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Opioid receptors

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https://www.readbyqxmd.com/read/28339456/in-errata-kratom-the-new-legal-high-on-the-block-the-case-of-an-emerging-opioid-receptor-agonist-with-substance-abuse-potential
#1
(no author information available yet)
No abstract text is available yet for this article.
March 2017: Pain Physician
https://www.readbyqxmd.com/read/28339433/management-of-neuropathic-chronic-pain-with-methadone-combined-with-ketamine-a-randomized-double-blind-active-controlled-clinical-trial
#2
Flavia Karine Rigo, Gabriela Trevisan, Maria C Godoy, Mateus Fortes Rossato, Gerusa D Dalmolin, Mariane A Silva, Mirian S Menezes, Wolnei Caumo, Juliano Ferreira
BACKGROUND: Methadone and ketamine are used in neuropathic pain management. However, the benefits of both drugs association are uncertain in the treatment of neuropathic pain. OBJECTIVE: Our primary objective was test the hypothesis that oral methadone combined with oral ketamine is more effective than oral methadone or ketamine alone in reducing neuropathic pain. STUDY DESIGN: We conducted a randomized, double blind, active-controlled parallel-group clinical trial...
March 2017: Pain Physician
https://www.readbyqxmd.com/read/28339431/perioperative-ketamine-administration-for-thoracotomy-pain
#3
Daniel W Moyse, Alan D Kaye, James H Diaz, Muhammad Y Qadri, David Lindsay, Srinivas Pyati
BACKGROUND: Of all the postsurgical pain conditions, thoracotomy pain poses a particular therapeutic challenge in terms of its prevalence, severity, and ensuing postoperative morbidity. Multiple pain generators contribute to the severity of post-thoracotomy pain, and therefore a multimodal analgesic therapy is considered to be a necessary strategy. Along with opioids, thoracic epidural analgesia, and paravertebral blocks, N-Methyl-D-Aspartate (NMDA) receptor antagonists such as ketamine have been used as adjuvants to improve analgesia...
March 2017: Pain Physician
https://www.readbyqxmd.com/read/28339199/structure-based-discovery-of-new-antagonist-and-biased-agonist-chemotypes-for-the-kappa-opioid-receptor
#4
Zhong Zheng, Xi-Ping Huang, Thomas J Mangano, Rodger Zou, Xin Chen, Saheem Zaidi, Bryan L Roth, Raymond C Stevens, Vsevolod Katritch
The ongoing epidemics of opioid overdose raises an urgent need for effective anti-addiction therapies and addiction-free painkillers. The κ-opioid receptor (KOR) has emerged as a promising target for both indications, raising demand for new chemotypes of KOR antagonists, as well as G-protein-biased agonists. We employed the crystal structure of the KOR-JDTic complex and ligand-optimized structural templates to perform virtual screening of available compound libraries for new KOR ligands. The prospective virtual screening campaign yielded a high 32% hit rate, identifying novel fragment-like and lead-like chemotypes of KOR ligands...
March 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28338547/satisfaction-with-methadone-and-opioid-receptor-genes-polymorphisms-in-treatment-refractory-heroin-dependent-patients
#5
José Pérez de Los Cobos, Saul Alcaraz, Núria Siñol, Maria Jesús Arranz, Joan Trujols, Francesca Batlle, Francesc Calafell, Santiago Durán-Sindreu, Juliana Salazar
No abstract text is available yet for this article.
March 23, 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28337574/the-rs504393-influences-the-level-of-nociceptive-factors-and-enhances-opioid-analgesic-potency-in-neuropathic-rats
#6
Klaudia Kwiatkowski, Anna Piotrowska, Ewelina Rojewska, Wioletta Makuch, Joanna Mika
Increasing evidence has indicated that activated glial cells releasing nociceptive factors, such as interleukins and chemokines, are of key importance for neuropathic pain. Significant changes in the production of nociceptive factors are associated with the low effectiveness of opioids in neuropathic pain. Recently, it has been suggested that CCL2/CCR2 signaling is important for nociception. Here, we studied the time course changes in the mRNA/protein level of CD40/Iba-1, CCL2 and CCR2 in the spinal cord/dorsal root ganglia (DRG) in rats following chronic constriction injury (CCI) of the sciatic nerve...
March 23, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28336575/pharmacologic-profile-of-naloxegol-a-peripherally-acting-%C3%A2%C2%B5-opioid-receptor-antagonist-for-the-treatment-of-opioid-induced-constipation
#7
Eike Floettmann, Khanh Bui, Mark Sostek, Kemal Payza, Michael Eldon
Opioid-induced constipation (OIC) is a common side effect of opioid pharmacotherapy for the management of pain because opioid agonists bind to µ-opioid receptors in the enteric nervous system (ENS). Naloxegol, a polyethylene glycol derivative of naloxone and a peripherally acting µ-opioid receptor antagonist, targets the physiologic mechanisms that cause OIC. Pharmacologic measures of opioid activity and pharmacokinetic measures of central nervous system (CNS) penetration were employed to characterize the mechanism of action of naloxegol...
March 23, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28333667/effect-of-penetration-enhancers-on-the-percutaneous-delivery-of-pain-management-actives
#8
John Trimble, Bob Light
Transdermal compositions for pain management are comprised of nonsteroidal anti-inflammatory drugs, opioid drugs, and adjuvant drugs acting on: voltage-gated channels, gamma-aminobutyric acid receptors, acute musculoskeletal pain, and as an antidepressant. In this work, baclofen, bupivacaine, cyclobenzaprine, diclofenac, gabapentin, ibuprofen, ketamine, and pentoxifylline were loaded in transdermal compositions, prepared using a mixture of lipids (isopropyl palmitate and mineral oil) and one of two selected penetration enhancer mixtures: alkyl dimethicone, phenyl trimethicone, and polyoxyethylene sorbitan monostearate; and cetostearyl polyoxyethylene ether and ethylene oxide/propylene oxide copolymer...
May 2016: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28333341/systemic-administration-of-sialorphin-attenuates-experimental-colitis-in-mice-via-interaction-with-mu-and-kappa-opioid-receptors
#9
M Salaga, A Mokrowiecka, D Jacenik, A I Cygankiewicz, E Malecka-Panas, R Kordek, W M Krajewska, M K Sobocinska, E Kamysz, J Fichna
Background and Aims: Pharmacological treatment and/or maintenance of remission in inflammatory bowel disease (IBD) is currently one of the biggest challenges in the field of gastroenterology. Here we aimed to assess the anti-inflammatory effect and the mechanism of action of sialorphin, the natural blocker of the endogenous opioid peptide-degrading enzymes neprilysin (NEP) and aminopeptidase N (APN), in the mouse models of IBD and the changes in the expression of these enzymes in IBD patients...
March 18, 2017: Journal of Crohn's & Colitis
https://www.readbyqxmd.com/read/28333316/convergent-balancing-selection-on-the-mu-opioid-receptor-in-primates
#10
Carolyn G Sweeney, Juliette M Rando, Helen N Panas, Gregory M Miller, Donna M Platt, Eric J Vallender
The mu opioid receptor is involved in many natural processes including stress response, pleasure, and pain. Mutations in the gene also have been associated with opiate and alcohol addictions as well as with responsivity to medication targeting these disorders. Two common and mutually exclusive polymorphisms have been identified in humans, A118G (N40D), found commonly in non-African populations, and C17T (V6A), found almost exclusively in African populations. While A118G has been studied extensively for associations and in functional assays, C17T is much less well understood...
March 15, 2017: Molecular Biology and Evolution
https://www.readbyqxmd.com/read/28332577/absence-of-role-of-dietary-protein-sensing-in-the-metabolic-benefits-of-duodenal-jejunal-bypass-in-the-mouse
#11
Aude Barataud, Daisy Goncalves, Jennifer Vinera, Carine Zitoun, Adeline Duchampt, Amandine Gautier-Stein, Gilles Mithieux
Roux-en-Y gastric bypass (RYGB) induces remission or substantial improvement of type 2 diabetes mellitus (T2D) but underlying mechanisms are still unclear. The beneficial effects of dietary proteins on energy and glucose homeostasis are mediated by the antagonist effects of peptides toward mu-opioid receptors (MORs), which are highly expressed in the distal gut. We hypothesized that the beneficial effects of RYGB could depend at least in part on the interaction of peptides from food with intestinal MORs. Duodenal-jejunal bypass (DJB) was performed in obese and lean wild-type (WT) or MOR deficient (MOR(-/-)) mice...
March 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28328199/fentanyl-initiated-polymers-prepared-by-atrp-for-targeted-delivery
#12
Devora Cohen-Karni, Marina Kovaliov, Shaohua Li, Stephen Jaffee, Nestor D Tomycz, Saadyah Averick
The targeted delivery of polymers to neurons is a challenging yet important goal for polymer based drug delivery. We prepared a fentanyl based atom transfer radical polymerization (ATRP) initiator to target the Mu opioid receptor (MOR) for neuronal targeting. We incorporated our recently discovered rigid acrylate linking group into the initiator to retain a high degree of binding to the MOR and grafted random or block copolymers of poly(oligo(ethylene oxide) methacrylate)-block-(glycidyl methacrylate). Trifluoroethanol promoted amine ring opening of the glycidyl methacrylate was used for post-polymerization modification of the fentanyl initiated polymers to attach a near-infrared fluorescent dye (ADS790WS) or to build a targeted siRNA delivery system via modification with secondary amines...
March 22, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28328155/does-dynorphin-play-a-role-in-the-onset-of-puberty-in-female-sheep
#13
J A Lopez, M N Bedenbaugh, R B McCosh, P W Weems, L J Meadows, B Wisman, L M Coolen, R L Goodman, S M Hileman
Puberty onset involves increased gonadotrophin-release (GnRH) release as a result of decreased sensitivity to oestrogen (E2 )-negative feedback. Because GnRH neurones lack E2 receptor α, this pathway must contain interneurones. One likely candidate is KNDy neurones (kisspeptin, neurokinin B, dynorphin). The overarching hypothesis of the present study was that the prepubertal hiatus in luteinising hormone (LH) release involves reduced kisspeptin and/or heightened dynorphin input. We first tested the specific hypothesis that E2 would reduce kisspeptin-immunopositive cell numbers and increase dynorphin-immunopositive cell numbers...
December 2016: Journal of Neuroendocrinology
https://www.readbyqxmd.com/read/28327612/endogenous-opioids-regulate-moment-to-moment-neuronal-communication-and-excitability
#14
Bryony L Winters, Gabrielle C Gregoriou, Sarah A Kissiwaa, Oliver A Wells, Danashi I Medagoda, Sam M Hermes, Neil T Burford, Andrew Alt, Sue A Aicher, Elena E Bagley
Fear and emotional learning are modulated by endogenous opioids but the cellular basis for this is unknown. The intercalated cells (ITCs) gate amygdala output and thus regulate the fear response. Here we find endogenous opioids are released by synaptic stimulation to act via two distinct mechanisms within the main ITC cluster. Endogenously released opioids inhibit glutamate release through the δ-opioid receptor (DOR), an effect potentiated by a DOR-positive allosteric modulator. Postsynaptically, the opioids activate a potassium conductance through the μ-opioid receptor (MOR), suggesting for the first time that endogenously released opioids directly regulate neuronal excitability...
March 22, 2017: Nature Communications
https://www.readbyqxmd.com/read/28326568/early-response-predicts-a-sustained-response-to-eluxadoline-in-patients-with-irritable-bowel-syndrome-with-diarrhoea-in-two-phase-3-studies
#15
W D Chey, L S Dove, D A Andrae, P S Covington
BACKGROUND: The mixed μ- and κ-opioid receptor agonist and δ-opioid receptor antagonist, eluxadoline, is licensed in the USA for the treatment of irritable bowel syndrome with diarrhoea (IBS-D), based on the results of two large Phase 3 clinical trials. AIM: To understand the time course of treatment benefits with eluxadoline by comparing responder rates over the first month of treatment with responder rates over longer treatment intervals. METHODS: In this post hoc analysis of two Phase 3 studies, composite and adequate relief (AR) responder rates were calculated over month 1 and patients were stratified by their responder status...
March 22, 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28325819/new-connections-getting-the-good-without-the-bad-opiate-edition
#16
Wei Wong
Researchers identify strategies to limit the adverse effects and liabilities of opioid receptor-targeting drugs.
March 21, 2017: Science Signaling
https://www.readbyqxmd.com/read/28325149/low-dose-naltrexone-in-the-treatment-of-fibromyalgia
#17
Samy K Metyas, Karen Yeter, John Solyman, Daniel Arkfeld
Fibromyalgia is a chronic pain disorder characterized by diffuse musculoskeletal pain, fatigue, sleep disturbance and cognitive impairment. A significant number of fibromyalgia patients do not respond adequately to the current drugs (pregabalin, milnacipran, duloxetine) approved for fibromyalgia treatment by the Food and Drug Administration (FDA). Thus, there is still a need for adjunctive therapies. Naltrexone is an opioid receptor antagonist used to treat alcohol and opioid dependence. It is hypothesized that low dose naltrexone causes transient blockade of opioid receptors centrally resulting in a rebound of endorphin function which may attenuate pain in fibromyalgia...
March 21, 2017: Current Rheumatology Reviews
https://www.readbyqxmd.com/read/28322978/delta-opioid-receptor-antagonism-leads-to-excessive-ethanol-consumption-in-mice-with-enhanced-activity-of-the-endogenous-opioid-system
#18
Piotr Poznanski, Anna Lesniak, Michal Korostynski, Klaudia Szklarczyk, Marzena Lazarczyk, Piotr Religa, Magdalena Bujalska-Zadrozny, Bogdan Sadowski, Mariusz Sacharczuk
The opioid system modulates the central reinforcing effects of ethanol and participates in the etiology of addiction. However, the pharmacotherapy of ethanol dependence targeted on the opioid system is little effective and varies due to individual patients' sensitivity. In the present study, we used two mouse lines with high (HA) and low (LA) activity of the endogenous opioid system to analyze the effect of opioid receptor blockade on ethanol drinking behavior. We found that LA and HA lines characterized by divergent magnitudes of swim stress-induced analgesia also differ in ethanol intake and preference...
March 18, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28322465/opioid-substitution-therapy-or-hidden-opioids-are-a-minefield-for-nalmefene-an-atypical-case-series-of-11-patients-in-lorraine
#19
Melissa Yéléhé-Okouma, Hervé Martini, Jérémie Lemarié, Pierre Labroca, Nadine Petitpain, Valérie Gibaja, François Paille, Pierre Gillet
Opioid antagonists such as naltrexone and nalmefene are used in drug therapy for alcoholism. Nalmefene, approved in Europe in February 2013 for the reduction of alcohol consumption is used in patients with alcohol dependence. We report 11 cases of opioid withdrawal syndrome after a single dose of nalmefene in patients usually treated with methadone, buprenorphine, but also with fentanyl or loperamide. Nalmefene is both a partial agonist and an antagonist of opioid receptors. Regarding to its opioid antagonist activity, nalmefene is contraindicated in patients with an opioid treatment...
March 21, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28322170/utilizing-delta-opioid-receptors-and-peptides-for-cytoprotection-implications-in-stroke-and-other-neurological-disorders
#20
Marci G Crowley, M Grant Liska, Trenton Lippert, Sydney Coreya, Cesar V Borlongan
The opioid system has been elucidated as a potential target for therapy in a variety of neurological disorders including stroke. Delta opioid receptors have been revealed to pose an especially compelling biological function for new neuroprotective therapies. Two distinct therapeutic mechanisms have been characterized for delta opioid receptors s, namely, these receptors aid in maintaining ionic homeostasis and initiate endogenous neuroprotective pathways. Specific agonists of delta opioid receptors, such as (D-Ala2, D-Leu5) enkephalin (DADLE), have displayed the ability to promote neuronal survival and mitigate apoptotic pathways...
March 20, 2017: CNS & Neurological Disorders Drug Targets
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