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https://www.readbyqxmd.com/read/28328552/il-1%C3%AE-levels-are-associated-with-chronic-multisite-pain-in-people-living-with-hiv
#1
Jessica S Merlin, Andrew O Westfall, Sonya L Heath, Burel R Goodin, Jesse C Stewart, Robert E Sorge, Jarred Younger
BACKGROUND: The pathophysiology of chronic pain experienced by people living with HIV (PLWH) in the current antiretroviral treatment era is poorly understood. We sought to investigate the relationship between inflammation and chronic pain in PLWH. We hypothesized that, among PLWH who have undetectable HIV viral loads, those with Chronic Multisite Pain (CMP) would have higher levels of circulating pain-related inflammatory markers than those without chronic pain. SETTING: This study was conducted at the University of Alabama at Birmingham's Center for AIDS Research Network of Integrated Clinical System (CNICS) site...
March 20, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/28324705/more-pain-more-gain-blocking-the-opioid-system-boosts-adaptive-cognitive-control
#2
Henk van Steenbergen, Daniel H Weissman, Dan J Stein, Susan Malcolm-Smith, Jack van Honk
The ability to adaptively increase cognitive control in response to cognitive challenges is crucial for goal-directed behavior. Recent findings suggest that aversive arousal triggers adaptive increases of control, but the neurochemical mechanisms underlying these effects remain unclear. Given the known contributions of the opioid system to hedonic states, we investigated whether blocking this system increases adaptive control modulations. To do so, we conducted a double-blind, placebo-controlled psychopharmacological study (n=52 females) involving a Stroop-like task...
March 7, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28323287/experimental-medication-treatment-approaches-for-depression
#3
REVIEW
D F Ionescu, G I Papakostas
Depression is one of the most common psychiatric conditions. Symptoms can lead to significant disability, which result in impairments in overall quality of life. Though there are many approved antidepressant treatments for depression-including selective serotonin reuptake inhibitors, tricyclic antidepressants and monoamine oxidase inhibitors-about a third of patients do not respond to these medications. Therefore, it is imperative for drug discovery to continue towards the development of novel and rapidly acting compounds, especially for patients with treatment-resistant depression...
March 21, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28318893/design-and-characterization-of-opioid-ligands-based-on-cycle-in-macrocycle-scaffold
#4
Anna Adamska-Bartłomiejczyk, Rossella De Marco, Luca Gentilucci, Alicja Kluczyk, Anna Janecka
The study reports on a series of novel cyclopeptides based on the structure Tyr-[d-Lys-Phe-Phe-Asp]NH2, a mixed mu and kappa opioid receptor agonist with low nanomolar affinity, in which Phe(4) residue was substituted by cyclic amino acids, such as Pro or its six-membered surrogates, piperidine-2-, 3- or 4-carboxylic acids (Pip, Nip and Inp, respectively). All derivatives exhibited high mu- and moderate delta-opioid receptor affinity, and almost no binding to the kappa-opioid receptor. Conformational analysis suggested that the cis conformation of the peptide bond Phe(3)-Xaa(4) influences receptor selectivity through the control of the position of Phe(3) side chain...
February 28, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28315071/delta-opioid-receptor-and-peptide-a-dynamic-therapy-for-stroke-and-other-neurological-disorders
#5
M Grant Liska, Marci G Crowley, Trenton Lippert, Sydney Corey, Cesar V Borlongan
Research of the opioid system and its composite receptors and ligands has revealed its promise as a potential therapy for neurodegenerative diseases such as stroke and Parkinson's Disease. In particular, delta opioid receptors (DORs) have been elucidated as a therapeutically distinguished subset of opioid receptors and a compelling target for novel intervention techniques. Research is progressively shedding light on the underlying mechanism of DORs and has revealed two mechanisms of DOR neuroprotection; DORs function to maintain ionic homeostasis and also to trigger endogenous neuroprotective pathways...
March 18, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28303899/the-behavioral-effects-of-the-antidepressant-tianeptine-require-the-mu-opioid-receptor
#6
Benjamin Adam Samuels, Katherine M Nautiyal, Andrew C Kruegel, Marjorie R Levinstein, Valerie M Magalong, Madalee M Gassaway, Steven G Grinnell, Jaena Han, Michael A Ansonoff, John E Pintar, Jonathan A Javitch, Dalibor Sames, René Hen
Depression is a debilitating chronic illness that affects around 350 million people worldwide. Current treatments, such as selective serotonin reuptake inhibitors (SSRIs), are not ideal because only a fraction of patients achieve remission. Tianeptine is an effective antidepressant with a previously unknown mechanism of action. We recently reported that tianeptine is a full agonist at the mu-opioid receptor (MOR). Here we demonstrate that the acute and chronic antidepressant-like behavioral effects of tianeptine in mice require MOR...
March 17, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28302509/binding-mode-analyses-of-nap-derivatives-as-mu-opioid-receptor-selective-ligands-through-docking-studies-and-molecular-dynamics-simulation
#7
Huiqun Wang, Saheem A Zaidi, Yan Zhang
Mu opioid receptor selective antagonists are highly desirable because of their utility as pharmacological probes for receptor characterization and functional studies. Furthermore, the mu opioid receptors act as an important target in drug abuse and addiction treatment. Previously, we reported NAP as a novel lead compound with high selectivity and affinity towards the mu opioid receptor. Based on NAP, we have synthesized its derivatives and further characterized their binding affinities and selectivity towards the receptor...
March 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28296137/percutaneous-peripheral-nerve-stimulation-for-the-treatment-of-chronic-low-back-pain-two-clinical-case-reports-of-sustained-pain-relief
#8
Leonardo Kapural, Christopher A Gilmore, John Chae, Richard L Rauck, Steven P Cohen, Michael F Saulino, Amorn Wongsarnpigoon, Meredith J McGee, Joseph W Boggs
As the leading cause of disability among U.S. adults, chronic low back pain (LBP) is one sof the most prevalent and challenging musculoskeletal conditions. Neuromodulation provides an opportunity to reduce or eliminate the use of opioids to treat chronic LBP, but the cost and invasiveness of existing methods have limited its broad adoption, especially earlier in the treatment continuum. The present case report details the results of a novel method of short-term percutaneous peripheral nerve stimulation (PNS) in 2 subjects with chronic LBP...
March 14, 2017: Pain Practice: the Official Journal of World Institute of Pain
https://www.readbyqxmd.com/read/28293525/surgical-site-infiltration-for-abdominal-surgery-a-novel-neuroanatomical-based-approach
#9
Girish P Joshi, Jeffrey E Janis, Eric M Haas, Bruce J Ramshaw, Mikio A Nihira, Brian J Dunkin
BACKGROUND: Provision of optimal postoperative analgesia should facilitate postoperative ambulation and rehabilitation. An optimal multimodal analgesia technique would include the use of nonopioid analgesics, including local/regional analgesic techniques such as surgical site local anesthetic infiltration. This article presents a novel approach to surgical site infiltration techniques for abdominal surgery based upon neuroanatomy. METHODS: Literature searches were conducted for studies reporting the neuroanatomical sources of pain after abdominal surgery...
December 2016: Plastic and Reconstructive Surgery. Global Open
https://www.readbyqxmd.com/read/28292508/pharmacy-based-statewide-naloxone-distribution-a-novel-top-down-bottom-up-approach
#10
Kate J Morton, Brianna Harrand, Carly Cloud Floyd, Craig Schaefer, Julie Acosta, Bridget Claire Logan, Karen Clark
OBJECTIVE: To highlight New Mexico's multifaceted approach to widespread pharmacy naloxone distribution and to share the interventions as a tool for improving pharmacy-based naloxone practices in other states. SETTING: New Mexico had the second highest drug overdose death rate in 2014 of which 53% were related to prescription opioids. Opioid overdose death is preventable through the use of naloxone, a safe and effective medication that reverses the effects of prescription opioids and heroin...
March 2017: Journal of the American Pharmacists Association: JAPhA
https://www.readbyqxmd.com/read/28292502/opioid-overdose-education-and-naloxone-distribution-development-of-the-veterans-health-administration-s-national-program
#11
Elizabeth M Oliva, Melissa L D Christopher, Daina Wells, Mark Bounthavong, Michael Harvey, Julianne Himstreet, Thomas Emmendorfer, Michael Valentino, Mariano Franchi, Francine Goodman, Jodie A Trafton
OBJECTIVES: To prevent opioid-related mortality, the Veterans Health Administration (VHA) developed a national Opioid Overdose Education and Naloxone Distribution (OEND) program. SETTING: VHA's OEND program sought national implementation of OEND across all medical facilities (n = 142). PRACTICE DESCRIPTION: This paper describes VHA's efforts to facilitate nationwide health care system-based OEND implementation, including the critical roles of VHA's national pharmacy services and academic detailing services...
March 2017: Journal of the American Pharmacists Association: JAPhA
https://www.readbyqxmd.com/read/28292501/indian-health-service-pharmacists-engaged-in-opioid-safety-initiatives-and-expanding-access-to-naloxone
#12
Hillary Duvivier, Samantha Gustafson, Morgan Greutman, Tenzin Jangchup, Ashlee Knapp Harden, Aimee Reinhard, Keith Warshany
OBJECTIVE: To develop effective pharmacy-based interventions to mitigate harm from opioid use disorders. Programs include responsible opioid prescribing, expanded access to medication-assisted treatment (MAT), naloxone, and community interventions. SETTING: Clinical pharmacists practicing at Indian Health Service (IHS) locations in the Southwest, Midwest, and Great Lakes regions. These pharmacists serve culturally diverse American Indian populations throughout the United States and interface with tribal and federal programs to impact the opioid epidemic in Indian Country...
March 2017: Journal of the American Pharmacists Association: JAPhA
https://www.readbyqxmd.com/read/28291693/synthesis-and-evaluation-of-a-ligand-targeting-the-%C3%AE-and-%C3%AE-opioid-receptors-for-drug-delivery-to-lung-cancer
#13
Guo Li, Philip S Low
A well-established approach to developing new imaging agents and treatments for cancer begins with the recognition of receptors that are overexpressed in cancer cells. Ideally, these same receptors would also be absent, or minimally expressed, in healthy tissue. The mu (μ) and delta (δ) opioid receptors (MOR and DOR respectively) match these criteria, with expression in cancer cells that is higher than primary lung epithelial cells. Naltrexone is a drug approved by the U.S. Food and Drug Administration (FDA) for treatment of alcohol dependence or prevention of relapse from opioid addiction...
June 28, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28291541/evidence-for-a-novel-neurohumoral-antinociceptive-mechanism-mediated-by-peripheral-capsaicin-sensitive-nociceptors-in-conscious-rats
#14
Gábor Pethő, Kata Bölcskei, Réka Füredi, Bálint Botz, Teréz Bagoly, Erika Pintér, János Szolcsányi
Stimulation of capsaicin-sensitive peripheral sensory nerve terminals induces remote anti-inflammatory effects throughout the body of anesthetized rats and guinea-pigs mediated by somatostatin. As somatostatin has also antinociceptive effects, the study aimed at investigating whether similar remote antinociceptive effects can be demonstrated in awake animals. In conscious rats, nociceptive nerve endings of the right hind paw decentralized by cutting the sciatic and saphenous nerves 18h before were chemically stimulated, and drop of the noxious heat threshold (heat hyperalgesia) induced by prior (18h before) plantar incision was measured on the contralateral, left hind paw using an increasing-temperature water bath...
February 10, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28291085/respiratory-effects-of-the-nociceptin-orphanin-fq-peptide-and-opioid-receptor-agonist-cebranopadol-in-healthy-human-volunteers
#15
Albert Dahan, Merel Boom, Elise Sarton, Justin Hay, Geert Jan Groeneveld, Meike Neukirchen, John Bothmer, Leon Aarts, Erik Olofsen
BACKGROUND: Cebranopadol is a novel strong analgesic that coactivates the nociceptin/orphanin FQ receptor and classical opioid receptors. There are indications that activation of the nociceptin/orphanin FQ receptor is related to ceiling in respiratory depression. In this phase 1 clinical trial, we performed a pharmacokinetic-pharmacodynamic study to quantify cebranopadol's respiratory effects. METHODS: Twelve healthy male volunteers received 600 μg oral cebranopadol as a single dose...
April 2017: Anesthesiology
https://www.readbyqxmd.com/read/28288815/rf313-an-orally-bioavailable-neuropeptide-ff-receptor-antagonist-opposes-effects-of-rf-amide-related-peptide-3-and-opioid-induced-hyperalgesia-in-rodents
#16
Khadija Elhabazi, Jean-Paul Humbert, Isabelle Bertin, Raphaelle Quillet, Valérie Utard, Martine Schmitt, Jean-Jacques Bourguignon, Emilie Laboureyras, Meric Ben Boujema, Guy Simonnet, Caroline Ancel, Valérie Simonneaux, Massimiliano Beltramo, Bernard Bucher, Tania Sorg, Hamid Meziane, Elodie Schneider, Benoit Petit-Demoulière, Brigitte Ilien, Frédéric Bihel, Frédéric Simonin
Although opiates represent the most effective analgesics, their use in chronic treatments is associated with numerous side effects including the development of pain hypersensitivity and analgesic tolerance. We recently identified a novel orally active neuropeptide FF (NPFF) receptor antagonist, RF313, which efficiently prevents the development of fentanyl-induced hyperalgesia in rats. In this study, we investigated the properties of this compound into more details. We show that RF313 exhibited a pronounced selectivity for NPFF receptors, antagonist activity at NPFF1 receptor (NPFF1R) subtype both in vitro and in vivo and no major side effects when administered in mice up to 30 mg/kg...
March 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28288109/in-silico-design-of-novel-probes-for-the-atypical-opioid-receptor-mrgprx2
#17
Katherine Lansu, Joel Karpiak, Jing Liu, Xi-Ping Huang, John D McCorvy, Wesley K Kroeze, Tao Che, Hiroshi Nagase, Frank I Carroll, Jian Jin, Brian K Shoichet, Bryan L Roth
The primate-exclusive MRGPRX2 G protein-coupled receptor (GPCR) has been suggested to modulate pain and itch. Despite putative peptide and small-molecule MRGPRX2 agonists, selective nanomolar-potency probes have not yet been reported. To identify a MRGPRX2 probe, we first screened 5,695 small molecules and found that many opioid compounds activated MRGPRX2, including (-)- and (+)-morphine, hydrocodone, sinomenine, dextromethorphan, and the prodynorphin-derived peptides dynorphin A, dynorphin B, and α- and β-neoendorphin...
March 13, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/28284867/role-of-the-sugar-moiety-on-the-opioid-receptor-binding-and-conformation-of-a-series-of-enkephalin-neoglycopeptides
#18
Mònica Rosa, Verónica Gonzalez-Nunez, Katherine Barreto-Valer, Filipa Marcelo, Julia Sánchez-Sánchez, Luis P Calle, Juan C Arévalo, Raquel E Rodríguez, Jesús Jiménez-Barbero, Gemma Arsequell, Gregorio Valencia
Glycosylation by simple sugars is a drug discovery alternative that has been explored with varying success for enhancing the potency and bioavailability of opioid peptides. Long ago we described two O-glycosides having either β-Glucose and β-Galactose of (d-Met(2), Pro(5))-enkephalinamide showing one of the highest antinociceptive activities known. Here, we report the resynthesis of these two analogs and the preparation of three novel neoglycopeptide derivatives (α-Mannose, β-Lactose and β-Cellobiose)...
February 27, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28283055/opioid-use-disorder-a-desperate-need-for-novel-treatments
#19
Brian S Fuehrlein, David A Ross
No abstract text is available yet for this article.
April 1, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28280516/evaluation-of-analgesic-activity-of-papaver-libanoticum-extract-in-mice-involvement-of-opioids-receptors
#20
Mohamad Ali Hijazi, Ahmed El-Mallah, Maha Aboul-Ela, Abdalla Ellakany
Papaver libanoticum is an endemic plant to Lebanese region (family Papaveraceae) that has not been investigated before. The present study aimed to explore the analgesic activity of dried ethanolic extract of Papaver libanoticum (PLE) using tail flick, hot plate, and acetic acid induced writhing models in mice. The involvement of opioid receptors in the analgesic mechanism was investigated using naloxone antagonism. Results demonstrated that PLE exhibited a potent dose dependent analgesic activity in all tested models for analgesia...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
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