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mu-opioid receptor

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https://www.readbyqxmd.com/read/28807672/pharmacological-characterization-of-novel-synthetic-opioids-nso-found-in-the-recreational-drug-marketplace
#1
REVIEW
Michael H Baumann, Susruta Majumdar, Valerie Le Rouzic, Amanda Hunkele, Rajendra Uprety, Xi Ping Huang, Jin Xu, Bryan L Roth, Ying-Xian Pan, Gavril W Pasternak
Novel synthetic opioids (NSO) are increasingly encountered in illicit heroin and counterfeit pain pills. Many NSO are resurrected from older biomedical literature or patent applications, so limited information is available about their biological effects. Here we examined the pharmacology of three structurally-distinct NSO found in the recreational drug market: N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylbutyramide (butyrylfentanyl), 3,4-dichloro-N-[(1R,2R)-2-(dimethylamino)cyclohexyl]-N-methylbenzamide (U-47700) and 1-cyclohexyl-4-(1,2-diphenylethyl)piperazine (MT-45)...
August 11, 2017: Neuropharmacology
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
#2
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/28796483/placement-of-hydroxy-moiety-on-pendant-of-peptidomimetic-scaffold-modulates-mu-and-kappa-opioid-receptor-efficacy
#3
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
#4
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/28782637/synthesis-and-activity-of-opioid-peptidomimetics-with-%C3%AE-2-and-%C3%AE-3-amino-acids
#5
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/28780411/increased-ethanol-drinking-in-humanized-mice-expressing-the-mu-opioid-receptor-a118g-polymorphism-are-mediated-through-sex-specific-mechanisms
#6
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
https://www.readbyqxmd.com/read/28747384/feeding-releases-endogenous-opioids-in-humans
#7
Jetro J Tuulari, Lauri Tuominen, Femke de Boer, Jussi Hirvonen, Semi Helin, Pirjo Nuutila, Lauri Nummenmaa
The endogenous opioid system supports a multitude of functions related to appetitive behaviour and feeding in humans and animals, and it has been proposed to support hedonic aspects of feeding thus contributing to development of obesity. Here we used positron emission tomography (PET) to investigate whether feeding results in hedonia-dependent endogenous opioid release in humans. Ten healthy males were recruited for the study. They were scanned with mu-opioid specific ligand [(11)C]carfentanil three times: following a palatable meal, a non-palatable meal, and after an overnight fast...
July 26, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28745394/opioids-for-chronic-non-cancer-pain-in-children-and-adolescents
#8
REVIEW
Tess E Cooper, Emma Fisher, Andrew L Gray, Elliot Krane, Navil Sethna, Miranda Al van Tilburg, Boris Zernikow, Philip J Wiffen
BACKGROUND: Pain is a common feature of childhood and adolescence around the world, and for many young people, that pain is chronic. The World Health Organization guidelines for pharmacological treatments for children's persisting pain acknowledge that pain in children is a major public health concern of high significance in most parts of the world. While in the past, pain was largely dismissed and was frequently left untreated, views on children's pain have changed over time, and relief of pain is now seen as importantWe designed a suite of seven reviews on chronic non-cancer pain and cancer pain (looking at antidepressants, antiepileptic drugs, non-steroidal anti-inflammatory drugs, opioids, and paracetamol as priority areas) in order to review the evidence for children's pain utilising pharmacological interventions in children and adolescents...
July 26, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28743488/mu-opioid-receptor-biased-ligands-a-safer-and-painless-discovery-of-analgesics
#9
REVIEW
Abraham Madariaga-Mazón, Andrés F Marmolejo-Valencia, Yangmei Li, Lawrence Toll, Richard A Houghten, Karina Martinez-Mayorga
Biased activation of G-protein-coupled receptors (GPCRs) is shifting drug discovery efforts and appears promising for the development of safer drugs. The most effective analgesics to treat acute pain are agonists of the μ opioid receptor (μ-OR), a member of the GPCR superfamily. However, the analgesic use of opioid drugs, such as morphine, is hindered by adverse effects. Only a few μ-OR agonists have been reported to selectively activate the Gi over β-arrestin signaling pathway, resulting in lower gastrointestinal dysfunction and respiratory suppression...
July 22, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28742625/online-sales-of-unscheduled-pharmaceutical-agents-a-case-report-of-tianeptine-use-in-the-united-states
#10
Swapnil Gupta, Ryan Wallace, Jordan Sloshower
: Tianeptine is a tricyclic antidepressant that stimulates mu-opioid receptors at high doses. It is marketed and used across Europe and Latin America as an antidepressant, but is not approved by the Food and Drug Administration for use in the United States. In the United States, tianeptine is sold through online health stores as a cognition enhancer, dietary supplement, or as research chemical. We report the case of a 36-year-old man with a history of major depressive disorder, responsive to sertraline, who turned to the unmonitored use of tianeptine purchased online to treat residual feelings of apathy and boredom...
July 24, 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28734904/identifying-novel-members-of-the-wntless-interactome-through-genetic-and-candidate-gene-approaches
#11
Jessica Petko, Trevor Tranchina, Goral Patel, Robert Levenson, Stephanie Justice-Bitner
Wnt signaling is an important pathway that regulates several aspects of embryogenesis, stem cell maintenance, and neural connectivity. We have recently determined that opioids decrease Wnt secretion, presumably by inhibiting the recycling of the Wnt trafficking protein Wntless (Wls). This effect appears to be mediated by protein-protein interaction between Wls and the mu-opioid receptor (MOR), the primary cellular target of opioid drugs. The goal of this study was to identify novel protein interactors of Wls that are expressed in the brain and may also play a role in reward or addiction...
July 20, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28699350/analgesic-properties-of-opioid-nk1-multitarget-ligands-with-distinct-in-vitro-profiles-in-naive-and-chronic-constriction-injury-mice
#12
Joanna Starnowska, Roberto Costante, Karel Guillemyn, Katarzyna Popiolek-Barczyk, Nga N Chung, Carole Lemieux, Attila Keresztes, Joost Van Duppen, Adriano Mollica, John Streicher, Jozef Vanden Broeck, Peter W Schiller, Dirk Tourwé, Joanna Mika, Steven Ballet, Barbara Przewlocka
The lower efficacy of opioids in neuropathic pain may be due to the increased activity of pronociceptive systems such as substance P. We present evidence to support this hypothesis in this work from the spinal cord in a neuropathic pain model in mice. Biochemical analysis confirmed the elevated mRNA and protein level of pronociceptive substance P, the major endogenous ligand of the neurokinin-1 (NK1) receptor, in the lumbar spinal cord of chronic constriction injury (CCI)-mice. To improve opioid efficacy in neuropathic pain, novel compounds containing opioid agonist and neurokinin 1 (NK1) receptor antagonist pharmacophores were designed...
July 26, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28674470/eluxadoline-viberzi-a-mu-opioid-receptor-agonist-for-the-treatment-of-irritable-bowel-syndrome-with-diarrhea
#13
Fraidy Maltz, Brooke Fidler
Eluxadoline (Viberzi) for the treatment of irritable bowel syndrome with diarrhea.
July 2017: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/28673713/alterations-in-opioid-inhibition-cause-widespread-nociception-but-do-not-affect-anxiety-like-behavior-in-oral-cancer-mice
#14
Yi Ye, Daniel G Bernabé, Elizabeth Salvo, Chi T Viet, Kentaro Ono, John C Dolan, Malvin Janal, Brad E Aouizerat, Christine Miaskowski, Brian L Schmidt
Widespread pain and anxiety are commonly reported in cancer patients. We hypothesize that cancer is accompanied by attenuation of endogenous opioid-mediated inhibition, which subsequently causes widespread pain and anxiety. To test this hypothesis we used a mouse model of oral squamous cell carcinoma (SCC) in the tongue. We found that mice with tongue SCC exhibited widespread nociceptive behaviors in addition to behaviors associated with local nociception that we reported previously. Tongue SCC mice exhibited a pattern of reduced opioid receptor expression in the spinal cord; intrathecal administration of respective mu (MOR), delta (DOR), and kappa (KOR) opioid receptor agonists reduced widespread nociception in mice, except for the fail flick assay following administration of the MOR agonist...
June 30, 2017: Neuroscience
https://www.readbyqxmd.com/read/28667175/the-relevance-of-agrp-neuron-derived-gaba-inputs-to-pomc-neurons-differs-for-spontaneous-and-evoked-release
#15
Andrew R Rau, Shane T Hentges
Hypothalamic agouti-related peptide (AgRP) neurons potently stimulate food intake, whereas proopiomelanocortin (POMC) neurons inhibit feeding. Whether AgRP neurons exert their orexigenic actions, at least in part, by inhibiting anorexigenic POMC neurons remains unclear. Here, the connectivity between GABA-releasing AgRP neurons and POMC neurons was examined in brain slices from male and female mice. Spontaneous GABA-mediated inhibitory postsynaptic currents (sIPSCs) in POMC neurons were unaffected by disturbing GABA release from AgRP neurons either by cell-type-specific deletion of the vesicular GABA transporter or by expression of botulinum toxin in AgRP neurons to prevent VAMP2-dependent vesicle fusion...
June 30, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28659791/pentazocine-protects-sn4741-cells-against-mpp-induced-cell-damage-via-up-regulation-of-the-canonical-wnt-%C3%AE-catenin-signaling-pathway
#16
Jiancai Wang, Jintao Gu, Hao Wu, Gang Zhu, Dayun Feng, Yuqian Li, Wei Guo, Keyong Tian, Guodong Gao, Li Gao
The Wnt/β-catenin signaling pathway has been linked to many neurodegenerative diseases including Parkinson's disease (PD). A glycoprotein named Dickkopf-1 (Dkk1) can combine with the receptor complex on cell membrane to inhibit Wnt/β-catenin signaling. Opioids, a series of compounds including morphine, fentanyl and pentazocine, have been reported to contribute to the up-regulation of Wnt/β-catenin signaling. Naloxone is an antagonist that has been used as an antidote to opioids through mu-opioid receptor...
2017: Frontiers in Aging Neuroscience
https://www.readbyqxmd.com/read/28653080/alterations-of-expression-of-inflammation-immune-related-genes-in-the-dorsal-and-ventral-striatum-of-adult-c57bl-6j-mice-following-chronic-oxycodone-self-administration-a-rna-sequencing-study
#17
Yong Zhang, Yupu Liang, Orna Levran, Matthew Randesi, Vadim Yuferov, Connie Zhao, Mary Jeanne Kreek
INTRODUCTION: Non-medical use of prescription opioids such as the mu opioid receptor (MOP-r) agonist oxycodone is a growing problem in the USA and elsewhere. There is limited information about oxycodone's impact on diverse gene systems in the brain. OBJECTIVES: The current study was designed to examine how chronic oxycodone self-administration (SA) affects gene expression in the terminal areas of the nigrostriatal and mesolimbic dopaminergic pathways in mice. METHOD: Adult male C57BL/6J mice underwent a 14-day oxycodone self-administration procedure (4 h/day, 0...
August 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28650467/genome-wide-loss-of-function-genetic-screening-identifies-opioid-receptor-%C3%AE-1-as-a-key-regulator-of-l-asparaginase-resistance-in-pediatric-acute-lymphoblastic-leukemia
#18
S M Kang, J L Rosales, V Meier-Stephenson, S Kim, K Y Lee, A Narendran
L-asparaginase is a critical chemotherapeutic agent for acute lymphoblastic leukemia (ALL). It hydrolyzes plasma asparagine into aspartate and NH3, causing asparagine deficit and inhibition of protein synthesis and eventually, leukemic cell death. However, patient relapse often occurs due to development of resistance. The molecular mechanism by which ALL cells acquire resistance to L-asparaginase is unknown. Therefore, we sought to identify genes that are involved in L-asparaginase resistance in primary leukemic cells...
June 26, 2017: Oncogene
https://www.readbyqxmd.com/read/28645621/two-delta-opioid-receptor-subtypes-are-functional-in-single-ventral-tegmental-area-neurons-and-can-interact-with-the-mu-opioid-receptor
#19
Elyssa B Margolis, Wakako Fujita, Lakshmi A Devi, Howard L Fields
The mu and delta opioid receptors (MOR and DOR) are highly homologous members of the opioid family of GPCRs. There is evidence that MOR and DOR interact, however the extent to which these interactions occur in vivo and affect synaptic function is unknown. There are two stable DOR subtypes: DPDPE sensitive (DOR1) and deltorphin II sensitive (DOR2); both agonists are blocked by DOR selective antagonists. Robust motivational effects are produced by local actions of both MOR and DOR ligands in the ventral tegmental area (VTA)...
June 21, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28642332/morphine-worsens-the-severity-and-prevents-pancreatic-regeneration-in-mouse-models-of-acute-pancreatitis
#20
Usman Barlass, Raini Dutta, Hassam Cheema, John George, Archana Sareen, Ajay Dixit, Zuobiao Yuan, Bhuwan Giri, Jingjing Meng, Santanu Banerjee, Sulagna Banerjee, Vikas Dudeja, Rajinder K Dawra, Sabita Roy, Ashok K Saluja
BACKGROUND: Opioids such as morphine are widely used for the management of pain associated with acute pancreatitis. Interestingly, opioids are also known to affect the immune system and modulate inflammatory pathways in non-pancreatic diseases. However, the impact of morphine on the progression of acute pancreatitis has never been evaluated. In the current study, we evaluated the impact of morphine on the progression and severity of acute pancreatitis. METHODS: Effect of morphine treatment on acute pancreatitis in caerulein, L-arginine and ethanol-palmitoleic acid models was evaluated after induction of the disease...
June 22, 2017: Gut
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