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https://www.readbyqxmd.com/read/28220108/adaptations-in-basal-and-hypothalamic-pituitary-adrenal-activated-deoxycorticosterone-responses-following-ethanol-self-administration-in-cynomolgus-monkeys
#1
Vanessa A Jimenez, Patrizia Porcu, A Leslie Morrow, Kathleen A Grant
Acute ethanol activates the hypothalamic-pituitary-adrenal (HPA) axis, while long-term exposure results in a blunted neuroendocrine state, particularly with regards to the primary endpoint, cortisol, the primary glucocorticoid produced in the adrenal cortex. However, it is unknown if this dampened neuroendocrine status also influences other adrenocortical steroids. Plasma concentration of the mineralocorticoid and neuroactive steroid precursor deoxycorticosterone (DOC) is altered by pharmacological challenges of the HPA axis in cynomolgus monkeys...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28219988/sex-differences-in-microglia-activity-within-the-periaqueductal-gray-of-the-rat-a-potential-mechanism-driving-the-dimorphic-effects-of-morphine
#2
H H Doyle, L N Eidson, D M Sinkiewicz, A Z Murphy
Although morphine remains the primary drug prescribed for alleviation of severe or persistent pain, both preclinical and clinical studies have shown that females require 2-3 times more morphine than males to produce comparable levels of analgesia. In addition to binding to the neuronal μ opioid receptor (MOR), morphine binds to the innate immune receptor toll-like receptor 4 (TLR4) localized primarily on microglia. Morphine action at TLR4 initiates a neuroinflammatory response that directly opposes the analgesic effects of morphine...
February 20, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28219718/a-novel-regulatory-role-of-rgs4-in-stat5b-activation-neurite-outgrowth-and-neuronal-differentiation
#3
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/28219707/22-azidosalvinorin-a-exhibits-antidepressant-like-effect-in-mice
#4
James Oluwagbamigbe Fajemiroye, Polepally Reddy Prabhakar, Carlos Luiz da Cunha, Elson Alves Costa, Jordan K Zjawiony
The increasing cases of depression has made the searches for new drugs and understanding of the underligning neurobiology of this psychiatric disorder a necessity. Here, we modified the structure of salvinorin A (a known halucinogen) and investigated antidepressant-like activity of its four derivatives; 22-methylsulfanylsalvinorin A(SA1), 2-O-cinnamoylsalvinorin B (CSB), 22-azidosalvinorin A (SA2), and 2-O-(4(')-azidophenylsulfonyl)salvinorin B (SA3). Prior to behavioural tests (Irwin test, open field test - OFT, forced swimming test - FST and tail suspension test - TST), SA1 was prepared by reacting salvinorin B and methylthioacetic acid with 89% yield; CSB was obtained from the reaction of salvinorin B and cinnamic acid with 92% yield; SA2 was obtained from the reaction of salvinorin B and azidoacetic acid with 81% yield; and SA3 was prepared by reacting salvinorin B with 4-azidophenylsulfonyl chloride with 80% yield...
February 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28219695/inhibitory-effects-of-dynorphin-3-14-on-the-lipopolysaccharide-induced-toll-like-receptor-4-signalling-pathway
#5
Siti Sarah Fazalul Rahiman, Michael Morgan, Paul Gray, Paul Nicholas Shaw, Peter John Cabot
Dynorphin 1-17 (DYN 1-17) is biotransformed rapidly to a range of fragments in rodent inflamed tissue with dynorphin 3-14 (DYN 3-14) being the most stable and prevalent. DYN 1-17 has been shown previously to be involved in the regulation of inflammatory response following tissue injury, in which the biotransformation fragments of DYN 1-17 may possess similar features. This study investigated the effects of DYN 3-14 on lipopolysaccharide (LPS)-induced nuclear factor-kappaB/p65 (NF-κB/p65) nuclear translocation and the release of pro-inflammatory cytokines interleukin-1beta (IL-1β) and tumor necrosis factor-alpha (TNF-α) in differentiated THP-1 cells...
February 17, 2017: Peptides
https://www.readbyqxmd.com/read/28218955/antihyperglycemiac-action-of-diosmin-a-citrus-flavonoid-is-induced-through-endogenous-%C3%AE-endorphin-in-type-i-like-diabetic-rats
#6
Chia-Chen Hsu, Mang Hung Lin, Juei Tang Cheng, Ming Chang Wu
Diosmin is one of the flavonoids contained in citrus and has been demonstrated to improve glucose metabolism in diabetic disorders. However, the mechanism(s) of diosmin in glucose regulation remain obscure. Therefore, we investigated the potential mechanism(s) for the antihyperglycemic action of diosmin in streptozotocin-induced diabetic rats (STZ-diabetic rats). Diosmin lowered hyperglycemia in a dose-dependent manner in STZ-diabetic rats. This action was inhibited by naloxone at a dose sufficient to block opioid receptors...
February 20, 2017: Clinical and Experimental Pharmacology & Physiology
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
#7
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
#8
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/28216001/loperamide-inhibits-sodium-channels-to-alleviate-inflammatory-hyperalgesia
#9
Ying Wu, Beiyan Zou, Lingli Liang, Min Li, Yuan-Xiang Tao, Haibo Yu, Xiaoliang Wang, Min Li
Previous studies demonstrated that Loperamide, originally known as an anti-diarrheal drug, is a promising analgesic agent primarily targeting mu-opioid receptors. However some evidences suggested that non-opioid mechanisms may be contributing to its analgesic effect. In the present study, Loperamide was identified as a Nav1.7 blocker in a pilot screen. In HEK293 cells expressing Nav1.7 sodium channels, Loperamide blocked the resting state of Nav1.7 channels (IC50 = 1.86 ± 0.11 μM) dose-dependently and reversibly...
February 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28215164/innovative-opioid-peptides-and-biased-agonism-novel-avenues-for-more-effective-and-safer-analgesics-to-treat-chronic-pain
#10
Andrea Bedini, Santi Mario Spampinato
Chronic pain is a clinically relevant and yet unsolved conditions that is poorly treated with the currently available drugs, thus highlighting the urgent need of innovative analgesics. Although opiates are not very effective in the treatment of inflammatory and neuropathic pain, developing novel opioid receptor peptide agonists, as well as modulating the opioid receptor-mediated responses in a ligand-specific fashion, may represent an innovative and promising strategy to identify more efficacious and safer antalgic drugs...
February 15, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28214687/gastroprotective-effect-and-mechanism-of-action-of-croton-rhamnifolioides-essential-oil-in-mice
#11
Cinara Soares Vidal, Anita Oliveira Brito Pereira Bezerra Martins, Andressa de Alencar Silva, Maria Rayane Correia de Oliveira, Jaime Ribeiro-Filho, Thaís Rodrigues de Albuquerque, Henrique Douglas Melo Coutinho, Jackson Roberto Guedes da Silva Almeida, Lucindo Jose Quintans, Irwin Rose Alencar de Menezes
BACKGROUND: Croton rhamnifolioides Pax is a plant species that have been used in the folk medicine to treat ulcers, inflammations and hypertension. However, despite the relevant data obtained from ethnopharmacological studies, the pharmacological properties endorsing the efficacy of this plant to treat ulcer remain to be elucidated. HYPOTHESIS/PURPOSE: The present study aimed to characterize the chemical profile and evaluate the gastroprotective activity of the essential oil obtained from C...
February 16, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28213891/opioids-and-the-immune-system-friend-or-foe
#12
REVIEW
Lisanne Mirja Plein, Heike L Rittner
Systemically administered opioids are among the most powerful analgesics for treating severe pain. Several negative side-effects (respiratory depression, addiction, nausea, confusion) and the risk of opioid-induced hyperalgesia accompany opioid administration. One other side effect is the potential of opioids to suppress the immune response and thereby to increase the vulnerability for infections. Several studies have investigated the link between opioids and immunosuppression in vitro, in vivo as well as in patients with divergent results: Exogenous opioids such as morphine and fentanyl can impair macrophage and natural killer cell as well as T cell function and weaken the gut barrier in vitro and in animal studies...
February 18, 2017: British Journal of Pharmacology
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
#13
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/28212183/cxcl12-cxcr4-signaling-contributes-to-the-pathogenesis-of-opioid-tolerance-a-translational-study
#14
Chih-Peng Lin, Kai-Hsiang Kang, Huang-Ju Tu, Ming-Yueh Wu, Tzu-Hung Lin, Houng-Chi Liou, Wei-Zen Sun, Wen-Mei Fu
BACKGROUND: Long-term opioid therapy for chronic pain may lead to analgesic tolerance, especially when administered intrathecally, thus preventing adequate pain relief. Discovering drug targets to treat opioid tolerance using a mechanism-based approach targeting opioid-induced neuroinflammation provides new therapeutic opportunities. In this study, we provide translational evidence that CXCL12/CXCR4 signaling contributes to the pathogenesis of opioid tolerance. METHODS: The CXCL12 levels in the cerebrospinal fluid of opioid-tolerant patients were compared with those of opioid-naive subjects...
March 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28211895/electroacupuncture-attenuates-cfa-induced-inflammatory-pain-by-suppressing-nav1-8-through-s100b-trpv1-opioid-and-adenosine-pathways-in-mice
#15
Hsien-Yin Liao, Ching-Liang Hsieh, Chun-Ping Huang, Yi-Wen Lin
Pain is associated with several conditions, such as inflammation, that result from altered peripheral nerve properties. Electroacupuncture (EA) is a common Chinese clinical medical technology used for pain management. Using an inflammatory pain mouse model, we investigated the effects of EA on the regulation of neurons, microglia, and related molecules. Complete Freund's adjuvant (CFA) injections produced a significant mechanical and thermal hyperalgesia that was reversed by EA or a transient receptor potential V1 (TRPV1) gene deletion...
February 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28204957/insights-into-the-role-of-opioid-receptors-in-the-gi-tract-experimental-evidence-and-therapeutic-relevance
#16
James J Galligan, Catia Sternini
Opioid drugs are prescribed extensively for pain treatment but when used chronically they induce constipation that can progress to opioid-induced bowel dysfunction. Opioid drugs interact with three classes of opioid receptors: mu opioid receptors (MORs), delta opioid receptors (DOR), and kappa opioid receptors (KORs), but opioid drugs mostly target the MORs. Upon stimulation, opioid receptors couple to inhibitory Gi/Go proteins that activate or inhibit downstream effector proteins. MOR and DOR couple to inhibition of adenylate cyclase and voltage-gated Ca(2+) channels and to activation of K(+) channels resulting in reduced neuronal activity and neurotransmitter release...
February 16, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28202437/oscillation-patterns-are-enhanced-and-firing-threshold-is-lowered-in-medullary-respiratory-neuron-discharges-by-threshold-doses-of-a-%C3%AE-opioid-receptor-agonist
#17
Peter M Lalley, Steve W Mifflin
μ-Opioid receptors are distributed widely in the brainstem respiratory network, and opioids with selectivity for μ-type receptors slow in-vivo respiratory rhythm in lowest effective doses. Several studies have reported μ-opioid receptor effects on the three-phase rhythm of respiratory neurons, but there are until now no reports of opioid effects on oscillatory activity within respiratory discharges. In this study, effects of the μ-opioid receptor agonist fentanyl on spike train discharge properties of several different types of rhythm-modulating medullary respiratory neuron discharges were analyzed...
February 15, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/28199982/n-acetyl-cysteine-attenuates-remifentanil-induced-postoperative-hyperalgesia-via-inhibiting-matrix-metalloproteinase-9-in-dorsal-root-ganglia
#18
Yue Liu, Yuan Ni, Wei Zhang, Yu-E Sun, Zhengliang Ma, Xiaoping Gu
Treatment of remifentanil-induced postoperative hyperalgesia (RIH) remains a clinical challenge because the mechanisms are not fully understood. Matrix metalloproteinase-9 (MMP-9) is a key component in neuroinflammation because of its facilitation of pro-inflammatory cytokine maturation. Therefore, inhibition of MMP-9 may represent a novel therapeutic approach to the treatment of RIH. Sprague-Dawley rats were randomly divided into three groups: Control, Incision and Remifentanil. A right plantar surgical incision was performed in Group Incision, and intraoperative remifentanil (0...
February 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28197194/cortical-regulation-of-striatal-projection-neurons-and-interneurons-in-a-parkinson-s-disease-rat-model
#19
Jia-Jia Wu, Si Chen, Li-Si Ouyang, Yu Jia, Bing-Bing Liu, Shu-Hua Mu, Yu-Xin Ma, Wei-Ping Wang, Jia-You Wei, You-Lan Li, Zhi Chen, Wan-Long Lei
Striatal neurons can be either projection neurons or interneurons, with each type exhibiting distinct susceptibility to various types of brain damage. In this study, 6-hydroxydopamine was injected into the right medial forebrain bundle to induce dopamine depletion, and/or ibotenic acid was injected into the M1 cortex to induce motor cortex lesions. Immunohistochemistry and western blot assay showed that dopaminergic depletion results in significant loss of striatal projection neurons marked by dopamine- and cyclic adenosine monophosphate-regulated phosphoprotein, molecular weight 32 kDa, calbindin, and μ-opioid receptor, while cortical lesions reversed these pathological changes...
December 2016: Neural Regeneration Research
https://www.readbyqxmd.com/read/28196272/deep-sequencing-of-71-candidate-genes-to-characterize-variation-associated-with-alcohol-dependence
#20
Shaunna L Clark, Daniel E Adkins, Gaurav Kumar, Karolina A Aberg, Sri Nerella, Linying Xie, Ann L Collins, James J Crowley, Corey R Quackenbush, Christopher E Hilliard, Andrey A Shabalin, Scott I Vrieze, Roseann E Peterson, William E Copeland, Judy L Silberg, Matt McGue, Hermine Maes, William G Iacono, Patrick F Sullivan, Elizabeth J Costello, Edwin J van den Oord
BACKGROUND: Previous genome-wide association studies (GWASs) have identified a number of putative risk loci for alcohol dependence (AD). However, only a few loci have replicated and these replicated variants only explain a small proportion of AD risk. Using an innovative approach, the goal of this study was to generate hypotheses about potentially causal variants for AD that can be explored further through functional studies. METHODS: We employed targeted capture of 71 candidate loci and flanking regions followed by next-generation deep sequencing (mean coverage 78X) in 806 European Americans...
February 14, 2017: Alcoholism, Clinical and Experimental Research
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