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https://www.readbyqxmd.com/read/29454675/targeting-immune-driven-opioid-analgesia-by-sigma-1-receptors-opening-the-door-to-novel-perspectives-for-the-analgesic-use-of-sigma-1-antagonists
#1
Miguel Á Tejada, Ángeles Montilla-García, Rafael González-Cano, Inmaculada Bravo-Caparrós, M Carmen Ruiz-Cantero, Francisco R Nieto, Enrique J Cobos
Immune cells have a known role in pronociception, since they release a myriad of inflammatory algogens which interact with neurons to facilitate pain signaling. However, these cells also produce endogenous opioid peptides with analgesic potential. The sigma-1 receptor is a ligand-operated chaperone that modulates neurotransmission by interacting with multiple protein partners, including the μ-opioid receptor. We recently found that sigma-1 antagonists are able to induce opioid analgesia by enhancing the action of endogenous opioid peptides of immune origin during inflammation...
February 15, 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29451852/delta-opioids-neuroprotective-roles-in-preclinical-studies
#2
Shahid Husain
Since ancient times, opioids have been used clinically and abused recreationally. In the early stages (about 1,000 AD) of opium history, an Arab physician, Avicenna, administered opioids to control diarrhea and eye diseases. 1 Opioids have very strong pain relieving properties and they also regulate numerous cellular responses. Opioid receptors are expressed throughout the body, including the nervous system, heart, lungs, liver, gastrointestinal tract, and retina. 2-6 Delta opioid receptors (DORs) are a very attractive target from the perspective of both receptor function and their therapeutic potential...
January 2018: Journal of Ocular Pharmacology and Therapeutics
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/29447951/suction-electrode-recording-in-locus-coeruleus-of-newborn-rat-brain-slices-reveals-network-bursting-comprising-summated-non-synchronous-spiking
#4
Vladimir Rancic, Bijal Rawal, Bogdan Panaitescu, Araya Ruangkittisakul, Klaus Ballanyi
The brainstem locus coeruleus (LC) controling behaviors like arousal, sleep, breathing, pain or opioid withdrawal is an established model for spontaneous action potential synchronization. Such synchronous 'spiking' might produce an extracellular field potential (FP) which is a crucial tool for neural network analyses. We found using ≥10 μm tip diameter suction electrodes in newborn rat brainstem slices that the LC generates at ∼1 Hz a robust rhythmic FP (rFP). During distinct rFP phases, LC neurons discharge with a jitter of ±33 ms single spikes that summate to a ∼200 ms-lasting population burst...
February 12, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29447132/role-of-gpcr-mu-opioid-receptor-tyrosine-kinase-epidermal-growth-factor-crosstalk-in-opioid-induced-hyperalgesic-priming-type-ii
#5
Dionéia Araldi, Luiz F Ferrari, Jon D Levine
Repeated stimulation of mu-opioid receptors (MORs), by an MOR-selective agonist DAMGO induces type II priming, a form of nociceptor neuroplasticity, which has 2 components: opioid-induced hyperalgesia (OIH) and prolongation of prostaglandin-E2 (PGE2)-induced hyperalgesia. We report that intrathecal antisense knockdown of the MOR in nociceptors, prevented the induction of both components of type II priming. Type II priming was also eliminated by SSP-saporin, which destroys the peptidergic class of nociceptors...
January 11, 2018: Pain
https://www.readbyqxmd.com/read/29445295/the-effect-of-exercise-frequency-on-neuropathic-pain-and-pain-related-cellular-reactions-in-the-spinal-cord-and-midbrain-in-a-rat-sciatic-nerve-injury-model
#6
Megumi Sumizono, Harutoshi Sakakima, Shotaro Otsuka, Takuto Terashi, Kazuki Nakanishi, Koki Ueda, Seiya Takada, Kiyoshi Kikuchi
Background: Exercise regimens are established methods that can relieve neuropathic pain. However, the relationship between frequency and intensity of exercise and multiple cellular responses of exercise-induced alleviation of neuropathic pain is still unclear. We examined the influence of exercise frequency on neuropathic pain and the intracellular responses in a sciatic nerve chronic constriction injury (CCI) model. Materials and methods: Rats were assigned to four groups as follows: CCI and high-frequency exercise (HFE group), CCI and low-frequency exercise (LFE group), CCI and no exercise (No-Ex group), and naive animals (control group)...
2018: Journal of Pain Research
https://www.readbyqxmd.com/read/29441714/time-dependent-regional-brain-distribution-of-methadone-and-naltrexone-in-the-treatment-of-opioid-addiction
#7
Belin G Teklezgi, Annapurna Pamreddy, Sooraj Baijnath, Hendrik G Kruger, Tricia Naicker, Nirmala D Gopal, Thavendran Govender
Opioid addiction is a serious public health concern with severe health and social implications; therefore, extensive therapeutic efforts are required to keep users drug free. The two main pharmacological interventions, in the treatment of addiction, involve management with methadone an mu (μ)-opioid agonist and treatment with naltrexone, μ-opioid, kappa (κ)-opioid and delta (δ)-opioid antagonist. MET and NAL are believed to help individuals to derive maximum benefit from treatment and undergo a full recovery...
February 14, 2018: Addiction Biology
https://www.readbyqxmd.com/read/29440403/suppression-of-rgsz1-function-optimizes-the-actions-of-opioid-analgesics-by-mechanisms-that-involve-the-wnt-%C3%AE-catenin-pathway
#8
Sevasti Gaspari, Immanuel Purushothaman, Valeria Cogliani, Farhana Sakloth, Rachael L Neve, David Howland, Robert H Ring, Elliott M Ross, Li Shen, Venetia Zachariou
Regulator of G protein signaling z1 (RGSz1), a member of the RGS family of proteins, is present in several networks expressing mu opioid receptors (MOPRs). By using genetic mouse models for global or brain region-targeted manipulations of RGSz1 expression, we demonstrated that the suppression of RGSz1 function increases the analgesic efficacy of MOPR agonists in male and female mice and delays the development of morphine tolerance while decreasing the sensitivity to rewarding and locomotor activating effects...
February 12, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29436492/allosterism-within-delta-opioid-kappa-opioid-receptor-heteromers-in-peripheral-sensory-neurons-regulation-of-kappa-opioid-agonist-efficacy
#9
Blaine Jacobs, Miryam M Pando, Elaine M Jennings, Teresa S Chavera, William P Clarke, Kelly A Berg
There is abundant evidence for formation of G protein coupled receptor heteromers in heterologous expression systems, however, little is known of the function of heteromers in native systems. Heteromers of delta and kappa opioid receptors (DOR-KOR heteromers) have been identified in native systems. We previously reported that activation of DOR-KOR heteromers expressed by rat pain-sensing neurons (nociceptors) produces robust, peripherally-mediated antinociception. Moreover, DOR agonist potency and efficacy is regulated by KOR antagonists via allosteric interactions within the DOR-KOR heteromer in a ligand-dependent manner...
February 7, 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29434817/%C3%AE-opioid-receptor-inhibition-prevents-remifentanil-induced-post-operative-hyperalgesia-via-regulating-glur1-trafficking-and-ampa-receptor-function
#10
Aifen Liu, Xiaopeng Wang, Hui Wang, Guoyi Lv, Yize Li, Hongmei Li
The interaction of remifentanil with glutamate systems has an important role in remifentanil-induced thermal and mechanical hyperalgesia. A previous study by our group suggested that the trafficking and function of glutamate receptor 1 (GluR1) subunits contributes to remifentanil-induced hyperalgesia by regulating the phosphorylation of GluR1 in dorsal horn neurons. The present study demonstrated that δ opioid receptor (DOR) inhibition prevented thermal and mechanical hyperalgesia, which was induced by remifentanil infusion via attenuating GluR1 subunit trafficking and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) function in dorsal horn neurons...
February 2018: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29433586/a-case-report-of-clonidine-induced-syncope-a-review-of-central-actions-of-an-old-cardiovascular-drug
#11
Alexander J Sandweiss, Christopher M Morrison, Anne Spichler, John Rozich
BACKGROUND: Clonidine is an imidazoline sympatholytic, acting on both α 2 -adrenergic and imidazoline receptors in the brainstem to induce antihypertensive and negative chronotropic effects in the vasculature and heart respectively. CASE PRESENTATION: A 69-year-old gentleman with hypertension presented to the emergency department after multiple syncopal episodes over the past 12 months. Electrocardiogram demonstrated sinus bradycardia with a heart rate of 42 beats per minute...
February 13, 2018: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29432603/in-vitro-screening-for-seizure-liability-using-microelectrode-array-technology
#12
Jenifer A Bradley, Harry H Luithardt, Monica R Metea, Christopher J Strock
Drug induced seizure liabilities produce significant compound attrition during drug discovery. Currently available in vitro cytotoxicity assays cannot predict all toxicity mechanisms due to the failure of these assays to predict sublethal target specific electrophysiological liabilities. Identification of seizurogenic and other electrophysiological effects at early stages of the drug development process is important to ensure that safe candidate compounds can be developed while chemical design is taking place, long before these liabilities are discovered in costly preclinical in vivo studies...
February 8, 2018: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29431655/fentanyl-induces-rapid-onset-hyperalgesic-priming-type-i-at-peripheral-and-type-ii-at-central-nociceptor-terminals
#13
Dioneia Araldi, Eugen V Khomula, Luiz F Ferrari, Jon D Levine
Systemic fentanyl induces hyperalgesic priming, long-lasting neuroplasticity in nociceptor function characterized by prolongation of inflammatory mediator hyperalgesia. To evaluate priming at both nociceptor terminals, we studied, in male Sprague--Dawley rats, the effect of local administration of agents that reverse Type I (protein translation) or Type II (combination of Src and mitogen-activated protein kinase [MAPK]) priming. While at the central terminal, priming induced by systemic, intradermal or intrathecal fentanyl was reversed by the combination of Src and MAPK inhibitors, at the peripheral terminal it was reversed by the protein translation inhibitor...
February 5, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29430855/dynorphinergic-system-alterations-in-the-corticostriatal-circuitry-of-neuropathic-mice-supports-its-role-in-the-negative-affective-component-of-pain
#14
Palmisano Martina, Caputi Francesca Felicia, Mercatelli Daniela, Romualdi Patrizia, Candeletti Sanzio
The dynorphinergic system is involved in pain transmission at spinal level, where dynorphin exerts antinociceptive or pronociceptive effects, based on its opioid or non-opioid actions. Surprisingly, little evidence is currently available concerning the supraspinal role of the dynorphinergic system in pain conditions. The present study aimed to investigate whether neuropathic pain is accompanied by prodynorphin (Pdyn) and κ-opioid receptor (Oprk1) gene expression alterations in selected mouse brain areas. To this end, mice were subjected to chronic constriction injury of the right sciatic nerve and neuropathic pain behavioral signs were ascertained after 14 days...
February 12, 2018: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/29428394/the-pharmacology-of-amphetamine-and-methylphenidate-relevance-to-the-neurobiology-of-attention-deficit-hyperactivity-disorder-and-other-psychiatric-comorbidities
#15
REVIEW
Stephen V Faraone
Psychostimulants, including amphetamines and methylphenidate, are first-line pharmacotherapies for individuals with attention-deficit/hyperactivity disorder (ADHD). This review aims to educate physicians regarding differences in pharmacology and mechanisms of action between amphetamine and methylphenidate, thus enhancing physician understanding of psychostimulants and their use in managing individuals with ADHD who may have comorbid psychiatric conditions. A systematic literature review of PubMed was conducted in April 2017, focusing on cellular- and brain system-level effects of amphetamine and methylphenidate...
February 8, 2018: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/29427652/evaluating-the-abuse-potential-of-psychedelic-drugs-for-medical-use-in-humans
#16
REVIEW
David J Heal, Jane Gosden, Sharon L Smith
Psychedelics comprise drugs come from various pharmacological classes including 5-HT 2A agonists, indirect 5-HT agonists, e.g. MDMA, NMDA antagonists and κ-opioid receptor agonists. There is resurgence in developing psychedelics to treat psychiatric disorders with high unmet clinical need. Many, but not all, psychedelics are schedule 1 controlled drugs (CDs), i.e. no approved medical use. For existing psychedelics in development, regulatory approval will require a move from schedule 1 to a CD schedule for drugs with medical use, i...
February 7, 2018: Neuropharmacology
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
#17
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/29426768/o6c-20-nor-salvinorin-a-is-a-stable-and-potent-kor-agonist
#18
Shun Hirasawa, Min Cho, Tarsis F Brust, Jeremy J Roach, Laura M Bohn, Ryan A Shenvi
Salvinorin A (SalA) is a potent and selective agonist of the kappa-opioid receptor (KOR), but its instability has frustrated medicinal chemistry efforts. Treatment of SalA with weak bases like DBU leads to C8 epimerization with loss of receptor affinity and signaling potency. Here we show that replacement of C20 with H and replacement of O6 with CH2 stabilizes the SalA scaffold relative to its C8 epimer, so much so that epimerization is completely supressed. This new compound, O6C-20-nor-SalA, retains high potency for agonism of KOR...
January 31, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29422496/opioid-antagonists-and-the-a118g-polymorphism-in-the-%C3%AE-opioid-receptor-gene-effects-of-gsk1521498-and-naltrexone-in-healthy-drinkers-stratified-by-oprm1-genotype
#19
Hisham Ziauddeen, Liam J Nestor, Naresh Subramaniam, Chris Dodds, Pradeep J Nathan, Sam R Miller, Bhopinder K Sarai, Kay Maltby, Disala Fernando, Liling Warren, Louise K Hosking, Dawn Waterworth, Anna Korzeniowska, Beta Win, Duncan B Richards, Lakshmi Vasist Johnson, Paul C Fletcher, Edward T Bullmore
This corrects the article DOI: 10.1038/npp.2016.60.
March 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29421449/potential-uses-of-isolated-toxin-peptides-in-neuropathic-pain-relief-a-literature-review
#20
REVIEW
M K Hamad, K He, H F Abdulrazeq, A M Mustafa, J Nakhla, M M Herzallah, A Mammis
Neuropathic pain is a subset of chronic pain that is caused by neurons that are damaged or firing aberrantly in the peripheral or central nervous systems. The treatment guidelines for neuropathic pain include antidepressants, calcium channel α 2 delta ligands, topical therapy, and opioids as a second line option. Unfortunately, pharmacotherapy has not been effective in the treatment of neuropathic pain except in the treatment of trigeminal neuralgia with carbamazepine. The inability to properly treat neuropathic pain causes frustration in both the patients and their treating physicians...
February 5, 2018: World Neurosurgery
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