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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
#1
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
#2
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/29341826/mu-opioid-receptors-inhibit-the-exercise-pressor-reflex-by-closing-n-type-calcium-channels-but-not-by-opening-girk-channels-in-rats
#3
Juan A Estrada, Marc P Kaufman
Mu opioid G-protein coupled receptors (MOR) interact with ion channels to decrease neuronal excitability. In humans, intrathecal administration of the MOR agonist, fentanyl, inhibits the exercise pressor reflex, an effect that can be attributed to either the opening of inward rectifying potassium channels (GIRK) or the closing of N-type calcium channels. The purpose of this study was to determine if the highly selective MOR agonist DAMGO attenuates the exercise pressor reflex, and which of these two channels are responsible for this effect...
January 17, 2018: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/29259544/dichotomous-effects-of-mu-opioid-receptor-activation-on-striatal-low-threshold-spike-interneurons
#4
Rasha Elghaba, Enrico Bracci
Striatal low-threshold spike interneurons (LTSIs) are tonically active neurons that express GABA and nitric oxide synthase and are involved in information processing as well as neurovascular coupling. While mu opioid receptors (MORs) and their ligand encephalin are prominent in the striatum, their action on LTSIs has not been investigated. We addressed this issue carrying out whole-cell recordings in transgenic mice in which the NPY-expressing neurons are marked with green fluorescent protein (GFP). The MOR agonist (D-Ala(2), N-MePhe(4), Gly-ol)-enkephalin (DAMGO) produced dual effects on subpopulations of LTSIs...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29237725/abin-1-negatively-regulates-%C3%AE-opioid-receptor-function
#5
Peilan Zhou, Jiebing Jiang, Hui Yan, Yulei Li, Junru Zhao, Xiao Wang, Ruibin Su, Zehui Gong
The μ-opioid receptor (MOR) is a Gi/o protein-coupled receptor that mediates analgesic, euphoric, and reward effects. Using a bacterial two-hybrid screen, we reported that the carboxyl tail of the rat MOR associates with A20-binding inhibitor of nuclear factor (NF)-κB (ABIN-1) (Zhou et al., 2015). This interaction was confirmed by direct protein - protein binding and co-immunoprecipitation of MOR and ABIN-1 proteins in cell lysates. Saturation binding studies showed that ABIN-1 had no effect on MOR binding...
December 13, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29042318/mechanisms-of-%C3%AE-opioid-receptor-inhibition-of-nmda-receptor-induced-substance-p-release-in-the-rat-spinal-cord
#6
Wenling Chen, Helena S Ennes, James A McRoberts, Juan Carlos Marvizón
The interaction between NMDA receptors and μ-opioid receptors in primary afferent terminals was studied by using NMDA to induce substance P release, measured as neurokinin 1 receptor internalization. In rat spinal cord slices, the μ-opioid receptor agonists morphine, DAMGO and endomorphin-2 inhibited NMDA-induced substance P release, whereas the antagonist CTAP right-shifted the concentration response of DAMGO. In vivo, substance P release induced by intrathecal NMDA after priming with BDNF was inhibited by DAMGO...
October 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29035918/dopaminergic-mechanisms-in-periaqueductal-gray-mediated-antinociception
#7
Glaucia Tobaldini, Rafael A Reis, Natalia F Sardi, Mayla K Lazzarim, Dabna H Tomim, Marcelo M S Lima, Luana Fischer
As important as perceiving pain is the ability to modulate this perception in some contextual salient situations. The periaqueductal gray (PAG) is perhaps the most important site of endogenous pain modulation; however, little is known about dopaminergic mechanisms underlying PAG-mediated antinociception. In this study, we used a pharmacological approach to evaluate this subject. We found that µ-opioid receptor-induced antinociception (DAMGO, 0.3 μg) from PAG was blocked by the coadministration of either D1-like or D2-like dopaminergic antagonists (SCH23390, 2, 4, and 6 μg or raclopride, 2 and 4 μg, respectively) both in the tail-flick and in the mechanical paw-withdrawal test...
October 13, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28951361/-%C3%A2%C2%B5-opioid-receptors-in-the-central-nucleus-of-the-amygdala-mediate-sodium-intake-in-rats
#8
Jun-Bao Yan, Zhi-Hong Hu
OBJECTIVE: To investigate the opioidergic mechanism of the central nucleus of the amygdala (CeA) for regulating sodium appetite in rats. METHDOS: Using the elaborate invasive cerebral cannulation and brain microinjection method, we observed the effects of bilateral intra-CeA injections of DAMGO (a selective µ-opioid receptor agonist) and CTAP (a highly selective µ-opioid receptor antagonist), either alone or in combination, on NaCl solution (0.3 mol/L) and water intake by rats in different models of Na(+) ingestion...
September 20, 2017: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
https://www.readbyqxmd.com/read/28864212/14-o-methylmorphine-a-novel-selective-mu-opioid-receptor-agonist-with-high-efficacy-and-affinity
#9
Ferenc Zádor, Mihály Balogh, András Váradi, Zoltán S Zádori, Kornél Király, Edina Szűcs, Bence Varga, Bernadette Lázár, Sándor Hosztafi, Pál Riba, Sándor Benyhe, Susanna Fürst, Mahmoud Al-Khrasani
14-O-methyl (14-O-Me) group in morphine-6-O-sulfate (M6SU) or oxymorphone has been reported to be essential for enhanced affinity, potency and antinociceptive effect of these opioids. Herein we report on the pharmacological properties (potency, affinity and efficacy) of the new compound, 14-O-methylmorphine (14-O-MeM) in in vitro. Additionally, we also investigated the antinociceptive effect of the novel compound, as well as its inhibitory action on gastrointestinal transit in in vivo. The potency and efficacy of test compound were measured by [ 35 S]GTPγS binding, isolated mouse vas deferens (MVD) and rat vas deferens (RVD) assays...
November 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28839004/ventilation-and-neurochemical-changes-during-%C3%A2%C2%B5-opioid-receptor-activation-or-blockade-of-excitatory-receptors-in-the-hypoglossal-motor-nucleus-of-goats
#10
Thomas M Langer, Suzanne E Neumueller, Emma Crumley, Nicholas J Burgraff, Sawan Talwar, Matthew Robert Hodges, Lawrence G Pan, Hubert V Forster
Neuromodulator interdependence posits that changes in one or more neuromodulators are compensated by changes in other modulators to maintain stability in the respiratory control network. Herein, we studied compensatory neuromodulation in the hypoglossal motor nucleus (HMN) after chronic implantation of microtubules unilaterally (n=5) or bilaterally (n=5) into the HMN. After recovery, receptor agonists or antagonists in mock cerebrospinal fluid (mCSF) were dialyzed during the awake and NREM sleep state. During day studies, dialysis of the µ-opioid inhibitory receptor agonist DAMGO (100 µM) decreased pulmonary ventilation (V̇I), breathing frequency (f), and genioglossus (GG) muscle activity, but did not alter neuromodulators measured in the effluent mCSF...
August 24, 2017: Journal of Applied Physiology
https://www.readbyqxmd.com/read/28836121/nerve-decompression-improves-spinal-synaptic-plasticity-of-opioid-receptors-for-pain-relief
#11
To-Jung Tseng, Ming-Ling Yang, Yu-Lin Hsieh, Miau-Hwa Ko, Sung-Tsang Hsieh
Nerve decompression is an essential therapeutic strategy for pain relief clinically; however, its potential mechanism remains poorly understood. Opioid analgesics acting on opioid receptors (OR) within the various regions of the nervous system have been used widely for pain management. We therefore hypothesized that nerve decompression in a neuropathic pain model of chronic constriction injury (CCI) improves the synaptic OR plasticity in the dorsal horn, which is in response to alleviate pain hypersensitivity...
August 23, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28815604/chronic-morphine-reduces-the-readily-releasable-pool-of-gaba-a-presynaptic-mechanism-of-opioid-tolerance
#12
Adrianne R Wilson-Poe, Hyo-Jin Jeong, Christopher W Vaughan
KEY POINTS: Chronic treatment with opioids, such as morphine, leads to analgesic tolerance. While postsynaptic opioid tolerance is well documented, the involvement of presynaptic mechanisms remains unclear. We show that chronic morphine reduces the ability of periaqueductal grey (PAG) neurons to maintain GABAergic transmission. This depression of GABAergic transmission was due to a reduction in the effective size of the readily releasable pool. This also led to a reduction in opioid presynaptic inhibition; these presynaptic adaptations need to be considered in the development of strategies to reduce opioid tolerance...
October 15, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28654029/measuring-g-protein-coupled-receptor-signaling-via-radio-labeled-gtp-binding
#13
Chirag Vasavda, Nicholas W Zaccor, Paul C Scherer, Charlotte J Sumner, Solomon H Snyder
G-Protein-Coupled Receptors (GPCRs) are a large family of transmembrane receptors that play critical roles in normal cellular physiology and constitute a major pharmacological target for multiple indications, including analgesia, blood pressure regulation, and the treatment of psychiatric disease. Upon ligand binding, GPCRs catalyze the activation of intracellular G-proteins by stimulating the incorporation of guanosine triphosphate (GTP). Activated G-proteins then stimulate signaling pathways that elicit cellular responses...
June 9, 2017: Journal of Visualized Experiments: JoVE
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
#14
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)...
September 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28587388/roles-of-the-%C3%A2%C2%B5-opioid-receptor-and-its-related-signaling-pathways-in-the-pathogenesis-of-premenstrual-syndrome-liver-qi-stagnation
#15
Chunhong Song, Ling Xue
The present study aimed to investigate the roles of the µ-opioid receptor (MOR) and its related signaling pathways in the pathogenesis of premenstrual syndrome (PMS) liver-qi stagnation, along with the therapeutic effects of the Shu-Yu capsule in treating the condition. A PMS liver-qi stagnation rat model was established using a chronic restraint stress method. The protein expression level of MOR within rat hippocampal tissue was detected via western blot analysis and cyclic adenosine monophosphate (cAMP) levels within the supernatant of a rat hippocampal cell culture were determined by ELISA...
June 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28583050/%C3%AE-opioid-and-5-ht1a-receptors-in-the-dorsomedial-hypothalamus-interact-for-the-regulation-of-panic-related-defensive-responses
#16
Camila Marroni Roncon, Paula Shimene de Melo Yamashita, Alana Tercino Frias, Elisabeth Aparecida Audi, Frederico Guilherme Graeff, Norberto Cysne Coimbra, Helio Zangrossi
The dorsomedial hypothalamus (DMH) and the dorsal periaqueductal gray (DPAG) have been implicated in the genesis and regulation of panic-related defensive behaviors, such as escape. Previous results point to an interaction between serotonergic and opioidergic systems within the DPAG to inhibit escape, involving µ-opioid and 5-HT1A receptors (5-HT1AR). In the present study we explore this interaction in the DMH, using escape elicited by electrical stimulation of this area as a panic attack index. The obtained results show that intra-DMH administration of the non-selective opioid receptor antagonist naloxone (0...
June 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28554847/panicolytic-like-action-of-bradykinin-in-the-dorsal-periaqueductal-gray-through-%C3%AE-opioid-and-b2-kinin-receptors
#17
Caio César Sestile, Jhonatan Christian Maraschin, Vanessa Scalco Gama, Hélio Zangrossi, Frederico Guilherme Graeff, Elisabeth Aparecida Audi
A wealth of evidence has shown that opioid and kinin systems may control proximal defense in the dorsal periaqueductal gray matter (dPAG), a critical panic-associated area. Studies with drugs that interfere with serotonin-mediated neurotransmission suggest that the μ-opioid receptor (MOR) synergistically interacts with the 5-HT1A receptor in the dPAG to inhibit escape, a panic-related behavior. A similar inhibitory effect has also been reported after local administration of bradykinin (BK), which is blocked by the non-selective opioid receptor antagonist naloxone...
May 26, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28502630/new-opioid-receptor-antagonist-naltrexone-14-o-sulfate-synthesis-and-pharmacology
#18
Ferenc Zádor, Kornél Király, András Váradi, Mihály Balogh, Ágnes Fehér, Dóra Kocsis, Anna I Erdei, Erzsébet Lackó, Zoltán S Zádori, Sándor Hosztafi, Béla Noszál, Pál Riba, Sándor Benyhe, Susanna Fürst, Mahmoud Al-Khrasani
Opioid antagonists, naloxone and naltrexone have long been used in clinical practice and research. In addition to their low selectivity, they easily pass through the blood-brain barrier. Quaternization of the amine group in these molecules, (e.g. methylnaltrexone) results in negligible CNS penetration. In addition, zwitterionic compounds have been reported to have limited CNS access. The current study, for the first time gives report on the synthesis and the in vitro [competition binding, G-protein activation, isolated mouse vas deferens (MVD) and mouse colon assay] pharmacology of the zwitterionic compound, naltrexone-14-O-sulfate...
May 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28455226/the-effect-of-selective-opioid-receptor-agonists-and-antagonists-on-epileptiform-activity-in-morphine-dependent-infant-mice-hippocampal-slices
#19
Yousef Panahi, Ehsan Saboory, Ali Rassouli, Goudarz Sadeghi-Hashjin, Shiva Roshan-Milani, Leila Derafshpour, Yousef Rasmi
Hippocampal slices of mouse brain were used to estimate how selective agonist and antagonist of opioid receptors alter Low-Mg(+2) artificial cerebrospinal fluid (LM-ACSF)-induced epileptiform activities in normal and morphine-dependent mice. Brain slices were obtained from control and morphine-dependent mice. The morphine-dependent group received morphine once a day for 5 consecutive days, and the control group received saline. All injections were administered subcutaneously (s.c) in a volume of 0.1mL on postnatal days 14-18...
August 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28407740/mu-opioid-receptor-and-delta-opioid-receptor-differentially-regulate-microglial-inflammatory-response-to-control-proopiomelanocortin-neuronal-apoptosis-in-the-hypothalamus-effects-of-neonatal-alcohol
#20
Pallavi Shrivastava, Miguel A Cabrera, Lucy G Chastain, Nadka I Boyadjieva, Shaima Jabbar, Tina Franklin, Dipak K Sarkar
BACKGROUND: Opioid receptors are known to control neurotransmission of various peptidergic neurons, but their potential role in regulation of microglia and neuronal cell communications is unknown. We investigated the role of mu-opioid receptors (MOR) and delta-opioid receptors (DOR) on microglia in the regulation of apoptosis in proopiomelanocortin (POMC) neurons induced by neonatal ethanol in the hypothalamus. METHODS: Neonatal rat pups were fed a milk formula containing ethanol or control diets between postnatal days 2-6...
April 14, 2017: Journal of Neuroinflammation
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