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https://www.readbyqxmd.com/read/28219718/a-novel-regulatory-role-of-rgs4-in-stat5b-activation-neurite-outgrowth-and-neuronal-differentiation
#1
Paschalina Pallaki, Eirini-Maria Georganta, Ioannis Serafimidis, Maria-Pagona Papakonstantinou, Vassilis Papanikolaou, Sofia Koutloglou, Elsa Papadimitriou, Adamantia Agalou, Aggeliki Tserga, Alexandra Simeonof, Dimitra Thomaidou, Maria Gaitanou, Zafiroula Georgoussi
The Regulator of G protein Signalling 4 (RGS4) is a multitask protein that interacts with and negatively modulates opioid receptor signalling. Previously, we showed that the δ-opioid receptor (δ-OR) forms a multiprotein signalling complex consisting of Gi/Go proteins and the Signal Transducer and Activator of Transcription 5B (STAT5B) that leads to neuronal differentiation and neurite outgrowth upon δ-ΟR activation. Here, we investigated whether RGS4 could participate in signalling pathways to regulate neurotropic events...
February 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28218838/design-and-synthesis-of-enantiomerically-pure-decahydroquinoxalines-as-potent-and-selective-%C3%AE%C2%BA-opioid-receptor-agonists-with-anti-inflammatory-activity-in-vivo
#2
Michael Soeberdt, Peter Molenveld, Roy P M Storcken, Renaud Bouzanne des Mazery, Geert Jan Sterk, Reshma Autar, Marjon G Bolster, Clemens Wagner, Sebastianus N H Aerts, Frank R van Holst, Anita Wegert, Giovanni Tangherlini, Bastian Frehland, Dirk Schepmann, Dieter Metze, Tobias Lotts, Ulrich Knie, Kun-Yuan Lin, Tai-Yu Huang, Chih-Ching Lai, Sonja Ständer, Bernhard Wünsch, Christoph Abels
In order to develop novel κ agonists restricted to the periphery, a diastereo- and enantioselective synthesis of (4aR,5S,8aS)-configured decahydroquinoxalines 5-8 was developed. Physicochemical and pharmacological properties were fine-tuned by structural modifications in the arylacetamide and amine part of the pharmacophore as well as in the amine part outside the pharmacophore. The decahydroquinoxalines 5-8 show single-digit nanomolar to subnanomolar κ-opioid receptor affinity, full κ agonistic activity in the [(35)S]GTPγS assay, and high selectivity over μ, δ, σ1, and σ2 receptors as well as the PCP binding site of the NMDA receptor...
February 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28216062/nalmefene-reduces-reward-anticipation-in-alcohol-dependence-an-experimental-functional-magnetic-resonance-imaging-study
#3
Darren R Quelch, Inge Mick, John McGonigle, Anna C Ramos, Remy S A Flechais, Mark Bolstridge, Eugenii Rabiner, Matthew B Wall, Rexford D Newbould, Björn Steiniger-Brach, Franz van den Berg, Malcolm Boyce, Dorrit Østergaard Nilausen, Lasse Breuning Sluth, Didier Meulien, Christoph von der Goltz, David Nutt, Anne Lingford-Hughes
BACKGROUND: Nalmefene is a µ- and δ-opioid receptor antagonist, κ-opioid receptor partial agonist that has recently been approved in Europe for treating alcohol dependence. It offers a treatment approach for alcohol-dependent individuals with "high-risk drinking levels" to reduce their alcohol consumption. However, the neurobiological mechanism underpinning its effects on alcohol consumption remains to be determined. Using a randomized, double-blind, placebo-controlled, within-subject crossover design we aimed to determine the effect of a single dose of nalmefene on striatal blood oxygen level-dependent (BOLD) signal change during anticipation of monetary reward using the monetary incentive delay task following alcohol challenge...
January 10, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28212204/1-2-4-dibromophenyl-3-6-6-trimethyl-1-5-6-7-tetrahydro-4h-indazol-4-one-a-novel-opioid-receptor-agonist-with-less-accompanying-gastrointestinal-dysfunction-than-morphine
#4
Po-Kuan Chao, Shau-Hua Ueng, Li-Chin Ou, Teng-Kuang Yeh, Wan-Ting Chang, Hsiao-Fu Chang, Shu-Chun Chen, Pao-Luh Tao, Ping-Yee Law, Horace H Loh, Ming-Fu Cheng, Jian-Ying Chuang, Chiung-Tong Chen, Chuan Shih, Shiu-Hwa Yeh
BACKGROUND: The authors investigated the pharmacology and signaling pathways of the opioid receptors modulated by compound 1, 1-(2,4-dibromophenyl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one. METHODS: In vitro studies of compound 1 were assessed by using a radioligand-binding assay (n = 3), a cyclic adenosine monophosphate assay (n = 3), a β-arrestin assay (n = 3), an internalization assay (n = 3), and an immunohistochemistry (n = 8). In vivo studies of compound 1 were characterized using a tail-flick test (n = 5 to 6), tail-clip test (n = 7), von Frey hair test (n = 5), and charcoal meal test (n = 5)...
February 17, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28190898/synthesis-and-opioid-receptor-binding-of-indium-iii-and-111-in-labeled-macrocyclic-conjugates-of-diprenorphine-novel-ligands-designed-for-imaging-studies-of-peripheral-opioid-receptors
#5
Shefali Srivastava, Emily A Fergason-Cantrell, Roger I Nahas, John R Lever
Radiolabeled diprenorphine (DPN) and analogs are widely used ligands for non-invasive brain imaging of opioid receptors. To develop complementary radioligands optimized for studies of the peripheral opioid receptors, we prepared a pair of hydrophilic DPN derivatives, conjugated to the macrocyclic chelator DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), for complexation with trivalent metals. The non-radioactive indium (III) complexes, tethered to the C6-oxygen position of the DPN scaffold by 6- to 9-atom spacers, displayed high affinities for binding to μ, δ and κ opioid receptors in vitro...
October 6, 2016: Tetrahedron
https://www.readbyqxmd.com/read/28182309/propagation-of-the-allosteric-modulation-induced-by-sodium-in-the-%C3%AE-opioid-receptor
#6
Xianqiang Sun, Genevieve Laroche, Xu Wang, Hans Ågren, Greg Bowman, Patrick M Giguère, Yaoquan Tu
Allosteric sodium in the helix bundle of a G protein-coupled receptor (GPCR) can modulate the receptor activation on the intracellular side. This phenomenon has confounded the GPCR community for decades. In this work, we present a theoretical model that reveals the mechanism of the allosteric modulation induced by sodium in the δ opioid receptor. We found that the allosteric sodium ion exploits a distinct conformation of the key residue Trp2746.48 to propagate the modulation to helixes 5 and 6, which further transmits along the helixes and regulates their positions on the intracellular side...
February 9, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28181908/effects-of-endogenous-cardioprotective-mechanisms-on-ischemia-reperfusion-injury
#7
Marcin Kunecki, Wojciech Płazak, Piotr Podolec, Krzysztof S Gołba
Ischemic heart disease have been remarked as a leading cause of morbidity and mortality in adults. Early restoration of cardiac perfusion is necessary to restore perfusion of ischemic heart muscle. Effective revascularization reduce mortality by limiting myocardial necrosis at the acute phase of the cardiac infarction. However, reperfusion may induce a cascade of pathophysiological reactions causing the increase of the infarct area of the myocardium This phenomenon known as ischemia-reperfusion injury is responsible for up to 50% of the final infarct size...
January 10, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
https://www.readbyqxmd.com/read/28167156/eluxadoline-demonstrates-a-lack-of-abuse-potential-in-phase-2-and-3-studies-of-patients-with-irritable-bowel-syndrome-with-diarrhea
#8
Reginald V Fant, Jack E Henningfield, Brooks D Cash, Leonard S Dove, Paul S Covington
BACKGROUND & AIMS: Eluxadoline is approved by the Food and Drug Administration for the treatment of adults with irritable bowel syndrome with diarrhea (IBS-D). Eluxadoline is a locally acting mixed μ- and κ-opioid receptor agonist and δ-opioid receptor antagonist. The abuse potential of eluxadoline was evaluated as part of the Phase 2 and 3 clinical trials assessing the efficacy, safety, and tolerability of the drug. METHODS: One Phase 2 (IBS-2001) and 2 Phase 3 (IBS-3001 and IBS-3002) randomized controlled trials enrolled patients meeting Rome III criteria for IBS-D...
February 3, 2017: Clinical Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28144772/a-combined-opiate-agonist-and-antagonist-treatment-reduces-prolactin-secreting-pituitary-tumor-growth
#9
George Maglakelidze, Olivia Wynne, Dipak K Sarkar
Prolactin secreting pituitary adenomas (prolactinomas) is the most common pituitary tumors in humans. Animal studies have identified aggressive prolactinoma development in fetal alcohol exposed rats. We have recently identified a combination treatment of a μ opioid receptor antagonist naltrexone and a δ opioid receptor agonist D-Ala2-,N-Me-Phe4,Gly-ol Enkephalin (DPDPE) increases innate immune function. In this study, we tested whether naltrexone and DPDPE combination therapy is useful to control pituitary tumor growth...
January 31, 2017: Journal of Cell Communication and Signaling
https://www.readbyqxmd.com/read/28115487/cholinergic-interneurons-underlie-spontaneous-dopamine-release-in-nucleus-accumbens
#10
Jordan T Yorgason, Douglas M Zeppenfeld, John T Williams
: The release of dopamine from terminals in the nucleus accumbens (NAc) is regulated by a number of factors, including voltage gated ion channels, D2-autoreceptors and nicotinic acetylcholine receptors (nAChRs). Cholinergic interneurons (CINs) drive dopamine release through activation of nAChRs on dopamine terminals. Using cyclic voltammetry in mouse brain slices, nAChR-dependent spontaneous dopamine transients and the mechanisms underlying the origin were examined in the NAc. Spontaneous events were infrequent (0...
January 23, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28107753/role-of-central-opioid-on-the-antinociceptive-effect-of-sulfated-polysaccharide-from-the-red-seaweed-solieria-filiformis-in-induced-temporomandibular-joint-pain
#11
Ianna Wivianne Fernandes Araújo, Hellíada Vasconcelos Chaves, José Mário Pachêco, Danielle Rocha Val, Lorena Vasconcelos Vieira, Rodrigo Santos, Raul Sousa Freitas, Renata Line Rivanor, Valdécio Silvano Monteiro, Juliana Trindade Clemente-Napimoga, Mirna Marques Bezerra, Norma Maria Barros Benevides
This study aimed to investigate the effect of sulfated polysaccharide from red seaweed Solieria filiformis (Fraction F II) in the inflammatory hypernociception in the temporomandibular joint (TMJ) of rats. Male Wistar rats were pretreated (30min) with a subcutaneous injection (s.c.) of vehicle or FII (0.03, 0.3 or 3.0mg/kg) followed by intra-TMJ injection of 1.5% Formalin or 5-hydroxytryptamine (5-HT, 225μg/TMJ). In other set of experiments rats were pretreated (15min) with an intrathecal injection of the non-selective opioid receptors Naloxone, or μ-opioid receptor antagonist CTOP, or δ-opioid receptor Naltridole hydrochloride, or κ-opioid receptor antagonist Nor-Binaltorphimine (Nor-BNI) followed by injection of FII (s...
January 17, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28105278/hydrazone-linker-as-a-useful-tool-for-preparing-chimeric-peptide-nonpeptide-bifunctional-compounds
#12
Jolanta Dyniewicz, Piotr F J Lipiński, Piotr Kosson, Anna Leśniak, Marta Bochyńska-Czyż, Adriana Muchowska, Dirk Tourwé, Steven Ballet, Aleksandra Misicka, Andrzej W Lipkowski
The area of multitarget compounds, joining two pharmacophores within one molecule, is a vivid field of research in medicinal chemistry. Not only pharmacophoric elements are essential for the design and activity of such compounds, but the type and length of linkers used to connect them are also crucial. In the present contribution, we describe compound 1 in which a typical opioid peptide sequence is combined with a fragment characteristic for neurokinin-1 receptor (NK1R) antagonists through a hydrazone bridge...
January 12, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28065754/mechanisms-involved-in-antinociception-induced-by-a-polysulfated-fraction-from-seaweed-gracilaria-cornea-in-the-temporomandibular-joint-of-rats
#13
Chistiane Oliveira Coura, Hellíada Vasconcelos Chaves, Danielle Rocha do Val, Lorena Vasconcelos Vieira, Felipe Dantas Silveira, Fernanda Maxcynne Lino Dos Santos Lopes, Francisco Isaac Fernandes Gomes, Annyta Fernandes Frota, Ricardo Basto Souza, Juliana Trindade Clemente-Napimoga, Mirna Marques Bezerra, Norma Maria Barros Benevides
Temporomandibular disorder is a common clinical condition involving pain in the temporomandibular joint (TMJ) region. This study assessed the antinociceptive effects of a polysulfated fraction from the red seaweed Gracilaria cornea (Gc-FI) on the formalin-induced TMJ hypernociception in rats and investigated the involvement of different mechanisms. Male Wistar rats were pretreated with injection (sc) of saline or Gc-FI 1h before intra- TMJ injection of formalin to evaluate the nociception. The results showed that pretreatment with Gc-FI significantly reduced formalin-induced nociceptive behavior...
April 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28063353/rationally-designed-benzopyran-fused-isoxazolidines-and-derived-%C3%AE-2-3-3-amino-alcohols-as-potent-analgesics-synthesis-biological-evaluation-and-molecular-docking-analysis
#14
Gagandeep Singh, Gurjit Singh, Rajbir Bhatti, Vivek Gupta, Ajay Mahajan, Palwinder Singh, Mohan Paul Singh Ishar
Based on structure activity analysis of morphine related opiates, we have synthesized some novel benzopyran fused isoxazolidines (2a-e) and derived conformationally constrained β(2,3,3)-amino alcohols (3a-e), which were evaluated in vivo for their anti-nociceptive activity through acetic acid induced writhing test (peripheral) and formalin induced algesia (central). Results showed that, compound 2a possesses significant opioid agonist activity. Further, molecular docking analysis reveals that compound 2a binds to δ-opioid receptor (DOR) with comparatively better D-score than to μ (MOR) and κ (KOR) receptors...
February 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28050773/the-effect-of-chronic-intermittent-hypoxia-on-respiratory-sensitivity-to-morphine-in-rats
#15
Jian Wu, Peng Li, Xiuying Wu
PURPOSE: Chronic intermittent hypoxia (CIH) is a characteristic of obstructive sleep apnea syndromes (OSAs). Recurrent hypoxia during the developmental period increases respiratory sensitivity to subsequent administration of opioids. However, it is unknown whether CIH affects respiratory sensitivity to opioids in adults. Our study aimed to assess the changes in respiratory sensitivity to morphine (MOR) under CIH and to explore the possible mechanisms in an adult rat model. METHODS: We applied CIH in adult Sprague-Dawley rats to simulate the hypoxia condition caused by OSAs...
January 3, 2017: Sleep & Breathing, Schlaf & Atmung
https://www.readbyqxmd.com/read/28049031/the-efficacy-of-dynorphin-fragments-at-the-%C3%AE%C2%BA-%C3%AE-and-%C3%AE-opioid-receptor-in-transfected-hek-cells-and-in-an-animal-model-of-unilateral-peripheral-inflammation
#16
M Morgan, A Heffernan, F Benhabib, S Wagner, A K Hewavitharana, P N Shaw, P J Cabot
Dynorphin 1-17 is an endogenous peptide that is released at sites of inflammation by leukocytes, binding preferentially to κ-opioid receptors (KOP) to mediate nociception. We have previously shown that dynorphin 1-17 is rapidly biotransformed to smaller peptide fragments in inflamed tissue homogenate. This study aimed to determine the efficacy and potency of selected dynorphin fragments produced in an inflamed environment at the KOP, μ and δ-opioid receptors (MOP and DOP respectively) and in a model of inflammatory pain...
December 31, 2016: Peptides
https://www.readbyqxmd.com/read/28033462/the-pharmacological-heterogeneity-of-nepenthone-analogs-in-conferring-highly-selective-and-potent-%C3%AE%C2%BA-opioid-agonistic-activities
#17
Wei Li, Jian-Dong Long, Yuan-Yuan Qian, Yu Long, Xue-Jun Xu, Yu-Jun Wang, Qing Shen, Zuo-Neng Wang, Xi-Cheng Yang, Li Xiao, Hong-Peng Sun, Yu-Long Xu, Yi-Yi Chen, Qiong Xie, Yong-Hui Wang, Li-Ming Shao, Jing-Gen Liu, Zhui-Bai Qiu, Wei Fu
To develop novel analgesics with no side effects or less side effects than traditional opioids is highly demanded to treat opioid receptor mediated pain and addiction issues. Recently, κ-opioid receptor (KOR) has been established as an attractive target, although its selective agonists could bear heterogeneous pharmacological activities. In this study, we designed and synthesized two new series of nepenthone derivatives by inserting a spacer (carbonyl) between 6α,14α-endo-ethenylthebaine and the 7α-phenyl substitution of the skeleton and by substituting the 17-N-methyl group with a cyclopropylmethyl group...
January 19, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28001096/targeting-delta-opioid-receptors-for-pain-treatment-drugs-in-phase-i-and-ii-clinical-development
#18
Viola Spahn, Christoph Stein
Opioids are widely used to treat severe pain. Most clinically used opioids activate µ-opioid receptors (MOR). Their ligands induce potent analgesia but also adverse effects. The δ-opioid receptor (DOR) is another member of the opioid receptor family that has been under intense investigation with the aim to avoid MOR-induced side effects. Areas covered: This article reviews DOR ligands which appeared to be promising after preclinical evaluation. A literature search using Pubmed, Cochrane library, ClinicalTrials...
February 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/27922029/safety-of-eluxadoline-in-patients-with-irritable-bowel-syndrome-with-diarrhea
#19
Brooks D Cash, Brian E Lacy, Philip S Schoenfeld, Leonard S Dove, Paul S Covington
OBJECTIVES: Eluxadoline is a mixed μ-opioid receptor (OR) and κ-OR agonist and δ-OR antagonist, approved for the treatment of irritable bowel syndrome with diarrhea (IBS-D). This analysis evaluated the safety and tolerability of eluxadoline 75 and 100 mg twice daily (BID) in one Phase 2 (IBS-2001) and two Phase 3 (IBS-3001 and IBS-3002) studies. METHODS: Adults with IBS-D (Rome III criteria) were randomized to placebo or eluxadoline (75 or 100 mg) BID for 12 (IBS-2001), 26 (IBS-3002), or 52 (IBS-3001) weeks...
February 2017: American Journal of Gastroenterology
https://www.readbyqxmd.com/read/27909965/correction-of-negative-effect-of-antenatal-hypoxia-on-liver-tissue-homeostasis-in-newborn-albino-rats-with-opioid-peptides
#20
O G Pinaeva, E N Sazonova, O A Lebed'ko, S S Timoshin
We studied the possibility of correction of the negative effects of antenatal hypoxia on the liver tissue homeostasis in 7-day-old albino rats by administration of opioid peptides in a dose of 100 μg/kg on postnatal days 2-6. Administration of mixed μ/δ-opioid receptor agonist Dalargin neutralized deviations of gravimetric indicators, parameters of proliferative activity, and activity of the nucleolar apparatus of hepatocytes. Administration of the non-opiate Leu-enkephalin analogue did not normalize gravimetric parameters and nucleolar apparatus parameters, however, it significantly increased the pool of proliferating hepatocytes...
December 2016: Bulletin of Experimental Biology and Medicine
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