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https://www.readbyqxmd.com/read/29930811/evaluation-of-morphine-like-effects-of-the-mixed-mu-delta-agonist-morphine-6-o-sulfate-in-rats-drug-discrimination-and-physical-dependence
#1
Jai Shankar K Yadlapalli, Shoban Babu Bommagani, Ryan D Mahelona, Anqi Wan, Brenda M Gannon, Narsimha R Penthala, Maxim Dobretsov, Peter A Crooks, William E Fantegrossi
Morphine-6-O-sulfate (M6S) is as a mixed-action mu/delta (μ/δ) opioid receptor agonist with high potency and analgesic efficacy. These studies used assays of drug discrimination and schedule-controlled responding to assess abuse-liability, tolerance, and physical dependence as compared to morphine in rats. Attempts to train 0.3 mg/kg (IP) M6S from saline failed, but all rats rapidly acquired the discrimination when the training dose was changed to 3.0 mg/kg morphine, and substitution tests showed that morphine and fentanyl both fully substituted for the training dose, M6S and M3A6S (3-O-acetyl ester of M6S) only partially substituted, and salvinorin A did not elicit morphine-like effects...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29907903/the-chemokine-ccl4-mip-1%C3%AE-evokes-antinociceptive-effects-in-mice-a-role-for-cd4-lymphocytes-and-met-enkephalin
#2
Mario García-Domínguez, Ana Lastra, Alicia R Folgueras, Rafael Cernuda-Cernuda, María Teresa Fernández-García, Agustín Hidalgo, Luis Menéndez, Ana Baamonde
In the present study, we characterize the antinociceptive effects produced by the chemokine CCL4 in mice. The intraplantar administration of very low doses of CCL4 (0.1-3 pg) produced bilateral antinociception assessed by the unilateral hot-plate test (UHP) without evoking chemotactic responses at the injection site. Moreover, the subcutaneous administration of CCL4 (3-100 pg/kg) also yielded bilateral antinociception in the UHP and the paw pressure test and reduced the number of spinal neurons that express Fos protein in response to noxious stimulation...
June 15, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29902466/amniotic-fluid-ingestion-enhances-central-%C3%AE-opioid-induced-hypoalgesia-in-rats-in-the-cold-water-tail-flick-assay-in-a-repeated-measures-design
#3
Alexis C Thompson, Casey Feeney, Mark B Kristal
Placental Opioid Enhancing Factor (POEF) is found in amniotic fluid (AF) and placenta. When ingested, it enhances opioid-mediated pain relief. Our laboratory has shown that ingestion of AF specifically enhances the hypoalgesia associated with δ-opioid receptor activation in the brain. The specific biochemical compound in AF responsible for the enhancement of δ-opioid activity is of great interest as an analgesic adjunct for pain but is unknown at this time. Research efforts to isolate and characterize this biochemical compound are hampered by the lack of an algesiometric assay that allows repeated measurement of pain threshold and repeated exposure to δ-opioid receptor activation...
June 11, 2018: Brain Research
https://www.readbyqxmd.com/read/29883706/induction-of-oxidative-stress-by-long-term-treatment-of-live-hek293-cells-with-therapeutic-concentration-of-lithium-is-associated-with-down-regulation-of-%C3%AE-opioid-receptor-amount-and-function
#4
Miroslava Vosahlikova, Hana Ujcikova, Stanislav Musil, Lenka Roubalova, Martin Alda, Petr Svoboda
The functional state of δ-opioid receptor signalling cascade in live cells exposed to a therapeutic concentration of lithium for a prolonged period of time (weeks) is not known because the previous studies of Li interference with OR were oriented to µ-OR only. The same applies to the analysis of the prolonged effect of Li on oxidative stress in context with δ-OR function. HEK293 cells stably expressing δ-OR were cultivated in the presence or absence of 1 mM LiCl for 7 or 21 days, homogenized and the post-nuclear (PNS) and plasma membrane (PM) fractions prepared from all four types of cells...
June 5, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29858157/cyclic-biphalin-analogues-with-a-novel-linker-lead-to-potent-agonist-activities-at-mu-delta-and-kappa-opioid-receptors
#5
Michael Remesic, Giorgia Macedonio, Adriano Mollica, Frank Porreca, Victor Hruby, Yeon Sun Lee
In an effort to improve biphalin's potency and efficacy at the µ-(MOR) and δ-opioid receptors (DOR), a series of cyclic biphalin analogues 1-5 with a cystamine or piperazine linker at the C-terminus were designed and synthesized by solution phase synthesis using Boc-chemistry. Interestingly, all of the analogues showed balanced opioid agonist activities at all opioid receptor subtypes due to enhanced κ-opioid receptor (KOR) activity. Our results indicate that C-terminal flexible linkers play an important role in KOR activity compared to that of the other cyclic biphalin analogues with a hydrazine linker...
May 26, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29768254/neuroprotection-against-hypoxic-ischemic-injury-%C3%AE-opioid-receptors-and-bdnf-trkb-pathway
#6
Shiying Sheng, Jingzhong Huang, Yi Ren, Feng Zhi, Xuansong Tian, Guoqiang Wen, Guanghong Ding, Terry C Xia, Fei Hua, Ying Xia
The delta-opioid receptor (DOR) is one of three classic opioid receptors in the opioid system. It was traditionally thought to be primarily involved in modulating the transmission of messages along pain signaling pathway. Although there were scattered studies on its other neural functions, inconsistent results and contradicting conclusions were found in past literatures, especially in terms of DOR's role in a hypoxic/ischemic brain. Taking inspiration from the finding that the turtle brain exhibits a higher DOR density and greater tolerance to hypoxic/ischemic insult than the mammalian brain, we clarified DOR's specific role in the brain against hypoxic/ischemic injury and reconciled previous controversies in this aspect...
May 11, 2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29737176/synthesis-and-structural-elucidation-of-a-pyranomorphinan-opioid-and-in-vitro-studies
#7
Mohd Imran Ansari, Jason R Healy, Kellie Hom, Jeffrey R Deschamps, Rae R Matsumoto, Andrew Coop
During optimization of the synthesis of the mixed μ opioid agonist/δ opioid antagonist 5-(hydroxymethyl)oxymorphone (UMB425) for scale-up, it was unexpectedly discovered that the 4,5-epoxy bridge underwent rearrangement on treatment with boron tribromide (BBr3 ) to yield a novel opioid with a little-studied pyranomorphinan skeleton. This finding opens the pyranomorphinans for further investigations of their pharmacological profiles and represents a novel drug class with the dual profile (μ vs δ) predicted to yield lower tolerance and dependence...
May 8, 2018: Organic Letters
https://www.readbyqxmd.com/read/29728020/-molecular-mechanism-of-bupleuri-radix-and-scutellariae-radix-drug-pair-for-depression-based-on-integrative-pharmacology-platform-of-traditional-chinese-medicine
#8
Jian-Ting Wang, Shang Wang, Song-Lin Liu, Yan-Chun Wang, Jia-Geng Li, Yu Chen
Xiaochaihu decoction is a classic prescription of traditional Chinese medicine. Modern research has proved its anti-depression effect. However, its pharmacological mechanism for anti-depression effect is difficult to be unveiled because of the complexity of compound Chinese medicines. Bupleuri Radix and Scutellariae Radix is the core drug pair of Xiaochaihu decoction. In this research, Bupleuri Radix and Scutellariae Radix were analyzed by the integrative pharmacology platform to study its molecular mechanism for anti-depression...
April 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29687347/%C3%AE-opioid-receptor-activation-attenuates-hypoxia-mpp-induced-downregulation-of-pink1-a-novel-mechanism-of-neuroprotection-against-parkinsonian-injury
#9
Yuan Xu, Feng Zhi, Ya Peng, Naiyuan Shao, Dhiaedin Khiati, Gianfranco Balboni, Yilin Yang, Ying Xia
There is emerging evidence suggesting that neurotoxic insults and hypoxic/ischemic injury are underlying causes of Parkinson's disease (PD). Since PTEN-induced kinase 1 (PINK1) dysfunction is involved in the molecular genesis of PD and since our recent studies have demonstrated that the δ-opioid receptor (DOR) induced neuroprotection against hypoxic and 1-methyl-4-phenyl-pyridimium (MPP+ ) insults, we sought to explore whether DOR protects neuronal cells from hypoxic and/or MPP+ injury via the regulation of PINK1-related pathways...
April 24, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29623611/m-trifluoromethyl-diphenyl-diselenide-regulates-prefrontal-cortical-mor-and-kor-protein-levels-and-abolishes-the-phenotype-induced-by-repeated-forced-swim-stress-in-mice
#10
Suzan Gonçalves Rosa, Ana Paula Pesarico, Franciele Martini, Cristina Wayne Nogueira
The present study aimed to investigate the m-trifluoromethyl-diphenyl diselenide [(m-CF3 -PhSe)2 ] effects on prefrontal cortical MOR and KOR protein levels and phenotype induced by repeated forced swim stress (FSS) in mice. Adult Swiss mice were subjected to repeated FSS sessions, and after that, they performed the spontaneous locomotor/exploratory activity, tail suspension, and splash tests. (m-CF3 -PhSe)2 (0.1 to 5 mg/kg) was administered to mice 30 min before the first FSS session and 30 min before the subsequent repeated FSS...
April 5, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29587571/clinical-opioids-differentially-induce-co-internalization-of-%C3%AE-and-%C3%AE-opioid-receptors
#11
Fenghua Bao, Chang-Lin Li, Xu-Qiao Chen, Ying-Jin Lu, Lan Bao, Xu Zhang
Opioid receptors play an important role in mediating the spinal analgesia. The μ-opioid receptor is the major target of opioid drugs widely used in clinics. However, the regulatory mechanisms of analgesic effect and tolerance for clinical μ-opioid receptor-targeting opioids remain to be fully investigated. Previous studies showed the interaction of δ-opioid receptor with μ-opioid receptor to form the μ-opioid receptor/δ-opioid receptor heteromers that could be processed in the degradation pathway after δ-opioid receptor agonist treatment...
January 2018: Molecular Pain
https://www.readbyqxmd.com/read/29583107/morphine-reduces-mouse-microglial-engulfment-induced-by-lipopolysaccharide-and-interferon-%C3%AE-via-%C3%AE-opioid-receptor-and-p38-mitogen-activated-protein-kinase
#12
Jung-Hee Ryu, Sang-Hwan Do, Sung-Hee Han, Zhiyi Zuo
Objective To investigate the effects of morphine on microglial phagocytosis during neuroinflammation. Methods C8-B4 mouse microglial cells were exposed to various concentrations of morphine after the stimulation with lipopolysaccharide and interferon-γ and then fluorescent immunostaining was performed to assess the percentage of microglia that engulfed fluorescent microspheres in total microglia. Naloxone, β funaltrexamine, or naltrindole was used with 1 μM morphine to assess the involvement of specific opioid receptor...
March 27, 2018: Neurological Research
https://www.readbyqxmd.com/read/29575372/radar-plots-a-novel-modality-for-displaying-disparate-data-on-the-efficacy-of-eluxadoline-for-the-treatment-of-irritable-bowel-syndrome-with-diarrhea
#13
D M Brenner, L S Dove, D A Andrae, P S Covington, C Gutman, W D Chey
BACKGROUND: Patients with irritable bowel syndrome with diarrhea (IBS-D) experience a range of abdominal and bowel symptoms; successful management requires alleviation of this constellation of symptoms. Eluxadoline, a locally active mixed μ- and κ-opioid receptor agonist and δ-opioid receptor antagonist, is approved for the treatment of IBS-D in adults based on the results of 2 Phase 3 studies. Radar plots can facilitate comprehensive, visual evaluation of diverse but interrelated efficacy endpoints...
March 25, 2018: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/29563057/opioid-receptor-and-%C3%AE-arrestin2-densities-and-distribution-change-after-sexual-experience-in-the-ventral-tegmental-area-of-male-rats
#14
René Garduño-Gutiérrez, Martha León-Olea, Gabriela Rodríguez-Manzo
Sexual experience modifies brain functioning and copulatory efficiency. Sexual activity, ejaculation in particular, is a rewarding behavior associated with the release of endogenous opioids, which modulate the activity of the mesolimbic dopaminergic system (MLS). In sexually exhausted rats, repeated ejaculation produces μ (MOR) and δ opioid receptor (DOR) internalization in ventral tegmental area (VTA) neurons, as well as long-lasting behavioral changes suggestive of brain plasticity processes. We hypothesized that in sexually naïve rats the endogenous opioids released during sexual experience acquisition, might contribute to brain plasticity processes involved in the generation of the behavioral changes induced by sexual experience...
May 15, 2018: Physiology & Behavior
https://www.readbyqxmd.com/read/29560360/the-potentially-beneficial-central-nervous-system-activity-profile-of-ivacaftor-and-its-metabolites
#15
Elena K Schneider, Rachel M McQuade, Vincenzo C Carbone, Felisa Reyes-Ortega, John W Wilson, Brenda Button, Ayame Saito, Daniel P Poole, Daniel Hoyer, Jian Li, Tony Velkov
Ivacaftor-lumacaftor and ivacaftor are two new breakthrough cystic fibrosis transmembrane conductance modulators. The interactions of ivacaftor and its two metabolites hydroxymethylivacaftor (iva-M1) and ivacaftorcarboxylate (iva-M6) with neurotransmitter receptors were investigated in radioligand binding assays. Ivacaftor displayed significant affinity to the 5-hydroxytryptamine (5-HT; serotonin) 5-HT2C receptor (p K i =6.06±0.03), β3 -adrenergic receptor (p K i =5.71±0.07), δ-opioid receptor (p K i =5...
January 2018: ERJ Open Research
https://www.readbyqxmd.com/read/29501769/the-efficacy-of-a-lectin-from-abelmoschus-esculentus-depends-on-central-opioid-receptor-activation-to-reduce-temporomandibular-joint-hypernociception-in-rats
#16
Shirley Moreira Alves, Raul Sousa Freitas, Danielle Rocha do Val, Lorena Vasconcelos Vieira, Ellen Lima de Assis, Francisco Isaac Fernandes Gomes, Carlos Alberto de Almeida Gadelha, Tatiane Santi Gadelha, José Thalles Jocelino Gomes de Lacerda, Juliana Trindade Clemente-Napimoga, Vicente de Paulo Teixeira Pinto, Gerardo Cristino Filho, Mirna Marques Bezerra, Hellíada Vasconcelos Chaves
Abelmoschus esculentus is largely cultivated in Northeastern Brazil for medicinal purposes, e.g. inflammatory conditions. This study aimed to evaluate the efficacy of Abelmoschus esculentus lectin (AEL) in reducing formalin-induced temporomandibular joint inflammatory hypernociception in rats. The behavioral experiments were performed in male Wistar rats (180-240 g). Rats were pre-treated (i.v.) with AEL (0.001, 0.01 or 0.1 mg/kg) 30 min before formalin injection (i.art.). To analyze the possible effect of opioid pathways on AEL efficacy, animals were pre-treated with naloxone or CTOP (μ opioid receptor antagonist), naltrindole (δ opioid receptor antagonist) or nor-binaltorphimine (κ opioid receptor antagonist) (i...
May 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29496478/non-pharmacological-treatment-affects-neuropeptide-expression-in-neuropathic-pain-model
#17
Fabio Martinez Santos, Joyce Teixeira Silva, Igor Rafael Correia Rocha, Daniel Oliveira Martins, Marucia Chacur
Chronic constriction injury (CCI) of the sciatic nerve elicits changes in neuropeptide expression on the dorsal root ganglia (DRG). The neural mobilization (NM) technique is a noninvasive method that has been proven clinically effective in reducing pain. The aim of this study was to analyze the expression of substance P, transient receptor potential vanilloid 1 (TRPV1) and opioid receptors in the DRG of rats with chronic constriction injury and to compare it to animals that received NM treatment. CCI was performed on adult male rats...
May 15, 2018: Brain Research
https://www.readbyqxmd.com/read/29441714/time-dependent-regional-brain-distribution-of-methadone-and-naltrexone-in-the-treatment-of-opioid-addiction
#18
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/29434817/%C3%AE-opioid-receptor-inhibition-prevents-remifentanil-induced-post-operative-hyperalgesia-via-regulating-glur1-trafficking-and-ampa-receptor-function
#19
Aifen Liu, Xiaopeng Wang, Hui Wang, Guoyi Lv, Yize Li, Hongmei Li
The interaction of remifentanil with glutamate systems has an important role in remifentanil-induced thermal and mechanical hyperalgesia. A previous study by our group suggested that the trafficking and function of glutamate receptor 1 (GluR1) subunits contributes to remifentanil-induced hyperalgesia by regulating the phosphorylation of GluR1 in dorsal horn neurons. The present study demonstrated that δ opioid receptor (DOR) inhibition prevented thermal and mechanical hyperalgesia, which was induced by remifentanil infusion via attenuating GluR1 subunit trafficking and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) function in dorsal horn neurons...
February 2018: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29432603/in-vitro-screening-for-seizure-liability-using-microelectrode-array-technology
#20
Jenifer A Bradley, Harry H Luithardt, Monica R Metea, Christopher J Strock
Drug-induced seizure liabilities produce significant compound attrition during drug discovery. Currently available in vitro cytotoxicity assays cannot predict all toxicity mechanisms due to the failure of these assays to predict sublethal target-specific electrophysiological liabilities. Identification of seizurogenic and other electrophysiological effects at early stages of the drug development process is important to ensure that safe candidate compounds can be developed while chemical design is taking place, long before these liabilities are discovered in costly preclinical in vivo studies...
May 1, 2018: Toxicological Sciences: An Official Journal of the Society of Toxicology
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