keyword
MENU ▼
Read by QxMD icon Read
search

Delta opioid

keyword
https://www.readbyqxmd.com/read/29860612/reinforcing-effects-of-opioid-cannabinoid-mixtures-in-rhesus-monkeys-responding-under-a-food-drug-choice-procedure
#1
David R Maguire, Charles P France
OBJECTIVE: Cannabinoid receptor agonists such as delta-9-tetrahydrocannabinol (Δ9 -THC) enhance the antinociceptive potency of mu opioid receptor agonists such as morphine, indicating that opioid/cannabinoid mixtures might be effective for treating pain. However, such enhancement will be beneficial only if cannabinoids do not also enhance adverse effects of opioids, including those related to abuse. In rhesus monkeys, cannabinoids fail to enhance and often decrease self-administration of the mu opioid receptor agonist heroin, suggesting that opioid/cannabinoid mixtures do not have greater reinforcing effects (abuse potential) compared with opioids alone...
June 3, 2018: Psychopharmacology
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
#2
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/29852083/endogenous-and-exogenous-opioids-in-pain
#3
Gregory Corder, Daniel C Castro, Michael R Bruchas, Grégory Scherrer
Opioids are the most commonly used and effective analgesic treatments for severe pain, but they have recently come under scrutiny owing to epidemic levels of abuse and overdose. These compounds act on the endogenous opioid system, which comprises four G protein-coupled receptors (mu, delta, kappa, and nociceptin) and four major peptide families (β-endorphin, enkephalins, dynorphins, and nociceptin/orphanin FQ). In this review, we first describe the functional organization and pharmacology of the endogenous opioid system...
May 31, 2018: Annual Review of Neuroscience
https://www.readbyqxmd.com/read/29795362/prolonged-dadle-exposure-epigenetically-promotes-bcl-2-expression-and-elicits-neuroprotection-in-primary-rat-cortical-neurons-via-the-pi3k-akt-nf-%C3%AE%C2%BAb-pathway
#4
Min Zhu, Ming Liu, Qi-Lin Guo, Cui-Qing Zhu, Jing-Chun Guo
Both in vivo and in vitro studies have shown the beneficial effects of the delta-opioid receptor (DOR) on neurodegeneration in hypoxia/ischemia. We previously reported that DOR stimulation with [(D-Ala2, D-Leu5) enkephalin] (DADLE), a potent DOR agonist, for both a short (minutes) and long (days) time has notable protective effects against sodium azide (NaN3 )-induced cell injury in primary cultured rat cortical neurons. We further demonstrated that short-term DADLE stimulation increased neuronal survival through the PKC-mitochondrial ERK pathway...
May 24, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29791710/postoperative-pain-and-analgesia-is-there-a-genetic-basis-to-the-opioid-crisis
#5
Randa K Elmallah, Prem N Ramkumar, Anton Khlopas, Rathika R Ramkumar, Morad Chughtai, Nipun Sodhi, Assem A Sultan, Michael A Mont
BACKGROUND: Multiple factors have been implicated in determining why certain patients have increased postoperative pain, with the potential to develop chronic pain. The purpose of this study was to: 1) identify and describe genes that affect postoperative pain perception and control; 2) address modifiable risk factors that result in epigenetic altered responses to pain; and 3) characterize differences in pain sensitivity and thresholds between opioid-naïve and opioid-dependent patients...
June 1, 2018: Surgical Technology International
https://www.readbyqxmd.com/read/29779230/role-of-mu-but-not-delta-or-kappa-opioid-receptors-in-context-induced-reinstatement-of-oxycodone-seeking
#6
Jennifer M Bossert, Jennifer K Hoots, Ida Fredriksson, Sweta Adhikary, Michelle Zhang, Marco Venniro, Yavin Shaham
Relapse to nonmedical use of prescription opioids often occurs after exposure to places previously associated with drug use. Here, we describe a rat model of context-induced reinstatement of oxycodone seeking after repeated cycles of drug self-administration and extinction-induced abstinence. We also determined the role of mu, delta, and kappa opioid receptors (MOR, DOR, KOR) in this reinstatement. We trained rats to self-administer oxycodone for 6 h/d in Context A; lever pressing was paired with a discrete cue...
May 19, 2018: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29771142/the-development-of-a-mouse-model-of-mtbi-induced-post-traumatic-migraine-and-identification-of-the-delta-opioid-receptor-as-a-novel-therapeutic-target
#7
Laura S Moye, Madeline L Novack, Alycia F Tipton, Harish Krishnan, Subhash C Pandey, Amynah Aa Pradhan
Background Post-traumatic headache is the most common and long-lasting impairment observed following mild traumatic brain injury, and frequently has migraine-like characteristics. The mechanisms underlying progression from mild traumatic brain injury to post-traumatic headache are not fully understood. The aim of this study was to develop a mouse model of post-traumatic headache and identify mechanisms and novel targets associated with this disorder. Methods We combined the closed head weight-drop method and the nitroglycerin chronic migraine model...
January 1, 2018: Cephalalgia: An International Journal of Headache
https://www.readbyqxmd.com/read/29768254/neuroprotection-against-hypoxic-ischemic-injury-%C3%AE-opioid-receptors-and-bdnf-trkb-pathway
#8
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/29754032/opioid-related-mortality-in-rural-america-geographic-heterogeneity-and-intervention-strategies
#9
Khary K Rigg, Shannon M Monnat, Melody N Chavez
Over the last two decades, opioid-related mortality rates have increased dramatically to become a serious public health concern in the United States. Opioid-related mortality has reached epidemic levels in certain rural areas of the U.S., such as Appalachia, New England, and the Mountain West, while remaining relatively low in others, such as the Delta South and Great Plains. Explanations for geographic variation in opioid mortality are unclear, contributing to ineffective policies and interventions. The goal of this article is to summarize the existing literature on the opioid epidemic in the rural U...
May 10, 2018: International Journal on Drug Policy
https://www.readbyqxmd.com/read/29734749/synthesis-and-structure-activity-relationships-of-cis-n-normetazocine-based-lp1-derivatives
#10
Lorella Pasquinucci, Carmela Parenti, Emanuele Amata, Zafiroula Georgoussi, Paschalina Pallaki, Valeria Camarda, Girolamo Calò, Emanuela Arena, Lucia Montenegro, Rita Turnaturi
(−)- cis - N -Normetazocine represents a rigid scaffold able to mimic the tyramine moiety of endogenous opioid peptides, and the introduction of different N -substituents influences affinity and efficacy of respective ligands at MOR (mu opioid receptor), DOR (delta opioid receptor), and KOR (kappa opioid receptor). We have previously identified LP1, a MOR/DOR multitarget opioid ligand, with an N -phenylpropanamido substituent linked to (−)- cis - N -Normetazocine scaffold. Herein, we report the synthesis, competition binding and calcium mobilization assays of new compounds 10 ⁻ 16 that differ from LP1 by the nature of the N -substituent...
May 5, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29729777/methadone-maximizing-safety-and-efficacy-for-pain-control-in-patients-with-cancer
#11
REVIEW
Mary Lynn McPherson, Ryan C Costantino, Alexandra L McPherson
Methadone is a valuable opioid in the management of patients who have cancer with pain. Methadone is a mu-, kappa-, and delta-opioid agonist, and an N-methyl-D-aspartate receptor antagonist. These mechanisms of action make methadone an attractive option for complex pain syndromes. It is critically important that providers consider a patient's risk status before beginning methadone. Careful consideration must be given to dosing methadone in both opioid-naïve and opioid-tolerant patients, with vigilant monitoring for therapeutic effectiveness and potential toxicity until the patient achieves steady state...
June 2018: Hematology/oncology Clinics of North America
https://www.readbyqxmd.com/read/29727730/dor-agonist-snc-80-exhibits-anti-parkinsonian-effect-via-downregulating-upr-oxidative-stress-signals-and-inflammatory-response-in-vivo
#12
Erfath Thanjeem Begum M, Dwaipayan Sen
The pathophysiology of Parkinson's disease exhibit imperative roles in unfolded protein response stress-induced oxidative stress and inflammation in general. Although, delta opioid receptor (DOR), has been found to represent anti-parkinsonian effect at behavioral level, its underlying mechanism remains elusive till date. In the present study the role of DOR agonist, SNC-80 and the consorted molecular mechanisms, which translates to behavioral recuperation, has been delineated. In order to mimic PD, mice were intra-peritoneally injected with MPTP, following exposure to SNC-80 and L-DOPA to elucidate amelioration of the MPTP-induced behavioral impairments...
May 1, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29722902/tolerance-to-high-internalizing-delta-opioid-receptor-agonist-is-critically-mediated-by-arrestin-2
#13
Ana Vicente-Sanchez, Isaac J Dripps, Alycia F Tipton, Heba Akbari, Areeb Akbari, Emily M Jutkiewicz, Amynah A Pradhan
BACKGROUND AND PURPOSE: Delta opioid receptor (δOR) agonists are potent antihyperalgesics in chronic pain models, but tolerance develops after prolonged use. Previous evidence indicates that distinct forms of tolerance occur depending on the internalization properties of δOR agonists. Due to the importance of arrestins in receptor internalization, we investigated the role of arrestin 2 (β-arrestin 1) in mediating the development of tolerance induced by high- and low-internalizing δOR agonists...
May 3, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29713172/gender-specific-association-of-functional-prodynorphin-68-bp-repeats-with-cannabis-exposure-in-an-african-american-cohort
#14
Vadim Yuferov, Eduardo R Butelman, Mary Jeanne Kreek
Background: Cannabis use disorders (CUDs) cause substantial neuropsychiatric morbidity and comorbidity. There is evidence for gender-based differences in CUDs, for instance, a greater prevalence in males than in females. The main active component of cannabis is delta 9-tetrahydrocannabinol (delta 9-THC), a partial agonist of the cannabinoid type 1 receptor. Preclinical studies show that genetic or pharmacological manipulation of the kappa opioid receptor/dynorphin system modulates the effects of delta 9-THC...
2018: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/29686629/critical-role-for-g-i-o-protein-activity-in-the-dorsal-striatum-in-the-reduction-of-voluntary-alcohol-intake-in-c57bl-6-mice
#15
Meridith T Robins, Terrance Chiang, Kendall L Mores, Doungkamol Alongkronrusmee, Richard M van Rijn
The transition from non-dependent alcohol use to alcohol dependence involves increased activity of the dorsal striatum. Interestingly, the dorsal striatum expresses a large number of inhibitory G-protein-coupled receptors (GPCRs), which when activated may inhibit alcohol-induced increased activity and can decrease alcohol consumption. Here, we explore the hypothesis that dorsal striatal Gi/o -protein activation is sufficient to reduce voluntary alcohol intake. Using a voluntary, limited-access, two-bottle choice, drink-in-the-dark model of alcohol (10%) consumption, we validated the importance of Gi/o signaling in this region by locally expressing neuron-specific, adeno-associated-virus encoded Gi/o -coupled muscarinic M4 designer receptors exclusively activated by designer drugs (DREADD) in the dorsal striatum and observed a decrease in alcohol intake upon DREADD activation...
2018: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29684591/in-vitro-and-in-vivo-activity-of-cyclopeptide-dmt-c-d-lys-phe-asp-nh-2-a-mu-opioid-receptor-agonist-biased-toward-%C3%AE-arrestin
#16
Katarzyna Gach-Janczak, Justyna Piekielna-Ciesielska, Anna Adamska-Bartłomiejczyk, Karol Wtorek, Federica Ferrari, Girolamo Calo', Agata Szymaszkiewicz, Joanna Piasecka-Zelga, Anna Janecka
Morphine and related drugs, which are the most effective analgesics for the relief of severe pain, act through activating opioid receptors. The endogenous ligands of these receptors are opioid peptides which cannot be used as antinociceptive agents due to their low bioactivity and stability in biological fluids. The major goal of opioid research is to understand the mechanism of action of opioid receptor agonists in order to improve therapeutic utility of opioids. Analgesic effects of morphine are mediated mostly through activation of the mu opioid receptor...
July 2018: Peptides
https://www.readbyqxmd.com/read/29681795/delta-opioid-receptor-signaling-promotes-resilience-to-stress-under-the-repeated-social-defeat-paradigm-in-mice
#17
Mathilde S Henry, Kanchan Bisht, Nathalie Vernoux, Louis Gendron, Angélica Torres-Berrio, Guy Drolet, Marie-Ève Tremblay
The adaptation to chronic stress is highly variable across individuals. Resilience to stress is a complex process recruiting various brain regions and neurotransmitter systems. The aim of this study was to investigate the involvement of endogenous opioid enkephalin (ENK) signaling in the development of stress resilience in mice. The translational model of repeated social defeat (RSD) stress was selected to mimic the unpredictable disruptions of daily life and induce resilience or vulnerability to stress. As in humans, adult C57BL/6J mice demonstrated a great variability in their response to stress under this paradigm...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29677442/synthesis-and-pharmacological-evaluation-of-novel-c-8-substituted-tetrahydroquinolines-as-balanced-affinity-mu-delta-opioid-ligands-for-the-treatment-of-pain
#18
Anthony F Nastase, Nicholas W Griggs, Jessica P Anand, Thomas J Fernandez, Aubrie A Harland, Tyler J Trask, Emily M Jutkiewicz, John R Traynor, Henry I Mosberg
The use of opioids for the treatment of pain, while largely effective, is limited by detrimental side effects including analgesic tolerance, physical dependence, and euphoria, which may lead to opioid abuse. Studies have shown that compounds with a μ-opioid receptor (MOR) agonist/δ-opioid receptor (DOR) antagonist profile reduce or eliminate some of these side effects including the development of tolerance and dependence. Herein we report the synthesis and pharmacological evaluation of a series of tetrahydroquinoline-based peptidomimetics with substitutions at the C-8 position...
May 2, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29664203/trends-and-patterns-of-opioid-analgesic-prescribing-regional-and-rural-urban-variations-in-kentucky-from-2012-to-2015
#19
Huong Luu, Svetla Slavova, Patricia R Freeman, Michelle Lofwall, Steven Browning, Heather Bush
PURPOSE: Increased opioid analgesic prescribing (OAP) has been associated with increased risk of prescription opioid diversion, misuse, and abuse. We studied regional and rural-urban variations in OAP trends in Kentucky, from 2012 to 2015, and examined potential county-level risk and protective factors. METHODS: This study used prescription drug monitoring data. Marginal models employing generalized estimating equations were used to model repeated counts of residents with opioid analgesic prescriptions within county-quarter, 2012-2015, with offset for resident population, by rural-urban classification exposure, and adjusting for time-varying socioeconomic and relevant health status measures...
April 17, 2018: Journal of Rural Health
https://www.readbyqxmd.com/read/29659874/carfentanil-in-impaired-driving-cases-and-the-importance-of-drug-seizure-data
#20
Nicholas B Tiscione, Ilene Alford
Drug seizures containing carfentanil continue to increase in Palm Beach County, FL, USA despite international efforts to control the distribution of the drug. The analysis of drug seizures from the county in 2016 and 2017 demonstrated that carfentanil was the most commonly identified fentanyl analog and was most often detected in combination with heroin, fentanyl, furanyl fentanyl and/or other fentanyl analogs. Carfentanil is an ultra-potent opioid requiring a method with adequate sensitivity for detection in blood specimens from impairment cases...
April 12, 2018: Journal of Analytical Toxicology
keyword
keyword
26194
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"