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Kappa opioid receptor

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https://www.readbyqxmd.com/read/29040826/maintenance-on-naltrexone-amphetamine-decreases-cocaine-vs-food-choice-in-male-rhesus-monkeys
#1
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...
October 13, 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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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/28967123/antidepressant-like-effects-of-bu10119-a-novel-buprenorphine-analogue-with-mixed-kappa-mu-opioid-receptor-antagonist-properties-in-mice
#10
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
https://www.readbyqxmd.com/read/28963507/peroxiredoxin-6-mediates-g%C3%AE-i-protein-coupled-receptor-inactivation-by-cjun-kinase
#11
Selena S Schattauer, Benjamin B Land, Kathryn L Reichard, Antony D Abraham, Lauren M Burgeno, Jamie R Kuhar, Paul E M Phillips, Shao En Ong, Charles Chavkin
Inactivation of opioid receptors limits the therapeutic efficacy of morphine-like analgesics and mediates the long duration of kappa opioid antidepressants by an uncharacterized, arrestin-independent mechanism. Here we use an iterative, discovery-based proteomic approach to show that following opioid administration, peroxiredoxin 6 (PRDX6) is recruited to the opioid receptor complex by c-Jun N-terminal kinase (JNK) phosphorylation. PRDX6 activation generates reactive oxygen species via NADPH oxidase, reducing the palmitoylation of receptor-associated Gαi in a JNK-dependent manner...
September 29, 2017: Nature Communications
https://www.readbyqxmd.com/read/28950813/a-review-on-the-antinociceptive-effects-of-mitragyna-speciosa-and-its-derivatives-in-animal-model
#12
Kok-Yong Chin, Wun Fui Mark-Lee
Mitragyna speciosa is a tropical plant with narcotic effects. The antinociceptive effects of its crude extracts, bioactive compounds and structurally modified derivatives have been examined in rodent models. This review aims to summarize the evidence on the antinociceptive effects of M. speciosa and its derivatives and explore whether they can offer an alternative to morphine in pain management. Methanolic and alkaloid extracts of M. speciosa were shown to attenuate the nociceptive response in rodents. Mitragynine and 7-hydroxymitragynine offered better antinociceptive effects than crude extracts...
September 25, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28942046/chronic-ethanol-exposure-increases-inhibition-of-optically-targeted-phasic-dopamine-release-in-the-nucleus-accumbens-core-and-medial-shell-ex-vivo
#13
James R Melchior, Sara R Jones
Dopamine signaling encodes reward learning and motivated behavior through modulation of synaptic signaling in the nucleus accumbens, and aberrations in these processes are thought to underlie obsessive behaviors associated with alcohol abuse. The nucleus accumbens is divided into core and shell sub-regions with overlapping but also divergent contributions to behavior. Here we optogenetically targeted dopamine projections to the accumbens allowing us to isolate stimulation of dopamine terminals ex vivo. We applied 5 pulse (phasic) light stimulations to probe intrinsic differences in dopamine release parameters across regions...
September 20, 2017: Molecular and Cellular Neurosciences
https://www.readbyqxmd.com/read/28939474/heroin-induced-suppression-of-saccharin-intake-in-oprm1-a118g-mice
#14
Christopher S Freet, Danielle N Alexander, Caesar G Imperio, Victor Ruiz-Velasco, Patricia S Grigson
The single nucleotide polymorphism of the μ-opioid receptor, OPRM1 A118G, has been associated with greater drug and alcohol use, increased sensitivity to pain, and reduced sensitivity to the antinociceptive effects of opiates. In the present studies, we employed a 'humanized' mouse model containing the wild-type (118AA) or variant (118GG) allele to examine behavior in a model of heroin-induced devaluation of an otherwise palatable saccharin cue when repeated saccharin-heroin pairings occurred every 24h (Experiment 1) or every 48h (Experiment 2)...
September 20, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28893975/agonist-dependent-and-independent-%C3%AE%C2%BA-opioid-receptor-phosphorylation-distinct-phosphorylation-patterns-and-different-cellular-outcomes
#15
Yi-Ting Chiu, Chongguang Chen, Daohai Yu, Stefan Schulz, Lee-Yuan Liu-Chen
We reported previously that the selective agonist U50,488H promoted phosphorylation of the mouse κ opioid receptor (KOPR) at residues S356, T357, T363, and S369. Here, we found that agonist (U50,488H)-dependent KOPR phosphorylation at all the residues was mediated by Gi/o α proteins and multiple protein kinases [GRK2, GRK3, GRK5, GRK6 and protein kinase C (PKC)]. In addition, PKC activation by phorbol ester induced agonist-independent KOPR phosphorylation. Compared with U50,488H, PKC activation promoted much higher S356/T357 phosphorylation, much lower T363 phosphorylation, and similar levels of S369 phosphorylation...
November 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28893017/a-comparative-study-of-analgesic-effect-of-intrathecal-nalbuphine-and-fentanyl-as-adjuvant-in-lower-limb-orthopaedic-surgery
#16
Shagufta Naaz, Usha Shukla, Swati Srivastava, Erum Ozair, Adil Asghar
INTRODUCTION: Intrathecal opioids when added to local anaesthetics decrease their dosage and provide haemodynamic stability. Nalbuphine is an agonist-antagonist and acts on kappa receptors providing analgesia. AIM: The study aims to compare the analgesic efficacy of fentanyl with that of two doses of nalbuphine when used with injection bupivacaine heavy in spinal anaesthesia. MATERIALS AND METHODS: A randomised, double blinded, prospective study on 90 patients of ASA I and II undergoing lower limb orthopaedic surgery under subarachnoid block was done...
July 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28886759/epigenetic-regulation-of-the-kappa-opioid-receptor-by-child-abuse
#17
Pierre-Eric Lutz, Jeffrey A Gross, Sabine K Dhir, Gilles Maussion, Jennie Yang, Alexandre Bramoulle, Michael J Meaney, Gustavo Turecki
BACKGROUND: Experiences of abuse and neglect during childhood are major predictors of the emergence of depressive and suicidal behaviors throughout life. The underlying biological mechanisms, however, remain poorly understood. Here, we focused on the opioid system as a potential brain substrate mediating these effects. METHODS: Postmortem samples from three brain structures regulating social bonds and emotions were analyzed. Groups were constituted of depressed individuals who died by suicide, with or without a history of severe child abuse, and of psychiatrically healthy control subjects...
July 27, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28844812/antidepressant-like-effects-of-3-carboxamido-seco-nalmefene-3cs-nalmefene-a-novel-opioid-receptor-modulator-in-a-rat-ifn-%C3%AE-induced-depression-model
#18
Charlotte K Callaghan, Jennifer Rouine, Reginald L Dean, Brian I Knapp, Jean M Bidlack, Daniel R Deaver, Shane M O'Mara
Patients receiving the cytokine immunotherapy, interferon-alpha (IFN-α) frequently present with neuropsychiatric consequences and cognitive impairments. Patients (25-80%) report symptoms of depression, including, anhedonia, irritability, fatigue and impaired motivation. Our lab has previously demonstrated treatment (170,000IU/kg sc, 3 times per week for 4weeks) of the pro-inflammatory cytokine, IFN-α, induced a depressive phenotype in rats in the forced swim test (FST). Here, we examine the biological mechanisms underlying behavioral changes induced by IFN-α, which may be reflective of mechanisms underlying inflammation associated depression...
August 24, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28830758/the-medicinal-chemistry-and-neuropharmacology-of-kratom-a-preliminary-discussion-of-a-promising-medicinal-plant-and-analysis-of-its-potential-for-abuse
#19
REVIEW
Andrew C Kruegel, Oliver Grundmann
The leaves of Mitragyna speciosa (commonly known as kratom), a tree endogenous to parts of Southeast Asia, have been used traditionally for their stimulant, mood-elevating, and analgesic effects and have recently attracted significant attention due to increased use in Western cultures as an alternative medicine. The plant's active alkaloid constituents, mitragynine and 7-hydroxymitragynine, have been shown to modulate opioid receptors, acting as partial agonists at mu-opioid receptors and competitive antagonists at kappa- and delta-opioid receptors...
August 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28807672/pharmacological-characterization-of-novel-synthetic-opioids-nso-found-in-the-recreational-drug-marketplace
#20
REVIEW
Michael H Baumann, Susruta Majumdar, Valerie Le Rouzic, Amanda Hunkele, Rajendra Uprety, Xi Ping Huang, Jin Xu, Bryan L Roth, Ying-Xian Pan, Gavril W Pasternak
Novel synthetic opioids (NSO) are increasingly encountered in illicit heroin and counterfeit pain pills. Many NSO are resurrected from older biomedical literature or patent applications, so limited information is available about their biological effects. Here we examined the pharmacology of three structurally-distinct NSO found in the recreational drug market: N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylbutyramide (butyrylfentanyl), 3,4-dichloro-N-[(1R,2R)-2-(dimethylamino)cyclohexyl]-N-methylbenzamide (U-47700) and 1-cyclohexyl-4-(1,2-diphenylethyl)piperazine (MT-45)...
August 11, 2017: Neuropharmacology
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