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Mu Agonist

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https://www.readbyqxmd.com/read/29215139/a-novel-and-selective-nociceptin-receptor-nop-agonist-1-1-cis-4-isopropylcyclohexyl-piperidin-4-yl-1h-indol-2-yl-methanol-at-312-decreases-acquisition-of-ethanol-induced-conditioned-place-preference-in-mice
#1
Nurulain T Zaveri, Paul V Marquez, Michael E Meyer, Willma E Polgar, Abdul Hamid, Kabirullah Lutfy
BACKGROUND: Nociceptin/Orphanin FQ (N/OFQ), the endogenous peptide agonist for the opioid receptor-like (ORL1) receptor (also known as NOP or the nociceptin receptor), has been shown to block the acquisition and expression of ethanol-induced conditioned place preference (CPP). Here, we report the characterization of a novel small-molecule NOP ligand AT-312 (1-(1-((cis)-4-isopropylcyclohexyl)piperidin-4-yl)-1H-indol-2-yl)methanol) in receptor binding and GTPγS functional assays in vitro...
December 7, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29197517/dpi-289-a-novel-mixed-delta-opioid-agonist-mu-opioid-antagonist-dama-has-l-dopa-sparing-potential-in-parkinson-s-disease
#2
Tom H Johnston, Eboo Versi, Patrick A Howson, Paula Ravenscroft, Susan H Fox, Michael P Hill, Bruce E Reidenberg, Ronald Corey, Jonathan M Brotchie
L-DOPA-induced dyskinesia (LID) remains a significant problem in the management of Parkinson's disease (PD). In rodent and macaque models of PD, delta opioid receptor agonists have anti-parkinsonian actions while mu opioid antagonists can reduce the expression of LID. DPI-289 is a novel molecule with a unique combination of opioid receptor DAMA actions: delta agonist (Ki: 0.73 nM); mu antagonist (Ki: 12 nM). We demonstrated that DPI-289 has oral bioavailability and established its pharmacokinetic profile in both rat and primate...
November 29, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29196181/cyclopeptide-dmt-d-lys-p-cf3-phe-phe-asp-nh2-a-novel-g-protein-biased-agonist-of-the-mu-opioid-receptor
#3
Justyna Piekielna-Ciesielska, Federica Ferrari, Girolamo Calo', Anna Janecka
Opioid peptides and alkaloid drugs such as morphine, mediate their analgesic effects, but also undesired side effects, mostly through activation of the mu opioid receptor which belongs to the G protein-coupled receptor (GPCR) family. A new important pharmacological concept in the field of GPCRs is biased agonism. Two mu receptor ligands, Dmt-c[D-Lys-Phe-Phe-Asp]NH2 (C-36) and Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 (F-81), were evaluated in terms of their ability to promote or block mu receptor/G protein and mu receptor/β-arrestin interactions...
November 28, 2017: Peptides
https://www.readbyqxmd.com/read/29191857/evaluation-of-11c-me-nb1-as-a-potential-pet-radioligand-for-measuring-glun2b-containing-nmda-receptors-drug-occupancy-and-receptor-crosstalk
#4
Stefanie D Krämer, Thomas Betzel, Linjing Mu, Ahmed Haider, Adrienne Herde Müller, Anna K Boninsegni, Claudia Keller, Marina Szermerski, Roger Schibli, Bernhard Wünsch, Simon M Ametamey
Clinical and preclinical research with modulators binding to the NMDA receptor GluN2B N-terminal domain (NTD) aim for the treatment of various neurological diseases. However, the interpretation of the results is hampered by the lack of a suitable NMDA PET tracer for assessing the receptor occupancy of candidate drugs. We have developed [11C]Me-NB1 as a PET tracer for imaging GluN1/GluN2B-containing NMDA receptors and used it to investigate in rats the dose-dependent receptor occupancy of eliprodil, a GluN2B NTD modulator...
November 30, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29183835/antinociceptive-effects-of-mixtures-of-mu-opioid-receptor-agonists-and-cannabinoid-receptor-agonists-in-rats-impact-of-drug-and-fixed-dose-ratio
#5
David R Maguire, Charles P France
Pain is a significant clinical problem, and there is a need for effective pharmacotherapies with fewer adverse effects than currently available drugs (e.g., mu opioid receptor agonists). Cannabinoid receptor agonists enhance the antinociceptive effects of mu opioid receptor agonists, but it remains unclear which drugs and in what proportion will yield the most effective and safest treatments. The antinociceptive effects of the mu opioid receptor agonists etorphine and morphine alone and in combination with the cannabinoid receptor agonists Δ9-THC and CP55940 were studied in male Sprague-Dawley rats (n=16) using a warm water tail withdrawal procedure...
November 25, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29180970/cebranopadol-a-mixed-opioid-agonist-reduces-cocaine-self-administration-through-nociceptin-opioid-and-mu-opioid-receptors
#6
Qianwei Shen, Yulin Deng, Roberto Ciccocioppo, Nazzareno Cannella
Cocaine addiction is a widespread psychiatric condition still waiting for approved efficacious medications. Previous studies suggested that simultaneous activation of nociceptin opioid (NOP) and mu opioid (MOP) receptors could be a successful strategy to treat cocaine addiction, but the paucity of molecules co-activating both receptors with comparable potency has hampered this line of research. Cebranopadol is a non-selective opioid agonist that at nanomolar concentration activates both NOP and MOP receptors and that recently reached phase-III clinical trials for cancer pain treatment...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29155273/mu-opioid-peptide-mop-and-nociceptin-orphanin-fq-peptide-nop-receptor-activation-both-contribute-to-the-discriminative-stimulus-properties-of-cebranopadol-in-the-rat
#7
Thomas M Tzschentke, Kris Rutten
The novel potent analgesic cebranopadol is an agonist at nociceptin/orphanin FQ peptide (NOP) and classical opioid receptors, with the highest in-vitro activity at NOP and mu-opioid peptide (MOP) receptors, and somewhat lower activity at kappa-opioid peptide (KOP) and delta-opioid peptide (DOP) receptors. We addressed the question of which of these pharmacological activities contribute to the stimulus properties of cebranopadol using a rat drug discrimination procedure. First, cebranopadol was tested in generalization tests against a morphine cue, including receptor-specific antagonism...
November 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29149605/bias-factor-and-therapeutic-window-correlate-to-predict-safer-opioid-analgesics
#8
Cullen L Schmid, Nicole M Kennedy, Nicolette C Ross, Kimberly M Lovell, Zhizhou Yue, Jenny Morgenweck, Michael D Cameron, Thomas D Bannister, Laura M Bohn
Biased agonism has been proposed as a means to separate desirable and adverse drug responses downstream of G protein-coupled receptor (GPCR) targets. Herein, we describe structural features of a series of mu-opioid-receptor (MOR)-selective agonists that preferentially activate receptors to couple to G proteins or to recruit βarrestin proteins. By comparing relative bias for MOR-mediated signaling in each pathway, we demonstrate a strong correlation between the respiratory suppression/antinociception therapeutic window in a series of compounds spanning a wide range of signaling bias...
November 16, 2017: Cell
https://www.readbyqxmd.com/read/29143891/in-search-of-the-ideal-promotility-agent-optimal-use-of-currently-available-promotility-agents-for-nutrition-therapy-of-the-critically-ill-patient
#9
REVIEW
Sarah J Diamond, Endashaw Omer, Laszlo Kiraly
PURPOSE OF REVIEW: Enteral nutrition therapy is essential in the management of critically ill patients. Prokinetic agents have been used successfully to aid in the delivery of nutrition and improve feeding tolerance in patients in the intensive care unit (ICU). The aim of this report is to review the existing promotility agents available for use in the critically ill as well as outline the role of potential investigative drugs in order to provide a guide to the management of this difficult and important clinical dilemma...
November 16, 2017: Current Gastroenterology Reports
https://www.readbyqxmd.com/read/29110331/radioligands-for-positron-emission-tomography-imaging-of-cannabinoid-type-2-receptor
#10
Francesco Spinelli, Linjing Mu, Simon M Ametamey
The cannabinoid type 2 (CB2) receptor is an immunomodulatory receptor mainly expressed in peripheral cells and organs of the immune system. The expression level of CB2 in the central nervous system under physiological conditions is negligible, however under neuroinflammatory conditions an upregulation of CB2 protein or mRNA mainly co-localized with activated microglial cells has been reported. Consequently, CB2 agonists have been confirmed to play a role in neuroprotective and anti-inflammatory processes. A suitable PET radioligand for imaging CB2 would provide an invaluable research tool to explore the role of CB2 receptor expression in inflammatory disorders...
November 6, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29103850/length-changes-in-scapholunate-interosseous-ligament-with-resisted-wrist-radial-and-ulnar-inclination
#11
Jun Tan, Jing Chen, Shuai Mu, Jin Bo Tang, Marc Garcia-Elias
PURPOSE: To investigate the changes in length of the scapholunate interosseous ligament (SLIL) when the wrist is resisting horizontal lateral load and the forearm is in full pronation in vivo. METHODS: We obtained computed tomography scans of the wrists of 6 volunteers in 3 situations: 0° position (0° extension and 0° ulnar inclination) and full forearm pronation without force, and in the same position but with resisted ulnar and radial deviation. Nine zones of 3 subregions of the SLIL were measured and analyzed with computer modeling...
November 2, 2017: Journal of Hand Surgery
https://www.readbyqxmd.com/read/29097440/desensitization-and-tolerance-of-mu-opioid-receptors-on-pontine-kolliker-fuse-neurons
#12
Erica S Levitt, John T Williams
Acute desensitization of mu opioid receptors is thought to be an initial step in the development of tolerance to opioids. Given the resistance of the respiratory system to develop tolerance, desensitization of neurons in the Kölliker-Fuse (KF), a key area in the respiratory circuit, was examined. The activation of G protein-coupled inwardly rectifying potassium (GIRK) current was measured using whole-cell voltage-clamp recordings from KF and locus coeruleus (LC) neurons contained in acute rat brain slices...
November 2, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29073492/tianeptine-is-associated-with-lower-risk-of-suicidal-ideation-worsening-during-the-first-weeks-of-treatment-onset-compared-with-other-antidepressants-a-naturalistic-study
#13
B Nobile, I Jaussent, Ph Gorwood, J Lopez Castroman, E Olié, S Guillaume, Ph Courtet
Worsening of suicidal ideation during the first weeks of antidepressant treatment is a poorly understood phenomenon that prompted regulatory bodies to issue specific warnings. To better understand the causes of this phenomenon, this study compared the risk of suicidal ideation worsening in patients taking different types of antidepressant medications. To this aim, 4017 depressed adult outpatients were followed by general practitioners and psychiatrists throughout France for 6 weeks after prescription of an antidepressant treatment...
October 16, 2017: Journal of Psychiatric Research
https://www.readbyqxmd.com/read/29054390/oral-pioglitazone-ameliorates-fructose-induced-peripheral-insulin-resistance-and-hippocampal-gliosis-but-not-restores-inhibited-hippocampal-adult-neurogenesis
#14
Wen-Chung Liu, Chih-Wei Wu, You-Lin Tain, Mu-Hui Fu, Chun-Ying Hung, I-Chun Chen, Lee-Wei Chen, Kay L H Wu
Diet-associated insulin resistance (IR) is intimately correlated with the progression of metabolic syndrome and hippocampal dysfunction. Pioglitazone (PIO), a selective peroxisome proliferator-activated receptor gamma (PPARγ) agonist, has been applied to enhance insulin sensitivity. With limited permeability to blood-brain-barrier, it is unclear that whether oral PIO available to cure both the peripheral IR and the impairment in the hippocampus. We evaluated the levels of peripheral and hippocampal IR via the homeostatic model assessment of insulin resistance and hippocampal IRS-1/Akt phosphorylation, respectively, of Wistar Kyoto rats fed with a regular chew or high fructose diet (HFD) for 12weeks...
October 18, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29054370/accessibility-of-axonal-g-protein-coupled-mu-opioid-receptors-requires-conceptual-changes-of-axonal-membrane-targeting-for-pain-modulation
#15
Shaaban A Mousa, Mohammed Shaqura, Mohammed Al-Madol, Sascha Tafelski, Baled I Khalefa, Mehdi Shakibaei, Michael Schäfer
The mechanisms of axonal trafficking and membrane targeting are well established for sodium channels, which are the principle targets for perineurally applied local anaesthetics. However, they have not been thoroughly investigated for G protein coupled receptors such as mu-opioid receptors (MOR). Focusing on these axonal mechanisms, we found that axonal MOR functionality is quite distinct in two different pain states, i.e. hindpaw inflammation and nerve injury. We observed axonal membrane MOR binding and functional G protein coupling exclusively at sites of CCI nerve injury...
October 17, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29044528/endomorphins-potentiate-asic-currents-and-enhance-the-lactic-acid-mediated-increase-in-arterial-blood-pressure-effects-amplified-in-hindlimb-ischemia
#16
Mohamed Farrag, Julie K Drobish, Henry L Puhl, Joyce S Kim, Paul B Herold, Marc P Kaufman, Victor Ruiz-Velasco
Chronic muscle ischemia leads to accumulation of lactic acid and other inflammatory mediators with a subsequent drop in interstitial pH. Acid-sensing ion channels (ASICs), expressed in thin muscle afferents, sense the decrease in pH and evoke a pressor reflex known to increase mean arterial pressure. The naturally occurring endomorphins are also released by primary afferents under ischemic conditions. We examined whether high affinity mu opioid receptor (MOR) agonists, endomorphin-1 (E-1) and -2 (E-2), modulate ASIC currents and the lactic acid-mediated pressor reflex...
October 16, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/29040826/maintenance-on-naltrexone-amphetamine-decreases-cocaine-vs-food-choice-in-male-rhesus-monkeys
#17
Megan J Moerke, Matthew L Banks, Kejun Cheng, Kenner C Rice, S Stevens Negus
BACKGROUND: Cocaine use disorder remains a significant public health issue for which there are no FDA-approved pharmacotherapies. Amphetamine maintenance reduces cocaine use in preclinical and clinical studies, but the mechanism of this effect is unknown. Previous studies indicate a role for endogenous opioid release and subsequent opioid receptor activation in some amphetamine effects; therefore, the current study examined the role of mu-opioid receptor activation in d-amphetamine treatment effects in an assay of cocaine-vs-food choice...
December 1, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29029015/an-experimental-study-comparing-the-respiratory-effects-of-tapentadol-and-oxycodone-in-healthy-volunteers
#18
R van der Schrier, K Jonkman, M van Velzen, E Olofsen, A M Drewes, A Dahan, M Niesters
Background: There is a clinical need for potent opioids that produce little or no respiratory depression. In the current study we compared the respiratory effects of tapentadol, a mu-opioid receptor agonist and noradrenaline reuptake inhibitor, and oxycodone, a selective mu-opioid receptor agonist. We hypothesize that tapentadol 100 mg has a lesser effect on the control of breathing than oxycodone 20 mg. Methods: Fifteen healthy volunteers were randomized to receive oral tapentadol (100 and 150 mg), oxycodone 20 mg or placebo immediate release tablets in a crossover double-blind randomized design...
December 1, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/28989282/spotlight-on-eluxadoline-for-the-treatment-of-patients-with-irritable-bowel-syndrome-with-diarrhea
#19
REVIEW
Konstantinos C Fragkos
BACKGROUND: Irritable bowel syndrome with diarrhea (IBS-D) has limited options for treatment currently, including mainly anti-motility medications, antispasmodics, and antidepressants. This review discusses the properties of a new drug, eluxadoline, a gut-targeting mu- and kappa-opioid receptor agonist and a delta-opioid receptor antagonist, and its efficacy and safety in patients with IBS-D. MATERIALS AND METHODS: A systematic review of the literature was undertaken to identify studies that had investigated eluxadoline as a treatment in IBS-D...
2017: Clinical and Experimental Gastroenterology
https://www.readbyqxmd.com/read/28891868/bivalent-ligand-that-activates-mu-opioid-receptor-and-antagonizes-mglur5-receptor-reduces-neuropathic-pain-in-mice
#20
Cristina D Peterson, Kelley F Kitto, Eyup Akgün, Mary M Lunzer, Maureen S Riedl, Lucy Vulchanova, George L Wilcox, Philip S Portoghese, Carolyn A Fairbanks
The mu opioid receptor (MOR) and metabotropic glutamate receptor 5 (mGluR5) are well-established pharmacological targets in the management of chronic pain. Both receptors are expressed in the spinal cord. MMG22, a bivalent ligand containing 2 pharmacophores separated by 22 atoms, which simultaneously activates MOR and antagonizes mGluR5, has been shown to produce potent reversal of tactile hypersensitivity in rodent models of lipopolysaccharide (LPS)-and bone cancer-induced chronic pain. This study assessed whether intrathecal MMG22 also is effective in reducing pain of neuropathic origin...
December 2017: Pain
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