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Kappa opioid receptor

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https://www.readbyqxmd.com/read/29441714/time-dependent-regional-brain-distribution-of-methadone-and-naltrexone-in-the-treatment-of-opioid-addiction
#1
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/29436492/allosterism-within-delta-opioid-kappa-opioid-receptor-heteromers-in-peripheral-sensory-neurons-regulation-of-kappa-opioid-agonist-efficacy
#2
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/29426768/o6c-20-nor-salvinorin-a-is-a-stable-and-potent-kor-agonist
#3
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/29396147/focusing-on-the-opioid-system-for-addiction-biomarker-discovery
#4
REVIEW
Raoul Belzeaux, Laurence Lalanne, Brigitte L Kieffer, Pierre-Eric Lutz
Substance use disorders (SUD) and behavioral addictions are devastating conditions that impose a severe burden on all societies, and represent difficult challenges for clinicians. Therefore, biomarkers are urgently needed to help predict vulnerability, clinical course, and response to treatment. Here, we elaborate on the potential for addiction biomarker discovery of the opioid system, particularly within the emerging framework aiming to probe opioid function in peripheral tissues. Mu, delta, and kappa opioid receptors all critically regulate neurobiological and behavioral processes that define addiction, and are also targeted by major pharmacotherapies used in the management of patients with SUD...
January 27, 2018: Trends in Molecular Medicine
https://www.readbyqxmd.com/read/29377758/levorphanol-for-treatment-of-intractable-neuropathic-pain-in-cancer-patients
#5
Akhila Reddy, Amy Ng, Tarun Mallipeddi, Eduardo Bruera
Neuropathic pain in cancer patients is often difficult to treat, requiring a combination of several different pharmacological therapies. We describe two patients with complex neuropathic pain syndromes in the form of phantom limb pain and Brown-Sequard syndrome who did not respond to conventional treatments but responded dramatically to the addition of levorphanol. Levorphanol is a synthetic strong opioid that is a potent N-methyl-d-aspartate receptor antagonist, mu, kappa, and delta opioid receptor agonist, and reuptake inhibitor of serotonin and norepinephrine...
January 29, 2018: Journal of Palliative Medicine
https://www.readbyqxmd.com/read/29376435/insights-into-future-therapeutics-for-atopic-dermatitis
#6
Taylor Edwards, Nupur U Patel, Amy Blake, Samantha Prabakaran, Danielle Reimer, Steven R Feldman, Lindsay C Strowd
Atopic Dermatitis (AD) is a common chronic inflammatory skin disorder with a constellation of symptoms. Currently, there are numerous therapies in various phases of drug development that target the pathogenesis of AD. Areas covered: Our paper aims to examine small molecule therapies and other novel agents registered for clinical trial in the phase II and mainly phase III stages of development. A literature search using PubMed as well as Clinicaltrials.gov was conducted. Clinical trial evidence of these novel agents was compiled and assessed...
February 2018: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/29371114/a-kappa-opioid-receptor-agonist-blocks-bone-cancer-pain-without-altering-bone-loss-tumor-size-or-cancer-cell-proliferation-in-a-mouse-model-of-cancer-induced-bone-pain
#7
Katie A Edwards, Joshua J Havelin, Mary I Mcintosh, Haley A Ciccone, Kathlene Pangilinan, Ian Imbert, Tally M Largent-Milnes, Tamara King, Todd W Vanderah, John M Streicher
Breast cancer metastasizes to bone, diminishing quality of life of patients due to pain, fracture, and limited mobility. Cancer-induced bone pain (CIBP) is characterized as moderate to severe ongoing pain, primarily managed by Mu opioid agonists such as fentanyl. However, opioids are limited by escalating doses and serious side effects. One alternative may be kappa opioid receptor (KOR) agonists. There are few studies examining KOR efficacy on CIBP, while KOR agonists are efficacious in peripheral and inflammatory pain...
January 22, 2018: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/29369967/lateralized-kappa-opioid-receptor-signaling-from-the-amygdala-central-nucleus-promotes-stress-induced-functional-pain
#8
Kelsey M Nation, Milena DeFelice, Pablo I Hernandez, David W Dodick, Volker Neugebauer, Edita Navratilova, Frank Porreca
The diffuse noxious inhibitory controls (DNIC) response is often decreased, or lost, in stress-related functional pain syndromes. As the dynorphin/kappa opioid receptor (KOR) pathway is activated by stress, we determined its role in DNIC using a model of stress-induced functional pain. Male, Sprague Dawley rats were primed for 7 days with systemic morphine resulting in opioid-induced hyperalgesia. Fourteen days after priming, when hyperalgesia was resolved, rats were exposed to environmental stress and DNIC was evaluated by measuring hindpaw response threshold to noxious pressure (test stimulus) following capsaicin injection in the forepaw (conditioning stimulus)...
January 23, 2018: Pain
https://www.readbyqxmd.com/read/29355609/is-nociception-mechanism-altered-in-offspring-of-morphine-abstinent-rats
#9
Ghorbangol Ashabi, Mitra-Sadat Sadat-Shirazi, Ardeshir Akbarabadi, Nasim Vousooghi, Zahra Kheiri, Heidar Toolee, Solmaz Khalifeh, Mohammad-Reza Zarrindast
To investigate the effect of parental drug abuse on children, nociception, electrophysiological alteration, mRNA expression of opioid receptors, and expression of certain intracellular proteins in offspring of morphine-abstinent rats were studied. Adult male and female animals received water soluble morphine for 21 days. Ten days after the last morphine administration, animals were placed for mating in four groups as follows: healthy (drug naïve) female and male, morphine-abstinent female and healthy male, morphine-abstinent male and healthy female, morphine-abstinent male and morphine-abstinent female...
January 18, 2018: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/29336871/epigenetic-regulation-of-the-kappa-opioid-receptor-gene-by-an-insertion-deletion-in-the-promoter-region
#10
Pierre-Eric Lutz, Daniel Almeida, Raoul Belzeaux, Ipek Yalcin, Gustavo Turecki
Preclinical and clinical studies have demonstrated that the kappa opioid receptor (KOR) regulates reward, hedonic tone and emotions. At therapeutic level, on-going clinical trials are assessing the potential of targeting the KOR for the management of depression, anxiety disorders and substance use disorders. However, genetic polymorphisms in the KOR gene that potentially contribute to its implication in these phenotypes have been poorly studied. Here we investigated an insertion-deletion in the promoter region of KOR (rs35566036), recently associated with alcohol addiction, in a cohort of depressed subjects who died by suicide, as well as psychiatrically healthy individuals...
January 11, 2018: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29296674/dynamic-strategic-bond-analysis-yields-a-ten-step-synthesis-of-20-nor-salvinorin-a-a-potent-%C3%AE%C2%BA-or-agonist
#11
Jeremy J Roach, Yusuke Sasano, Cullen L Schmid, Saheem Zaidi, Vsevolod Katritch, Raymond C Stevens, Laura M Bohn, Ryan A Shenvi
Salvinorin A (SalA) is a plant metabolite that agonizes the human kappa-opioid receptor (κ-OR) with high affinity and high selectivity over mu- and delta-opioid receptors. Its therapeutic potential has stimulated extensive semisynthetic studies and total synthesis campaigns. However, structural modification of SalA has been complicated by its instability, and efficient total synthesis has been frustrated by its dense, complex architecture. Treatment of strategic bonds in SalA as dynamic and dependent on structural perturbation enabled the identification of an efficient retrosynthetic pathway...
December 27, 2017: ACS Central Science
https://www.readbyqxmd.com/read/29273415/design-synthesis-and-opioid-activity-of-arodyn-analogs-cyclized-by-ring-closing-metathesis-involving-tyr-allyl
#12
Wei-Jie Fang, Thomas F Murray, Jane V Aldrich
Kappa (κ) opioid receptor selective antagonists are useful pharmacological tools in studying κ opioid receptors and have potential to be used as therapeutic agents for the treatment of a variety of diseases including mood disorders and drug addiction. Arodyn (Ac[Phe1-3,Arg4,d-Ala8]Dyn A-(1-11)NH2) is a linear acetylated dynorphin A (Dyn A) analog that is a potent and selective κ opioid receptor antagonist (Bennett et al. J Med Chem 2002;45:5617-5619) and prevents stress-induced reinstatement of cocaine-seeking behavior following central administration (Carey et al...
November 21, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29259946/genetic-analysis-of-mu-and-kappa-opioid-receptor-and-comt-enzyme-in-cancer-pain-tunisian-patients-under-opioid-treatment
#13
Imen Chatti, Jean-Baptiste Woillard, Amira Mili, Isabelle Creveaux, Ilhem Ben Charfeddine, Jihène Feki, Sarah Langlais, Leila Ben Fatma, Ali Saad, Moez Gribaa, Frédéric Libert
Background: Pain and its opioid treatments are complex measurable traits. Responses to morphine in terms of pain control is likely to be determined by many factors, including the underlying pain sensitivity of the patient, along with nature and extent of the painful process, concomitant medications, genetic and other clinical and environmental factors. This study investigated genetic polymorphisms implicated in the inter-individual pain response variability to opioid treatment in the Tunisian population...
December 2017: Iranian Journal of Public Health
https://www.readbyqxmd.com/read/29248520/new-therapies-for-atopic-dermatitis-additional-treatment-classes
#14
Paras P Vakharia, Jonathan I Silverberg
BACKGROUND: A wide array of miscellaneous agents is being studied for the treatment of atopic dermatitis (AD), including targeted topical, oral systemic and biologic agents. OBJECTIVE: To review the known efficacy and safety to-date for such agents being studied for the treatment of AD. METHODS: A non-systematic review of the literature was performed. PubMed and ClinicalTrials.gov were searched for studies assessing agents not described in previous chapters for the treatment of AD...
December 14, 2017: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/29233847/pharmacological-evidence-for-a-putative-conserved-allosteric-site-on-opioid-receptors
#15
Kathryn E Livingston, M Alexander Stanczyk, Neil Burford, Andrew Alt, Merixtell Canals, John R Traynor
Allosteric modulators of G protein-coupled receptors (GPCRs), including opioid receptors, have been proposed as possible therapeutic agents with enhanced selectivity. BMS-986122 is a positive allosteric modulator (PAM) of the mu-opioid receptor (μ-OR). BMS-986187 is a structurally distinct PAM for the delta-opioid receptor (δ-OR) that has been reported to show 100-fold selectivity in promoting δ-OR over μ-OR agonism. Here we use ligand binding and second messenger assays to show that BMS-986187 is actually an effective PAM at μ-OR and at the kappa opioid receptor (κ-OR), but is ineffective at the nociceptin receptor (NOPR)...
December 12, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29215139/a-novel-and-selective-nociceptin-receptor-nop-agonist-1-1-cis-4-isopropylcyclohexyl-piperidin-4-yl-1h-indol-2-yl-methanol-at-312-decreases-acquisition-of-ethanol-induced-conditioned-place-preference-in-mice
#16
Nurulain T Zaveri, Paul V Marquez, Michael E Meyer, Willma E Polgar, Abdul Hamid, Kabirullah Lutfy
BACKGROUND: Nociceptin/Orphanin FQ (N/OFQ), the endogenous peptide agonist for the opioid receptor-like (ORL1) receptor (also known as NOP or the nociceptin receptor), has been shown to block the acquisition and expression of ethanol-induced conditioned place preference (CPP). Here, we report the characterization of a novel small-molecule NOP ligand AT-312 (1-(1-((cis)-4-isopropylcyclohexyl)piperidin-4-yl)-1H-indol-2-yl)methanol) in receptor binding and GTPγS functional assays in vitro...
December 7, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29191753/melanin-concentrating-hormone-acts-through-hypothalamic-kappa-opioid-system-and-p70s6k-to-stimulate-acute-food-intake
#17
Amparo Romero-Picó, Estrella Sanchez-Rebordelo, Monica Imbernon, David González-Touceda, Cintia Folgueira, Ana Senra, Johan Fernø, Clémence Blouet, Roberto Cabrera, Margriet van Gestel, Roger A Adan, Miguel López, Rafael Maldonado, Ruben Nogueiras, Carlos Diéguez
Melanin-Concentrating Hormone (MCH) is one of the most relevant orexigenic factors specifically located in the lateral hypothalamic area (LHA), with its physiological relevance demonstrated in studies using several genetically manipulated mice models. However, the central mechanisms controlling MCH-induced hyperphagia remain largely uncharacterized. Here, we show that central injection of MCH in mice deficient for kappa opoid receptor (k-OR) failed to stimulate feeding. To determine the hypothalamic area responsible for this MCH/k-OR interaction, we performed virogenetic studies and found that downregulation of k-OR by adeno-associated viruses (shOprk1-AAV) in LHA, but not in other hypothalamic nuclei, was sufficient to block MCH-induced food intake...
December 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29156533/serotonin-induces-peripheral-antinociception-via-the-opioidergic-system
#18
Danielle Aguiar Diniz, Júlia Alvarenga Petrocchi, Larissa Caldeira Navarro, Tâmara Cristina Souza, Marina Gomes Miranda E Castor, Igor Dimitri Gama Duarte, Thiago Roberto Lima Romero
PURPOSE: Studies conducted since 1969 have shown that the release of serotonin (5-HT) in the dorsal horn of the spinal cord contributes to opioid analgesia. In the present study, the participation of the opioidergic system in antinociceptive effect serotonin at the peripheral level was examined. METHODS: The paw pressure test was used with mice (Swiss, males from 35 g) which had increased pain sensitivity by intraplantar injection of PGE2 (2 μg). Serotonin (250 ng), administered locally to the right paw of animals, produces antinociception in this model...
November 15, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29155273/mu-opioid-peptide-mop-and-nociceptin-orphanin-fq-peptide-nop-receptor-activation-both-contribute-to-the-discriminative-stimulus-properties-of-cebranopadol-in-the-rat
#19
Thomas M Tzschentke, Kris Rutten
The novel potent analgesic cebranopadol is an agonist at nociceptin/orphanin FQ peptide (NOP) and classical opioid receptors, with the highest in-vitro activity at NOP and mu-opioid peptide (MOP) receptors, and somewhat lower activity at kappa-opioid peptide (KOP) and delta-opioid peptide (DOP) receptors. We addressed the question of which of these pharmacological activities contribute to the stimulus properties of cebranopadol using a rat drug discrimination procedure. First, cebranopadol was tested in generalization tests against a morphine cue, including receptor-specific antagonism...
November 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29142121/the-role-of-kappa-opioid-receptors-in-glutamate-input-selection-in-the-ventral-striatum
#20
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
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