keyword
MENU ▼
Read by QxMD icon Read
search

µ Opioid Receptors

keyword
https://www.readbyqxmd.com/read/29649035/pharmacological-characterization-of-levorphanol-a-g-protein-biased-opioid-analgesic
#1
Valerie Le Rouzic, Ankita Narayan, Amanda Hunkle, Gina F Marrone, Zhigang Lu, Susruta Majumdar, Jin Xu, Ying-Xian Pan, Gavril W Pasternak
BACKGROUND: Levorphanol is a potent analgesic that has been used for decades. Most commonly used for acute and cancer pain, it also is effective against neuropathic pain. The recent appreciation of the importance of functional bias and the uncovering of multiple µ opioid receptor splice variants may help explain the variability of patient responses to different opioid drugs. METHODS: Here, we evaluate levorphanol in a variety of traditional in vitro receptor binding and functional assays...
April 11, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29615610/alcohol-exposure-disrupts-mu-opioid-receptor-mediated-long-term-depression-at-insular-cortex-inputs-to-dorsolateral-striatum
#2
Braulio Muñoz, Brandon M Fritz, Fuqin Yin, Brady K Atwood
Drugs of abuse, including alcohol, ablate the expression of specific forms of long-term synaptic depression (LTD) at glutamatergic synapses in dorsal striatum (DS), a brain region involved in goal-directed and habitual behaviors. This loss of LTD is associated with altered DS-dependent behavior. Given the role of the µ-opioid receptor (MOR) in behavioral responding for alcohol, we explored the impact of alcohol on various forms of MOR-mediated synaptic depression that we find are differentially expressed at specific DS synapses...
April 3, 2018: Nature Communications
https://www.readbyqxmd.com/read/29589831/cellular-tolerance-at-the-%C3%A2%C2%B5-opioid-receptor-is-phosphorylation-dependent
#3
Seksiri Arttamangkul, Daniel A Heinz, James R Bunzow, Xianqiang Song, John T Williams
Phosphorylation of the μ-opioid receptor (MOR) is known as a key step in desensitization and internalization but the role in the development of long-term tolerance at the cellular level is not known. Viral expression of wild type (exWT) and mutant MORs, where all phosphorylation sites on the C-terminus (Total Phosphorylation Deficient (TPD)) were mutated to alanine, were examined in locus coeruleus neurons in a MOR knockout rat. Both receptors activated potassium conductance similar to endogenous receptors in wild type animals...
March 28, 2018: ELife
https://www.readbyqxmd.com/read/29554653/endomorphin-2-inhibits-the-activity-of-the-spinoparabrachial-projection-neuron-through-presynaptic-mechanisms-in-the-spinal-dorsal-horn-in-rats
#4
Jun-Bin Yin, Ya-Cheng Lu, Ban Feng, Zhen-Yu Wu, Ying-Biao Chen, Ting Zhang, Zhen-Zhen Kou, Ming-Ming Zhang, Han Zhang, Jin-Lian Li, Hui Li, Tao Chen, Yu-Lin Dong, Yun-Qing Li
BACKGROUND/AIMS: Spinal dorsal horn (SDH) is one of the most important regions for analgesia produced by endomorphin-2 (EM2), which has a higher affinity and specificity for the µ-opioid receptor (MOR) than morphine. Many studies have focused on substantia gelatinosa (SG, lamina II) neurons to elucidate the cellular basis for its antinociceptive effects. However, the complicated types and local circuits of interneurons in the SG make it difficult to understand the real effects of EM2...
March 15, 2018: Neuro-Signals
https://www.readbyqxmd.com/read/29542370/role-of-primary-care-physicians-in-intrathecal-pain-management-a-narrative-review-of-the-literature
#5
Gladstone C McDowell, Joseph Winchell
OBJECTIVES: The majority of patients seeking medical care for chronic pain consult a primary care physician (PCP). Because systemic opioids are commonly prescribed to patients with chronic pain, PCPs are attempting to balance the competing priorities of providing adequate pain relief while reducing risks for opioid misuse and overdose. It is important for PCPs to be aware of pain management strategies other than systemic opioid dose escalation when patients with chronic pain fail to respond to conservative therapies and to initiate a multimodal treatment plan...
March 28, 2018: Postgraduate Medicine
https://www.readbyqxmd.com/read/29516505/methadone-against-cancer-lost-in-translation
#6
REVIEW
Dirk Theile, Gerd Mikus
Recently, the opioid analgesic D,L-methadone has gained much attention as a potential antineoplastic compound, considerably triggered through lay press and media. In consequence, physicians and pharmacists are currently confronted with numerous patients willing to use D,L-methadone against their malignancies. Well-performed in vitro and in vivo models have in fact shown pro-apoptotic effects of D,L-methadone or other opioids, but also proliferation-stimulating properties. Moreover, the mechanisms of proposed opioid-stimulated apoptosis are incompletely described or contradicting...
March 8, 2018: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/29496478/non-pharmacological-treatment-affects-neuropeptide-expression-in-neuropathic-pain-model
#7
Fabio Martinez Santos, Joyce Teixeira Silva, Igor Rafael Correia Rocha, Daniel Oliveira Martins, Marucia Chacur
Chronic constriction injury (CCI) of the sciatic nerve elicits changes in neuropeptide expression on the dorsal root ganglia (DRG). The neural mobilization (NM) technique is a noninvasive method that has been proven clinically effective in reducing pain. The aim of this study was to analyze the expression of substance P, transient receptor potential vanilloid 1 (TRPV1) and opioid receptors in the DRG of rats with chronic constriction injury and to compare it to animals that received NM treatment. CCI was performed on adult male rats...
May 15, 2018: Brain Research
https://www.readbyqxmd.com/read/29477761/concurrent-assessment-of-the-antinociceptive-and-behaviorally-disruptive-effects-of-opioids-in-squirrel-monkeys
#8
Sarah L Withey, Carol A Paronis, Jack Bergman
Although the clinical application of opioids for pain management is often hindered by undesired behavioral impairment, preclinical assays of antinociception typically do not provide information regarding the behaviorally disruptive effects of opioids that may accompany their antinociceptive effects. To address this, we modified a warm water tail withdrawal procedure to determine concurrently the effects of opioids on tail withdrawal latency (antinociception) and indices of food-maintained operant behavior (rates of responding and reinforcement density) in squirrel monkeys...
February 22, 2018: Journal of Pain: Official Journal of the American Pain Society
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
keyword
keyword
114380
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"