Research Bulletin
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