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µ Opioid Receptors

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https://www.readbyqxmd.com/read/29473323/adult-spinal-opioid-receptor-%C3%A2%C2%B51-expression-after-incision-is-altered-by-early-life-repetitive-tactile-and-noxious-procedures-in-rats
#1
Nynke J van den Hoogen, Roel Ri van Reij, Jacob Patijn, Dick Tibboel, Elbert Aj Joosten
Clinical and experimental data suggests that noxious stimulation at critical stages of development results in long-term changes on nociceptive processing in later life. Here, we use an established, well-documented rat model of repetitive noxious procedures closely mimicking the clinical situation in the NICU. In order to understand molecular changes underlying the long-term consequences of repetitive stimulation of the developing nociceptive system the present study aims to analyse the presence of the µ-opioid-receptor-1 (OPRM1)...
February 22, 2018: Developmental Neurobiology
https://www.readbyqxmd.com/read/29461271/endothelin-signaling-contributes-to-modulation-of-nociception-in-early-stage-tongue-cancer-in-rats
#2
Akihiko Furukawa, Masamichi Shinoda, Asako Kubo, Kuniya Honda, Ryuta Akasaka, Yoshiyuki Yonehara, Koichi Iwata
BACKGROUND: Patients with early stage tongue cancer do not frequently complain of tongue pain. Endothelin-1 signaling is upregulated in the cancerous tongue at the early stage. We tested the hypothesis that endothelin-1 signaling contributes to the modulation of tongue nociception. METHODS: Squamous cell carcinoma cells were inoculated into the tongue under general anesthesia. Lingual mechanical sensitivity under light anesthesia using forceps from days 1 to 21 (n = 8) and the amounts of endothelin-1 and β-endorphin in the tongue on days 6, 14, and 21 (n = 5 to 7) were examined after the inoculation...
February 15, 2018: Anesthesiology
https://www.readbyqxmd.com/read/29451744/design-synthesis-and-biological-evaluation-of-novel-bivalent-ligands-targeting-dopamine-d2-like-receptors-and-%C3%A2%C2%B5-opioid-receptor
#3
Mingcheng Qian, Lakshmi Vasudevan, Jelle Huysentruyt, Martijn D P Risseeuw, Christophe Stove, Patrick M L Vanderheyden, Kathleen Van Craenenbroeck, Serge Van Calenbergh
Nowadays, there is mounting evidence that intermolecular receptor-receptor interactions may result in altered receptor recognition, pharmacology and signaling. Heterobivalent ligands have been proven useful molecular probes for confirming and targeting heteromeric receptors. This paper describes the design and synthesis of novel heterobivalent ligands for dopamine D2-like receptors (D2-likeR) and the µ opioid receptor (µOR) and their evaluation using radioactive ligand binding and functional assays.
February 16, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29427348/the-effect-of-tramadol-on-sneeze-induced-urethral-continence-reflex-through-%C3%AE-opioid-receptors-in-the-spinal-cord-in-rats
#4
Asuka Ashikari, Minoru Miyazato, Ryu Kimura, Takuma Oshiro, Seiichi Saito
AIMS: We examined the efficacy of tramadol on the urethral reflex during sneezing, as well as the role of µ-opioid receptors in the spinal cord, in rats. METHODS: Forty-one female Sprague-Dawley rats were used. The rats were divided into normal female rats and rats with vaginal distension (VD), which mimics stress urinary incontinence (SUI) in humans. Under urethane anesthesia, the sneeze-induced amplitude of urethral responses (AUR) and baseline pressure (BP) were examined after intravenous injection of tramadol using a microtransducer-tipped catheter in both rat groups...
February 10, 2018: Neurourology and Urodynamics
https://www.readbyqxmd.com/read/29419653/long-term-use-of-naldemedine-in-the-treatment-of-opioid-induced-constipation-in-patients-with-chronic-non-cancer-pain-a-randomized-double-blind-placebo-controlled-phase-3-study
#5
Lynn R Webster, Srinivas Nalamachu, Bart Morlion, Jyotsna Reddy, Yuko Baba, Tadaaki Yamada, Juan Camilo Arjona Ferreira
The long-term safety of naldemedine, a peripherally acting µ-opioid receptor antagonist, was evaluated in patients with opioid-induced constipation and chronic non-cancer pain in a 52-week, randomized, double-blind, phase 3 study. Eligible adults who could be on a routine laxative regimen were randomized 1:1 to receive once-daily oral naldemedine 0.2 mg (n = 623) or placebo (n = 623). The primary endpoint was summary measures of treatment-emergent adverse events (AEs). Additional endpoints included opioid withdrawal on the Clinical Opiate Withdrawal Scale and the Subjective Opiate Withdrawal Scale, pain intensity on Numeric Rating Scale, frequency of bowel movements, and constipation-related symptoms and quality of life on the Patient Assessment of Constipation Symptoms and Patient Assessment of Constipation Quality of Life scales, respectively...
February 6, 2018: Pain
https://www.readbyqxmd.com/read/29382866/modulation-of-neurally-mediated-vasodepression-and-bradycardia-by-electroacupuncture-through-opioids-in-nucleus-tractus-solitarius
#6
Stephanie C Tjen-A-Looi, Liang-Wu Fu, Zhi-Ling Guo, John C Longhurst
Stimulation of vagal afferent endings with intravenous phenylbiguanide (PBG) causes both bradycardia and vasodepression, simulating neurally mediated syncope. Activation of µ-opioid receptors in the nucleus tractus solitarius (NTS) increases blood pressure. Electroacupuncture (EA) stimulation of somatosensory nerves underneath acupoints P5-6, ST36-37, LI6-7 or G37-39 selectively but differentially modulates sympathoexcitatory responses. We therefore hypothesized that EA-stimulation at P5-6 or ST36-37, but not LI6-7 or G37-39 acupoints, inhibits the bradycardia and vasodepression through a µ-opioid receptor mechanism in the NTS...
January 30, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29378417/epigenetic-modifications-following-noxious-stimuli-in-infants
#7
Linda A Hatfield, Rebecca K Hoffman, Rosemary C Polomano, Yvette Conley
PURPOSE: To recruit healthy full- and preterm infants into genetic research and determine the effectiveness of a noninvasive DNA sampling technique for comparing epigenetic modifications. BACKGROUND: Noxious stimuli during a vulnerable period of infant neuronal plasticity may trigger long-term epigenetic changes affecting neurodevelopment, pain modulation, and reactivity. Recognizing epigenetic pain findings is problematic because parents are reluctant to enroll newborns into genetic research...
January 1, 2018: Biological Research for Nursing
https://www.readbyqxmd.com/read/29374492/prediction-of-opioid-dose-in-cancer-pain-patients-using-genetic-profiling-not-yet-an-option-with-support-vector-machine-learning
#8
Anne Estrup Olesen, Debbie Grønlund, Mikkel Gram, Frank Skorpen, Asbjørn Mohr Drewes, Pål Klepstad
OBJECTIVE: Use of opioids for pain management has increased over the past decade; however, inadequate analgesic response is common. Genetic variability may be related to opioid efficacy, but due to the many possible combinations and variables, statistical computations may be difficult. This study investigated whether data processing with support vector machine learning could predict required opioid dose in cancer pain patients, using genetic profiling. Eighteen single nucleotide polymorphisms (SNPs) within the µ and δ opioid receptor genes and the catechol-O-methyltransferase gene were selected for analysis...
January 27, 2018: BMC Research Notes
https://www.readbyqxmd.com/read/29340866/-in-silico-study-of-the-binding-of-two-novel-antagonists-to-the-nociceptin-receptor
#9
Stefano Della Longa, Alessandro Arcovito
Antagonists of the nociceptin receptor (NOP) are raising interest for their possible clinical use as antidepressant drugs. Recently, the structure of NOP in complex with some piperidine-based antagonists has been revealed by X-ray crystallography. In this study, a multi-flexible docking (MF-docking) procedure, i.e. docking to multiple receptor conformations extracted by preliminary molecular dynamics trajectories, together with hybrid quantum mechanics/molecular mechanics (QM/MM) simulations have been carried out to provide the binding mode of two novel NOP antagonists, one of them selective (BTRX-246040, formerly named LY-2940094) and one non selective (AT-076), i...
January 16, 2018: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/29334500/overexpression-of-%C3%A2%C2%B5-opioid-receptors-in-peripheral-afferents-but-not-in-combination-with-enkephalin-decreases-neuropathic-pain-behavior-and-enhances-opioid-analgesia-in-mouse
#10
Amanda H Klein, Husam K Mohammad, Rabiah Ali, Brad Peper, Steven P Wilson, Srinivasa N Raja, Matthias Ringkamp, Sarah Sweitzer
BACKGROUND: The current study used recombinant herpes simplex virus type I to increase expression of µ-opiate receptors and the opioid ligand preproenkephalin in peripheral nerve fibers in a mouse model of neuropathic pain. It was predicted that viral vector delivery of a combination of genes encoding the µ-opioid receptor and preproenkephalin would attenuate neuropathic pain and enhance opioid analgesia. The behavioral effects would be paralleled by changes in response properties of primary afferent neurons...
January 15, 2018: Anesthesiology
https://www.readbyqxmd.com/read/29332567/nociceptin-orphanin-fq-peptide-nop-receptor-modulators-an-update-in-structure-activity-relationships
#11
Carlo Mustazza, Stefano Pieretti, Francesca Marzoli
Nociceptin /Orphanin FQ Peptide" receptor (NOPr) is a G-protein-coupled receptor with the nociceptin/orphanin FQ peptide (N/OFQ) as endogenous agonist. It is expressed in the nervous system as well as in some non-neural tissues. Its activation has pronociceptive effect at the supraspinal level, whereas at the spinal level it produces nociceptive effects at low doses and antinociceptive effects at higher doses. NOPr is also involved in mood and blood pressure regulation, immunoregulation, airway constriction, feeding, urination, bowel motility, learning and memory...
January 10, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29317054/promising-horizon-to-alleviate-alzeheimer-s-disease-pathological-hallmarks-via-inhibiting-mtor-signaling-pathway-a-new-application-for-a-commonplace-analgesic
#12
Leila Pourtalebi Jahromi, Zahra Sasanipour, Amir Azadi
Alzheimer's disease (AD) is a very prevalent and burdensome disease of elderlies but albeit extensive studies, mechanisms underlying its pathology and consequently its definite treatment is ambiguous. Intra and extra-cellular aggregation of abnormal proteins and impaired autophagy machinery, two closely related events taking place in AD brains proposed to be directly controlled by mTOR signaling pathway. On the other hand, tramadol that is a very well tolerated opioid analgesic has been revealed to inhibit mTOR upstream controllers through interaction with specific types of muscarinic, serotonergic, nicotinic and NMDA receptors, although it seems to induce the opposite effect via µ-opioid receptor...
January 2018: Medical Hypotheses
https://www.readbyqxmd.com/read/29302220/a-brief-review-of-the-genetics-and-pharmacogenetics-of-opioid-use-disorders
#13
Wade Berrettini
Increased physician prescribing of opioids to treat chronic nonprogressive pain has been accompanied by an increase in opioid addiction. Twin studies of opioid addiction are consistent with an inherited component of risk, approximately 50%. Several genome-wide association study (GWAS) reports indicate that genetic risk for opioid addiction is conveyed by many alleles of small effect (odds ratios <1.5). These reports have detected alleles in potassium-ion-channel genes (KCNC1 and KCNG2) and in a glutamate receptor auxiliary protein (CNIH3)...
September 2017: Dialogues in Clinical Neuroscience
https://www.readbyqxmd.com/read/29211767/investigating-endogenous-%C3%A2%C2%B5-opioid-receptors-in-human-keratinocytes-as-pharmacological-targets-using-novel-fluorescent-ligand
#14
Cheryl Leong, Christine Neumann, Srinivas Ramasamy, Bhimsen Rout, Lim Yi Wee, Mei Bigliardi-Qi, Paul L Bigliardi
Opioids in skin function during stress response, regeneration, ageing and, particularly in regulating sensation. In chronic pruritus, topical treatment with Naltrexone changes μ-opioid receptor (μ-OR) localization to relieve itch. The molecular mechanisms behind the effects of Naltrexone on μ-OR function in reduction of itching behavior has not been studied. There is an immediate need to understand the endogenous complexity of μ-OR dynamics in normal and pathological skin conditions. Here we evaluate real-time behavior of μ-OR-Endomorphine complexes in the presence of agonist and antagonists...
2017: PloS One
https://www.readbyqxmd.com/read/29165386/alterations-in-rat-accumbens-endocannabinoid-and-gaba-content-during-fentanyl-treatment-the-role-of-ghrelin
#15
Magdalena Sustkova-Fiserova, Chrysostomos Charalambous, Tereza Havlickova, Marek Lapka, Pavel Jerabek, Nina Puskina, Kamila Syslova
The opioid-induced rise of extracellular dopamine, endocannabinoid anandamide and γ-aminobutyric acid (GABA) concentrations triggered by opioids in the nucleus accumbens shell (NACSh) most likely participate in opioid reward. We have previously demonstrated that systemic administration of ghrelin antagonist (JMV2959) significantly decreased morphine-induced dopamine and anandamide (N-arachidonoylethanolamine, AEA) increase in the NACSh. Fentanyl is considered as a µ-receptor-selective agonist. The aim of this study was to test whether JMV2959, a growth hormone secretagogue receptor (GHS-R1A) antagonist, can influence the fentanyl-induced effects on anandamide, 2-arachidonoylglycerol (2-AG) and GABA in the NACSh and specify the involvement of GHS-R1A located in the ventral tegmental area (VTA) and nucleus accumbens (NAC)...
November 22, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29141251/opioid-receptors-contribute-to-antinociceptive-effect-of-tianeptine-on-colorectal-distension-induced-visceral-pain-in-rats
#16
S Sırrı Bilge, Fatih İlkaya, Özge Darakcı, Engin Çiftcioğlu, Ayhan Bozkurt
Tianeptine is a clinically effective atypical antidepressant with distinct neurochemical properties. In this study, we aimed to investigate the contribution of opioid receptors in the antinociceptive effect of tianeptine on visceral pain in awake rats and to differentiate the subtype and the localization (central and/or peripheral) of these opioid receptors involved in this antinociception. Visceromotor response to noxious colorectal distension (CRD) was quantified with electromyographic recordings, obtained from previously implanted electrodes into the external oblique musculature of rats under anesthesia, before and after tianeptine administration...
November 15, 2017: Pharmacology
https://www.readbyqxmd.com/read/29132133/endomorphins-promising-endogenous-opioid-peptides-for-the-development-of-novel-analgesics
#17
Zheng-Hui Gu, Bo Wang, Zhen-Zhen Kou, Yang Bai, Tao Chen, Yu-Lin Dong, Hui Li, Yun-Qing Li
Endomorphin-1 (EM1) and endomorphin-2 (EM2) are two endogenous ligands that belong to the opioid peptide family and have the highest affinity and selectivity for the µ-opioid receptor (MOR). The neuroanatomical distribution, ultrastructural features and neural circuitry of EM-containing neuronal structures have been morphologically demonstrated. In addition, the modulation effects of the EMs in different areas reflect their potential endogenous roles in many major physiological processes, including their remarkable roles in the transmission and modulation of noxious information...
November 13, 2017: Neuro-Signals
https://www.readbyqxmd.com/read/29127441/verification-of-a-genetic-locus-for-methamphetamine-intake-and-the-impact-of-morphine
#18
Emily C Eastwood, Amy J Eshleman, Aaron Janowsky, Tamara J Phillips
A quantitative trait locus (QTL) on proximal chromosome (Chr) 10 accounts for > 50% of the genetic variance in methamphetamine (MA) intake in mice selectively bred for high (MAHDR) and low (MALDR) voluntary MA drinking. The µ-opioid receptor (MOP-r) gene, Oprm1, resides at the proximal end of Chr 10, and buprenorphine reduces MA intake in MAHDR mice. However, this drug has only partial agonist effects at MOP-r. We investigated the impact of a full MOP-r agonist, morphine, on MA intake and saccharin intake, measured MOP-r density and affinity in several brain regions of the MA drinking lines and their C57BL/6J (B6) and DBA/2J (D2) progenitor strains, and measured MA intake in two congenic strains of mice to verify the QTL and reduce the QTL interval...
November 10, 2017: Mammalian Genome: Official Journal of the International Mammalian Genome Society
https://www.readbyqxmd.com/read/29092627/evidence-based-review-of-pharmacotherapy-for-opioid-induced-constipation-in-noncancer-pain
#19
Julie A Murphy, Erica A Sheridan
OBJECTIVE: To summarize and evaluate the existing literature regarding medications to treat opioid-induced constipation (OIC) in patients with chronic noncancer pain (CNCP). DATA SOURCES: PubMed, EMBASE, and Web of Science were searched using the following terms: constipation, opioid, chronic, pain, noncancer, nonmalignant, methylnaltrexone, alvimopan, lubiprostone, naloxegol, and naldemedine. STUDY SELECTION AND DATA EXTRACTION: The search was limited to randomized controlled trials reporting human outcomes...
October 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/29090081/eluxadoline-in-irritable-bowel-syndrome-with-diarrhea-rationale-evidence-and-place-in-therapy
#20
REVIEW
Kenneth Barshop, Kyle Staller
Irritable bowel syndrome (IBS) is the most common gastrointestinal (GI) disorder worldwide, however treatment options for diarrhea-predominant IBS (IBS-D) remain limited. Eluxadoline, a µ- and κ-opioid receptor agonist and δ-opioid receptor antagonist, was recently approved for the treatment of IBS-D. A novel compound first described in 2008, eluxadoline was shown to normalize GI transit, with a subsequent phase I demonstrating its safety and tolerability in healthy adults. In 2016, two randomized, double-blind, placebo-controlled phase III trials studying eluxadoline use at 75 mg and 100 mg twice daily over 26 weeks demonstrated a significant improvement in stool consistency and many global symptoms of IBS...
November 2017: Therapeutic Advances in Chronic Disease
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