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https://www.readbyqxmd.com/read/29142121/the-role-of-kappa-opioid-receptors-in-glutamate-input-selection-in-the-ventral-striatum
#1
Angelica P Escobar
No abstract text is available yet for this article.
November 15, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29137290/expression-of-protein-kinase-a-and-the-kappa-opioid-receptor-in-selected-brain-regions-and-conditioned-place-aversion-in-morphine-dependent-rats
#2
Xiuhua Song, Wenqiang Li, Yuzhong Shi, Jingdan Zhang, Yi Li
This study examined adaptive changes in protein kinase A (PKA) and kappa opioid receptor (KOR) in selected addiction-related brain regions before and after conditioned place aversion (CPA). Seventy-two male SD rats were randomly assigned to an experimental group (morphine + naloxone, "MN") and 2 control groups: MS (morphine + saline) and SN (saline + naloxone). MN rats were intraperitoneally injected with morphine twice per day for 6.5 days and naloxone once and trained to establish CPA model. MS and SN rats were injected with equivalent volumes of morphine plus saline and saline plus naloxone, respectively...
October 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29131554/the-pathophysiology-incidence-impact-and-treatment-of-opioid-induced-nausea-and-vomiting
#3
Theresa Mallick-Searle, Mechele Fillman
PURPOSE: Opioid medications are integral in managing acute moderate-to-severe pain. Opioid analgesics bind to μ (mu), κ (kappa), or δ (delta) opioid receptors in the brain, spinal cord, and digestive tract. However, opioids cause adverse effects that may interfere with their therapeutic use. Some adverse effects wane over time, but patients using opioids for acute pain struggle with opioid-induced nausea and vomiting (OINV) the entire time they take the opioid. This article discusses the underlying mechanisms, clinical implications, and treatment strategies of OINV...
November 2017: Journal of the American Association of Nurse Practitioners
https://www.readbyqxmd.com/read/29114861/kappa-opioid-receptors-regulate-hippocampal-synaptic-homeostasis-and-epileptogenesis
#4
Bridget N Queenan, Raymond L Dunn, Victor R Santos, Yang Feng, Megan N Huizenga, Robert J Hammack, Stefano Vicini, Patrick A Forcelli, Daniel T S Pak
OBJECTIVE: Homeostatic synaptic plasticity (HSP) serves as a gain control mechanism at central nervous system (CNS) synapses, including those between the dentate gyrus (DG) and CA3. Improper circuit control of DG-CA3 synapses is hypothesized to underlie epileptogenesis. Here, we sought to (1) identify compounds that preferentially modulate DG-CA3 synapses in primary neuronal culture and (2) determine if these compounds would delay or prevent epileptogenesis in vivo. METHODS: We previously developed and validated an in vitro assay to visualize the behavior of DG-CA3 synapses and predict functional changes...
November 8, 2017: Epilepsia
https://www.readbyqxmd.com/read/29107424/selective-kappa-opioid-antagonists-for-treatment-of-addiction-are-we-there-yet
#5
REVIEW
Mohamed A Helal, Eman S Habib, Amar G Chittiboyina
Kappa opioid receptor (KOP) is a G-protein coupled receptor mainly expressed in the cerebral cortex and hypothalamus. It is implicated in nociception, diuresis, emotion, cognition, and immune system functions. KOP agonists possess a strong analgesic effect accompanied by a feeling of dysphoria. On the other hand, antagonists of this receptor were found to block depression, anxiety, and drug-seeking behaviors in animal models. Recently, great interest has been given to the development of selective KOP antagonists as an addiction treatment that does not cause dependence itself or show high relapse rates like the currently used agents...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29100992/antagonism-of-the-kappa-opioid-receptor-attenuates-thc-induced-place-aversions-in-adult-male-sprague-dawley-rats
#6
Matthew M Clasen, Shaun M Flax, Briana J Hempel, Kejun Cheng, Kenner C Rice, Anthony L Riley
RATIONALE: Prior research with transgenic mice in which the kappa opioid receptor (KOR) has been suppressed or activated suggests that the aversive effects of THC are mediated by activity of this receptor subtype. If the activity of the KOR system is responsible for mediating the THC's aversive effects, then selective antagonism of the KOR by norBNI should block such aversive effects. To test this hypothesis, rats were pretreated with norBNI 24h prior to place conditioning with THC to assess its effect on the acquisition of THC-induced place aversions...
October 31, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29063139/dissociable-effects-of-the-kappa-opioid-receptor-agonist-nalfurafine-on-pain-itch-stimulated-and-pain-itch-depressed-behaviors-in-male-rats
#7
Matthew L Lazenka, Megan J Moerke, E Andrew Townsend, Kevin B Freeman, F Ivy Carroll, S Stevens Negus
RATIONALE: Nalfurafine is a G protein signaling-biased kappa opioid receptor (KOR) agonist approved in Japan for second-line treatment of uremic pruritus. Neither nalfurafine nor any other KOR agonist is currently approved anywhere for treatment of pain, but recent evidence suggests that G protein signaling-biased KOR agonists may have promise as candidate analgesics/antipruritics with reduced side effects compared to nonbiased or ß-arrestin-signaling-biased KOR agonists. OBJECTIVES: This study compared nalfurafine effects in rats using assays of pain-stimulated and pain-depressed behavior used previously to evaluate other candidate analgesics...
October 24, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29056156/dynorphin-kappa-opioid-receptor-signaling-in-preclinical-models-of-alcohol-drug-and-food-addiction
#8
Anushree Karkhanis, Katherine M Holleran, Sara R Jones
The dynorphin/kappa opioid receptor (KOR) system is implicated in the "dark side" of addiction, in which stress exacerbates maladaptive responses to drug and alcohol exposure. For example, acute stress and acute ethanol exposure result in an elevation in dynorphin, the KOR endogenous ligand. Activation of KORs results in modulation of several neurotransmitters; however, this chapter will focus on its regulatory effects on dopamine in mesolimbic areas. Specifically, KOR activation has an inhibitory effect on dopamine release, thereby influencing reward processing...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/29055075/association-between-genetic-polymorphisms-and-pain-sensitivity-in-patients-with-hip-osteoarthritis
#9
Anne E Olesen, Lecia M Nielsen, Søren Feddersen, Joachim Erlenwein, Frank Petzke, Michael Przemeck, Lona L Christrup, Asbjørn M Drewes
BACKGROUND: Factors such as age, gender and genetic polymorphisms may explain individual difference in pain phenotype. Genetic associations to pain sensitivity have previously been investigated in osteoarthritis patients with focus on the P2X7, TRPV1 and TACR1 genes. However, other genes may play a role as well. Osteoarthritis is a common joint disease and many patients suffering from this disease are thought to have increased sensitivity to noxious stimuli resulting from sensitization in the nociceptive system...
October 20, 2017: Pain Practice: the Official Journal of World Institute of Pain
https://www.readbyqxmd.com/read/29040826/maintenance-on-naltrexone-amphetamine-decreases-cocaine-vs-food-choice-in-male-rhesus-monkeys
#10
Megan J Moerke, Matthew L Banks, Kejun Cheng, Kenner C Rice, S Stevens Negus
BACKGROUND: Cocaine use disorder remains a significant public health issue for which there are no FDA-approved pharmacotherapies. Amphetamine maintenance reduces cocaine use in preclinical and clinical studies, but the mechanism of this effect is unknown. Previous studies indicate a role for endogenous opioid release and subsequent opioid receptor activation in some amphetamine effects; therefore, the current study examined the role of mu-opioid receptor activation in d-amphetamine treatment effects in an assay of cocaine-vs-food choice...
December 1, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29038479/probing-ligand-recognition-of-the-opioid-pan-antagonist-at-076-at-nociceptin-kappa-mu-and-delta-opioid-receptors-through-structure-activity-relationships
#11
V Blair Journigan, Willma E Polgar, Edward W Tuan, James Lu, Pankaj R Daga, Nurulain T Zaveri
Few opioid ligands binding to the three classic opioid receptor subtypes, mu, kappa and delta, have high affinity at the fourth opioid receptor, the nociceptin/orphanin FQ receptor (NOP). We recently reported the discovery of AT-076 (1), (R)-7-hydroxy-N-((S)-1-(4-(3-hydroxyphenyl)piperidin-1-yl)-3-methylbutan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, a pan antagonist with nanomolar affinity for all four subtypes. Since AT-076 binds with high affinity at all four subtypes, we conducted a structure-activity relationship (SAR) study to probe ligand recognition features important for pan opioid receptor activity, using chemical modifications of key pharmacophoric groups...
October 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29037662/effects-of-pharmacological-manipulation-of-the-kappa-opioid-receptors-on-the-aversive-effects-of-nicotine
#12
Melissa Ward, Haval Norman, Manoranjan S D'Souza
Nicotine, an addictive component of tobacco smoke, produces both rewarding and aversive effects. Increasing the aversive effects of nicotine may help in promoting smoking cessation. However, neural targets mediating the aversive effects of nicotine have not been fully identified. In this study, we evaluated the role of kappa opioid receptors (KORs) in the aversive effects of nicotine (0.4 mg/kg, base; s.c.) using the nicotine-induced conditioned taste aversion (CTA) model in Wistar rats. The KORs were activated using the selective KOR agonist (±)U-50,488H (0, 0...
October 14, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29025923/plasticity-of-signaling-by-spinal-estrogen-receptor-alpha-kappa-opioid-receptor-and-mglurs-over-the-rat-reproductive-cycle-regulates-spinal-endomorphin-2-antinociception-relevance-of-endogenous-biased-agonism
#13
Nai-Jiang Liu, Vijaya Murugaiyan, Emiliya M Storman, Stephen A Schnell, Arjun Kumar, Martin W Wessendorf, Alan R Gintzler
We previously showed that intrathecal application of endomorphin 2 [EM2; the highly specific endogenous mu-opioid receptor (MOR) ligand] induces antinociception that varies with stage of the rat estrous cycle -- minimal during diestrus and prominent during proestrus. Earlier studies, however, did not identify proestrus-activated signaling strategies that enable spinal EM2 antinociception. We now report that in female rats, increased spinal dynorphin release and kappa-opioid receptor (KOR) signaling, as well as the emergence of glutamate-activated mGluR1 signaling, are critical to the transition from an EM2 non-responsive (during diestrus) to an analgesically responsive state (during proestrus)...
October 12, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29020387/reversal-of-stress-induced-social-interaction-deficits-by-buprenorphine
#14
Caroline A Browne, Edgardo Falcon, Shivon A Robinson, Olivier Berton, Irwin Lucki
Background: Patients with post-traumatic stress disorder (PTSD) frequently report persistent problems with social interactions, emerging after a traumatic experience. Chronic social defeat stress (CSDS) is a widely used rodent model of stress that produces robust and sustained social avoidance behavior. The avoidance of other rodents can be reversed by 28 days of treatment with selective serotonin reuptake inhibitors (SSRIs), the only pharmaceutical class approved by the U. S. Food and Drug Administration for treating PTSD...
August 31, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28989282/spotlight-on-eluxadoline-for-the-treatment-of-patients-with-irritable-bowel-syndrome-with-diarrhea
#15
REVIEW
Konstantinos C Fragkos
BACKGROUND: Irritable bowel syndrome with diarrhea (IBS-D) has limited options for treatment currently, including mainly anti-motility medications, antispasmodics, and antidepressants. This review discusses the properties of a new drug, eluxadoline, a gut-targeting mu- and kappa-opioid receptor agonist and a delta-opioid receptor antagonist, and its efficacy and safety in patients with IBS-D. MATERIALS AND METHODS: A systematic review of the literature was undertaken to identify studies that had investigated eluxadoline as a treatment in IBS-D...
2017: Clinical and Experimental Gastroenterology
https://www.readbyqxmd.com/read/28987634/heterodimerization-of-apelin-and-opioid-receptors-and-cardiac-inotropic-and-lusitropic-effects-of-apelin-in-2k1c-hypertension-role-of-perk1-2-and-pkc
#16
Farzaneh Rostamzadeh, Hamid Najafipour, Mahboobeh Yeganeh-Hajahmadi, Saeed Esmaeili-Mahani, Siyavash Joukar, Maryam Iranpour
AIMS: Kappa Opioid receptors (KORs) change the impact of apelin on the phosphorylated ERK1/2 (pERK1/2). However, the role of interaction between KOR and apelin receptors (APJ) on the cardiac contractility effects of apelin and in regulation of pERK1/2 and PKC in the heart of renovascular hypertensive (2K1C) rats is unknown. MAIN METHODS: Hemodynamic factors, the heterodimerization of KOR and APJ, the expression of KOR mRNA and protein and pERK1/2 in the left ventricle of 2K1C rats were measured following APJ, KOR, PKC and Gi path inhibition by F13A, nor-BNI, chelerythrine and PTX respectively...
October 4, 2017: Life Sciences
https://www.readbyqxmd.com/read/28975684/salvinorin-a-reduces-neuropathic-nociception-in-the-insular-cortex-of-the-rat
#17
U Coffeen, A Canseco-Alba, K Simón-Arceo, A Almanza, F Mercado, M León-Olea, F Pellicer
BACKGROUND: Neuropathic pain is one of the most important challenges in public health. The search for novel treatments is important for an adequate relief without adverse effects. In this sense salvinorin A (SA), the main diterpene of the medicinal plant Salvia divinorum is an important antinociceptive compound, which acts as a potent agonist of kappa opioid receptor (KOR) and cannabinoid CB1 receptors. METHODS: We evaluated nociceptive responses in a neuropathic pain model induced by the sciatic nerve ligature (SNL) in the right hind paw, after the microinjection of SA, Salvinorin B (SB), KOR and CB1 antagonists directly in the insular cortex (IC) in male wistar rats...
October 4, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28974443/toxicological-aspects-of-the-interesterified-fat-from-processed-foods-influences-on-opioid-system-and-its-reward-effects-in-rats
#18
Laura H Milanesi, Karine Roversi, Caren T D Antoniazzi, Hecson J Segat, Maikel Kronbauer, Lívia F D'avila, Verônica T Dias, Marcel H M Sari, Raquel C S Barcelos, Luana H Maurer, Tatiana Emanuelli, Marilise E Burger, Fabíola Trevizol
Considering the high consumption of processed foods, interesterified fat (IF) has been used to replace trans fat, since it may harm nervous system functions. Opioids are intensely used to alleviate pain, and have a highly addictive potential. Therefore, their improper use is related to addiction, tolerance, and withdrawal syndrome. Wistar rats received soybean oil (SO) or IF during gestation, lactation and post-weaning until pups' adolescence. On post-natal day 39, animals received morphine (4 mg/kg i.p.) in the conditioned place preference (CPP) paradigm...
September 30, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28971325/a-novel-oral-fluid-assay-lc-qtof-ms-for-the-detection-of-fentanyl-and-clandestine-opioids-in-oral-fluid-after-reported-heroin-overdose
#19
Matthew K Griswold, Peter R Chai, Alex J Krotulski, Melissa Friscia, Brittany P Chapman, Neha Varma, Edward W Boyer, Barry K Logan, Kavita M Babu
INTRODUCTION: The adulteration of heroin with non-pharmaceutical fentanyl and other high-potency opioids is one of the factors contributing to striking increases in overdose deaths. To fully understand the magnitude of this problem, accurate detection methods for fentanyl and other novel opioid adulterant exposures are urgently required. The objective of this work was to compare the detection of fentanyl in oral fluid and urine specimens using liquid chromatography quadrupole time-of-flight mass spectrometry (LC-QTOF-MS) in a population of heroin users presenting to the Emergency Department after overdose...
October 2, 2017: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
https://www.readbyqxmd.com/read/28967123/antidepressant-like-effects-of-bu10119-a-novel-buprenorphine-analogue-with-mixed-kappa-mu-opioid-receptor-antagonist-properties-in-mice
#20
Abdulrahman Almatroudi, Mehrnoosh Ostovar, Christopher P Bailey, Stephen M Husbands, Sarah J Bailey
BACKGROUND AND PURPOSE: Κ-opioid receptor antagonists have potential for treating neuropsychiatric disorders. We have investigated the in vivo pharmacology of a novel buprenorphine analogue, BU10119, for the first time. EXPERIMENTAL APPROACH: To determine the opioid pharmacology of BU10119 (0.3-3 mg/kg, i.p.) in vivo, the warm-water tail withdrawal assay was used in adult male CD1 mice. A range of behavioural paradigms was used to investigate the locomotor effects, rewarding properties and antidepressant or anxiolytic potential of BU10119...
October 1, 2017: British Journal of Pharmacology
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