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https://www.readbyqxmd.com/read/28432424/variations-of-isovaline-structure-related-to-activity-in-the-formalin-foot-assay-in-mice
#1
Timothy Fung, Yahya I Asiri, Richard Wall, Stephan K W Schwarz, Ernest Puil, Bernard A MacLeod
Current centrally acting analgesics such as opioids are associated with adverse effects that limit their use and threaten patient safety. Isovaline is a novel prototype analgesic that produces peripheral antinociception in several pain models with little or no effect on the central nervous system. The aim of this study was to establish a preliminary structure-activity relationship for isovaline derivatives by assaying efficacy in the formalin foot assay and central adverse effect profile in mice. Selected compounds were tested using the formalin foot assay to determine efficacy in reducing formalin-induced behaviors...
April 21, 2017: Amino Acids
https://www.readbyqxmd.com/read/28426670/mice-expressing-a-hyper-sensitive-form-of-the-cb1-cannabinoid-receptor-cb1-show-modestly-enhanced-alcohol-preference-and-consumption
#2
David J Marcus, Angela N Henderson-Redmond, Maciej Gonek, Michael L Zee, Jill C Farnsworth, Randa A Amin, Mary-Jeanette Andrews, Brian J Davis, Ken Mackie, Daniel J Morgan
We recently characterized S426A/S430A mutant mice expressing a desensitization-resistant form of the CB1 receptor. These mice display an enhanced response to endocannabinoids and ∆9-THC. In this study, S426A/S430A mutants were used as a novel model to test whether ethanol consumption, morphine dependence, and reward for these drugs are potentiated in mice with a "hyper-sensitive" form of CB1. Using an unlimited-access, two-bottle choice, voluntary drinking paradigm, S426A/S430A mutants exhibit modestly increased intake and preference for low (6%) but not higher concentrations of ethanol...
2017: PloS One
https://www.readbyqxmd.com/read/28425121/role-of-the-dynorphin-kappa-opioid-receptor-system-in-the-motivational-effects-of-ethanol
#3
Rachel I Anderson, Howard C Becker
Evidence has demonstrated that dynorphin (DYN) and the kappa opioid receptor (KOR) system contribute to various psychiatric disorders, including anxiety, depression, and addiction. More recently, this endogenous opioid system has received increased attention as a potential therapeutic target for treating alcohol use disorders. In this review, we provide an overview and synthesis of preclinical studies examining the influence of alcohol (ethanol) exposure on DYN/KOR expression and function, as well as studies examining the effects of DYN/KOR manipulation on ethanol's rewarding and aversive properties...
April 20, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/28410599/the-role-of-vitamin-c-in-the-treatment-of-pain-new-insights
#4
REVIEW
Anitra C Carr, Cate McCall
The vitamin C deficiency disease scurvy is characterised by musculoskeletal pain and recent epidemiological evidence has indicated an association between suboptimal vitamin C status and spinal pain. Furthermore, accumulating evidence indicates that vitamin C administration can exhibit analgesic properties in some clinical conditions. The prevalence of hypovitaminosis C and vitamin C deficiency is high in various patient groups, such as surgical/trauma, infectious diseases and cancer patients. A number of recent clinical studies have shown that vitamin C administration to patients with chronic regional pain syndrome decreases their symptoms...
April 14, 2017: Journal of Translational Medicine
https://www.readbyqxmd.com/read/28402252/constitutive-activation-of-kappa-opioid-receptors-at-ventral-tegmental-area-inhibitory-synapses-following-acute-stress
#5
Abigail M Polter, Kelsey Barcomb, Rudy W Chen, Paige M Dingess, Nicholas M Graziane, Travis E Brown, Julie A Kauer
Stressful experiences potently activate kappa opioid receptors (κORs). κORs in the ventral tegmental area regulate multiple aspects of dopaminergic and non-dopaminergic cell function. Here we show that at GABAergic synapses on rat VTA dopamine neurons, a single exposure to a brief cold-water swim stress induces prolonged activation of κORs. This is mediated by activation of the receptor during the stressor followed by a persistent, ligand-independent constitutive activation of the κOR itself. This lasting change in function is not seen at κORs at neighboring excitatory synapses, suggesting distinct time courses and mechanisms of regulation of different subsets of κORs...
April 12, 2017: ELife
https://www.readbyqxmd.com/read/28381725/pursuit-of-neurotransmitter-functions-being-attracted-with-fascination-of-the-synapse
#6
Shiro Konishi
 In the beginning of the 1970s, only two chemical substances, acetylcholine and γ-aminobutyric acid (GABA), had been definitely established as neurotransmitters. Under such circumstances, I started my scientific career in Professor Masanori Otsuka's lab searching for the transmitter of primary sensory neurons. Until 1976, lines of evidence had accumulated indicating that the undecapeptide substance P could be released as a transmitter from primary afferent fibers into spinal synapses, although the substance P-mediated synaptic response had yet to be identified...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28381559/identification-of-a-signaling-cascade-that-maintains-constitutive-delta-opioid-receptor-incompetence-in-peripheral-sensory-neurons
#7
Allison Doyle Brackley, Shayda Sarrami, Ruben Gomez, Kristi A Guerrero, Nathaniel A Jeske
Mu opioid receptor (MOR) agonists are often used to treat severe pain, but can result in adverse side effects. To circumvent systemic side effects, targeting peripheral opioid receptors is an attractive alternative treatment for severe pain. Activation of the delta opioid receptor (DOR) produces similar analgesia with reduced side effects. However, until primed by inflammation, peripheral DOR is analgesically incompetent, raising interest in the mechanism. We recently identified a novel role for G protein-coupled receptor kinase 2 (GRK2) that renders DOR analgesically incompetent at the plasma membrane...
April 5, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28379862/vermont-hub-and-spoke-model-of-care-for-opioid-use-disorder-development-implementation-and-impact
#8
John R Brooklyn, Stacey C Sigmon
BACKGROUND: Opioid use disorders (OUDs) are reaching epidemic proportions in the United States, and many geographic areas struggle with a persistent shortage in availability of opioid agonist treatment. Over the past 5 years, Vermont addiction medicine physicians and public health leaders have responded to these challenges by developing an integrated hub-and-spoke opioid treatment network. METHODS: In the present report, we review the development, implementation, and impact of this novel hub-and-spoke model for expanding OUD treatment in Vermont...
April 4, 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28378462/targeting-multiple-opioid-receptors-improved-analgesics-with-reduced-side-effects
#9
REVIEW
Thomas Günther, Pooja Dasgupta, Anika Mann, Elke Miess, Andrea Kliewer, Sebastian Fritzwanker, Ralph Steinborn, Stefan Schulz
Classical opioid analgesics, including morphine, mediate all of their desired and undesired effects by specific activation of the μ-opioid receptor (μ receptor). The use of morphine for treating chronic pain, however, is limited by the development of constipation, respiratory depression, tolerance and dependence. Analgesic effects can also be mediated through other members of the opioid receptor family such as the κ-opioid receptor (κ receptor), δ-opioid receptor (δ receptor) and the nociceptin/orphanin FQ peptide receptor (NOP receptor)...
April 5, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28378414/oxytocin-and-opioid-addiction-revisited-old-drug-new-applications
#10
REVIEW
Panos Zanos, Polymnia Georgiou, Carol Weber, Fiona Robinson, Christos Kouimtsidis, Ramin Niforooshan, Alexis Bailey
Opioid addiction has devastating health and socio-economic consequences, and current pharmacotherapy is limited and often accompanied by side effects, thus novel treatment is warranted. Traditionally, the neurohypophyseal peptide oxytocin (OT) is known for its effects on mediating reward, social affiliation and bonding, stress and learning and memory. There is now strong evidence that OT is a possible candidate for the treatment of drug addiction and depression-addiction co-morbidities. This review summarizes and critically discusses the preclinical evidence surrounding the consequences of pharmacological manipulation of the oxytocinergic system on opioid addiction-related processes, as well as the effects of opioids on the OT system at different stages of the addiction cycle...
April 5, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28377055/original-endomorphin-1-analogues-exhibit-good-analgesic-effects-with-minimal-implications-for-human-sperm-motility
#11
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/28376659/kappa-opioid-receptor-antagonists-a-possible-new-class-of-therapeutics-for-migraine-prevention
#12
Jennifer Y Xie, Milena De Felice, Caroline M Kopruszinski, Nathan Eyde, Justin LaVigne, Bethany Remeniuk, Pablo Hernandez, Xu Yue, Naomi Goshima, Michael Ossipov, Tamara King, John M Streicher, Edita Navratilova, David Dodick, Hugh Rosen, Ed Roberts, Frank Porreca
Background Stress is the most commonly reported migraine trigger. Dynorphin, an endogenous opioid peptide acting preferentially at kappa opioid receptors (KORs), is a key mediator of stress responses. The aim of this study was to use an injury-free rat model of functional cephalic pain with features of migraine and medication overuse headache (MOH) to test the possible preventive benefit of KOR blockade on stress-induced cephalic pain. Methods Following sumatriptan priming to model MOH, rats were hyper-responsive to environmental stress, demonstrating delayed cephalic and extracephalic allodynia and increased levels of CGRP in the jugular blood, consistent with commonly observed clinical outcomes during migraine...
January 1, 2017: Cephalalgia: An International Journal of Headache
https://www.readbyqxmd.com/read/28371816/evaluation-of-an-integrated-multidisciplinary-program-to-address-unsafe-use-of-opioids-prescribed-for-pain
#13
William C Becker, Sara N Edmond, Dana J Cervone, Ajay Manhapra, John J Sellinger, Brent A Moore, Ellen L Edens
Objectives. : Unsafe use of opioids prescribed for pain is a common challenge in primary care. We aimed to describe a novel clinical program designed to address this issue-the Opioid Reassessment Clinic-and evaluate preliminary efficacy. Methods. : The Opioid Reassessment Clinic is a multidisciplinary care team staffed by an internist, addiction psychiatrist, advanced practice nurse, and health psychologist designed to perform enhanced assessment and longitudinal treatment of patients with unsafe use of opioids prescribed for pain...
March 23, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28369738/mu-opioid-receptor-social-behaviour-and-autism-spectrum-disorder-reward-matters
#14
REVIEW
Lucie P Pellissier, Jorge Gandia, Thibaut Laboute, Jerome Aj Becker, Julie Le Merrer
The endogenous opioid system is well known to relieve pain and underpin the rewarding properties of most drugs of abuse. Among opioid receptors, the μ opioid receptor (μOR) mediates most of the analgesic and rewarding properties of opioids. Based on striking similarities between social distress, physical pain and opiate withdrawal, μOR has been proposed to play a critical role in modulating social behaviour in humans and animals. This review summarizes experimental data demonstrating such role and proposes a novel model, the μOR Balance Model, to account for μOR contribution to the subtle regulation of social behaviour...
April 3, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28368571/recent-advances-in-the-realm-of-allosteric-modulators-for-opioid-receptors-for-future-therapeutics
#15
Michael Remesic, Victor J Hruby, Frank Porreca, Yeon Sun Lee
Opioids, and more specifically μ-opioid receptor (MOR) agonists such as morphine, have long been clinically used as therapeutics for severe pain states but often come with serious side effects such as addiction and tolerance. Many studies have focused on bringing about analgesia from the MOR with attenuated side effects, but its underlying mechanism is not fully understood. Recently, focus has been geared toward the design and elucidation of the orthosteric site with ligands of various biological profiles and mixed subtype opioid activities and selectivities, but targeting the allosteric site is an area of increasing interest...
April 7, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28368370/mnsod-mediated-by-hsv-vectors-in-the-periaqueductal-gray-suppresses-morphine-withdrawal-in-rats
#16
T Iida, H Yi, S Liu, D Ikegami, W Zheng, Q Liu, K Takahashi, Y Kashiwagi, W F Goins, J C Glorioso, S Hao
Morphine appears to be the most active metabolite of heroin, therefore, the effects of morphine are important in understanding the ramifications of heroin abuse. Opioid physical dependence (withdrawal response) may have very long-lasting effects on the motivation for reward, including the incubation of cue-induced drug-seeking behavior. However, the exact mechanisms of morphine withdrawal (MW) are not clear yet, and its treatment remains elusive. Periaqueductal gray (PAG) is one of the important sites in the pathogenesis of MW...
April 3, 2017: Gene Therapy
https://www.readbyqxmd.com/read/28368122/synthesis-and-evaluation-of-a-64-cu-conjugate-a-selective-%C3%AE-opioid-receptor-positron-emission-tomography-imaging-agent
#17
Azadeh Pirisedigh, Véronique Blais, Samia Ait-Mohand, Khaled Abdallah, Brian J Holleran, Richard Leduc, Yves L Dory, Louis Gendron, Brigitte Guérin
Given the putative selectivity of the antagonist TIPP (Tyr-Tic-Phe-Phe) for δ-opioid receptors (DOP), this compound was selected for the design of a novel (64)Cu-radiolabeled potent and selective DOP positron emission tomography (PET) imaging agent. Ex vivo autoradiography of TIPPD-PEG-K(NOTA/(64)Cu)-NH2 on rat brain sections produced a distribution pattern consistent with the known expression of DOP. Taken together, the in vitro and ex vivo data indicate that this (64)Cu-tracer holds promise for studying the DOP by means of PET...
April 3, 2017: Organic Letters
https://www.readbyqxmd.com/read/28366739/the-evolution-of-fangs-venom-and-mimicry-systems-in-blenny-fishes
#18
Nicholas R Casewell, Jeroen C Visser, Kate Baumann, James Dobson, Han Han, Sanjaya Kuruppu, Michael Morgan, Anthony Romilio, Vera Weisbecker, Syed A Ali, Jordan Debono, Ivan Koludarov, Ivo Que, Gregory C Bird, Gavan M Cooke, Amanda Nouwens, Wayne C Hodgson, Simon C Wagstaff, Karen L Cheney, Irina Vetter, Louise van der Weerd, Michael K Richardson, Bryan G Fry
Venom systems have evolved on multiple occasions across the animal kingdom, and they can act as key adaptations to protect animals from predators [1]. Consequently, venomous animals serve as models for a rich source of mimicry types, as non-venomous species benefit from reductions in predation risk by mimicking the coloration, body shape, and/or movement of toxic counterparts [2-5]. The frequent evolution of such deceitful imitations provides notable examples of phenotypic convergence and are often invoked as classic exemplars of evolution by natural selection...
March 20, 2017: Current Biology: CB
https://www.readbyqxmd.com/read/28364579/frequency-of-prescription-opioid-misuse-and-suicidal-ideation-planning-and-attempts
#19
Lisham Ashrafioun, Todd M Bishop, Kenneth R Conner, Wilfred R Pigeon
The goal of this study was to examine the relationship between past-year frequency of prescription opioid misuse and past-year suicidal ideation, suicide planning, and suicide attempts. Secondary data analyses were conducted using data from 41,053 participants of the 2014 National Survey of Drug Use and Health. Past-year frequency of prescription opioid misuse was grouped into 4 categories: none, less than monthly (1-11 times), monthly to weekly (12-51 times), and weekly or more (52 times or more). Binomial logistic regression analyses adjusted for demographics, overall health rating, depression, anxiety, and substance use disorders to test the associations between frequency of prescription opioid misuse and suicide-related variables...
March 19, 2017: Journal of Psychiatric Research
https://www.readbyqxmd.com/read/28363796/structure-constrained-endomorphin-analogs-display-differential-antinociceptive-mechanisms-in-mice-after-spinal-administration
#20
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
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