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https://www.readbyqxmd.com/read/29451852/delta-opioids-neuroprotective-roles-in-preclinical-studies
#1
Shahid Husain
Since ancient times, opioids have been used clinically and abused recreationally. In the early stages (about 1,000 AD) of opium history, an Arab physician, Avicenna, administered opioids to control diarrhea and eye diseases. 1 Opioids have very strong pain relieving properties and they also regulate numerous cellular responses. Opioid receptors are expressed throughout the body, including the nervous system, heart, lungs, liver, gastrointestinal tract, and retina. 2-6 Delta opioid receptors (DORs) are a very attractive target from the perspective of both receptor function and their therapeutic potential...
January 2018: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29441714/time-dependent-regional-brain-distribution-of-methadone-and-naltrexone-in-the-treatment-of-opioid-addiction
#2
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
#3
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/29421449/potential-uses-of-isolated-toxin-peptides-in-neuropathic-pain-relief-a-literature-review
#4
REVIEW
M K Hamad, K He, H F Abdulrazeq, A M Mustafa, J Nakhla, M M Herzallah, A Mammis
Neuropathic pain is a subset of chronic pain that is caused by neurons that are damaged or firing aberrantly in the peripheral or central nervous systems. The treatment guidelines for neuropathic pain include antidepressants, calcium channel α 2 delta ligands, topical therapy, and opioids as a second line option. Unfortunately, pharmacotherapy has not been effective in the treatment of neuropathic pain except in the treatment of trigeminal neuralgia with carbamazepine. The inability to properly treat neuropathic pain causes frustration in both the patients and their treating physicians...
February 5, 2018: World Neurosurgery
https://www.readbyqxmd.com/read/29396147/focusing-on-the-opioid-system-for-addiction-biomarker-discovery
#5
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
#6
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/29355609/is-nociception-mechanism-altered-in-offspring-of-morphine-abstinent-rats
#7
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/29352503/in-vivo-effects-of-%C3%AE-opioid-receptor-agonist-%C3%AE-opioid-receptor-antagonist-peptidomimetics-following-acute-and-repeated-administration
#8
Jessica P Anand, Kelsey E Kochan, Anthony F Nastase, Deanna Montgomery, Nicholas W Griggs, John R Traynor, Henry I Mosberg, Emily M Jutkiewicz
BACKGROUND AND PURPOSE: Mu opioid receptor (μ-receptor) agonists are used for pain management, but produce adverse effects including tolerance, dependence, and euphoria. The co-administration of a μ-receptor agonist with a delta opioid receptor (δ-receptor) antagonist has been shown to produce antinociception with reduced development of some side effects. We characterized the effects of three μ-receptor agonist/δ-receptor antagonist peptidomimetics in vivo after acute and repeated administration to determine if this profile provides a viable alternative to traditional opioid analgesics...
January 19, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29304922/the-appropriate-use-of-opioids-in-the-treatment-of-refractory-restless-legs-syndrome
#9
Michael H Silber, Philip M Becker, Mark J Buchfuhrer, Christopher J Earley, William G Ondo, Arthur S Walters, John W Winkelman
Restless legs syndrome (RLS) is a distinct disorder, differing from chronic pain in many ways. Refractory RLS is characterized by unresponsiveness to dopamine agonists or alpha-2-delta ligands due to inadequate efficacy, augmentation, or adverse effects. This may result in severely impaired quality of life, profound insomnia, and suicidal depression. Opioid therapy is a mainstay in the management of these patients. This article summarizes the basic science and clinical evidence in support of their use, including the positive result of a large controlled multicenter study of 306 subjects, and outlines an approach to their use in clinical practice...
January 2018: Mayo Clinic Proceedings
https://www.readbyqxmd.com/read/29301275/generation-and-characterization-of-antibodies-against-opioid-receptors-from-zebrafish
#10
Juan C Arévalo, Enrique Hernández-Jiménez, Ada Jiménez-González, María Torres-Valle, Roman S Iwasaki, Roger López-Bellido, Cristina Vicente-García, Raquel E Rodríguez
The opioid system is well conserved among species and plays a critical role in pain and addiction systems. The use of zebrafish as an experimental model to study development and genetics is extraordinary and has been proven to be relevant for the study of different diseases. The main drawback to its use for the analysis of different pathologies is the lack of protein tools. Antibodies that work in other models are not suitable for zebrafish due to the low degree of homology that exists among the opioid receptor protein sequences in different species...
January 2, 2018: International Journal of Molecular Sciences
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/29288293/delta-opioid-receptors-recycle-to-the-membrane-after-sorting-to-the-degradation-path
#12
Iness Charfi, Khaled Abdallah, Louis Gendron, Graciela Pineyro
Soon after internalization delta opioid receptors (DOPrs) are committed to the degradation path by G protein-coupled receptor (GPCR)-associated binding protein. Here we provide evidence that this classical post-endocytic itinerary may be rectified by downstream sorting decisions which allow DOPrs to regain to the membrane after having reached late endosomes (LE). The LE sorting mechanism involved ESCRT accessory protein Alix and the TIP47/Rab9 retrieval complex which supported translocation of the receptor to the TGN, from where it subsequently regained the cell membrane...
December 29, 2017: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/29283978/review-hibernation-based-approaches-in-the-treatment-of-hemorrhagic-shock
#13
Andrea Wolf, Elizabeth R Lusczek, Gregory J Beilman
Hemorrhagic shock is the leading cause of preventable death after trauma. Hibernation-based treatment approaches have been of increasing interest for various biomedical applications. Due to apparent similarities in tissue perfusion and metabolic activity between severe blood loss and the hibernating state, hibernation-based approaches have also emerged for the treatment of hemorrhagic shock. Research has shown that hibernators are protected from shock-induced injury and inflammation. Utilizing the adaptive mechanisms that prevent injury in these animals may help alleviate the detrimental effects of hemorrhagic shock in non-hibernating species...
December 27, 2017: Shock
https://www.readbyqxmd.com/read/29278419/role-of-signaling-molecules-in-behaviors-mediated-by-the-%C3%AE-receptor-agonist-snc80
#14
Isaac J Dripps, Brett T Boyer, Richard R Neubig, Kenner C Rice, John R Traynor, Emily M Jutkiewicz
BACKGROUND AND PURPOSE: G protein-coupled receptors exist in multiple conformations that can engage distinct signaling mechanisms which in turn may lead to diverse behavioral outputs. In rodent models, activation of the delta opioid receptor (δ-receptor) has been shown to elicit antihyperalgesia, antidepressant-like effects, and convulsions. We recently showed that these δ-receptor-mediated behaviors are differentially regulated by the GTPase-activating protein regulator of G protein signaling 4 (RGS4), which facilitates termination of G protein signaling...
December 26, 2017: British Journal of Pharmacology
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/29222847/synthesis-of-novel-norsufentanil-analogues-via-a-four-component-ugi-reaction-and-in-vivo-docking-and-qsar-studies-of-their-analgesic-activity
#16
Majid Nami, Peyman Salehi, Minoo Dabiri, Morteza Bararjanian, Sajjad Gharaghani, Mona Khoramjouy, Ahmed Al-Harrasi, Mehrdad Faizi
Novel substituted amino acid tethered norsufentanil derivatives were synthesized by the four-component Ugi reaction. Norsufentanil was reacted with succinic anhydride to produce the corresponding carboxylic acid. The resulting carboxylic acid has undergone a multicomponent reaction with different aldehydes, amines, and isocyanides to produce a library of the desired compounds. In all cases, amide bond rotation was observed in the NMR spectra. In vivo analgesic activity of the synthesized compounds was evaluated by a tail flick test...
December 8, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29214743/gc-ms-ms-detects-potential-pregabalin-abuse-in-susceptible-subjects-hair
#17
Federica Ianni, Kyriaki Aroni, Alessio Gili, Roccaldo Sardella, Mauro Bacci, Massimo Lancia, Benedetto Natalini, Cristiana Gambelunghe
Pregabalin, a GABA analogue, binds to the alpha 2 delta subunit of voltage-dependent calcium channels. It is recognized as efficacious in pathologies such as epilepsy, neuropathic pain and anxiety disorders. Since pregabalin prescriptions have increased worldwide, reports of its abuse have been accumulating, mainly in patients with opioid abuse disorders. The present study investigated potential pregabalin abuse by means of hair analysis, a matrix that provides valuable retrospective information. Half of the pool of 280 susceptible patients had been occasional drug users and were being monitored for driving licence renewals...
December 7, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29197517/dpi-289-a-novel-mixed-delta-opioid-agonist-mu-opioid-antagonist-dama-has-l-dopa-sparing-potential-in-parkinson-s-disease
#18
Tom H Johnston, Eboo Versi, Patrick A Howson, Paula Ravenscroft, Susan H Fox, Michael P Hill, Bruce E Reidenberg, Ronald Corey, Jonathan M Brotchie
L-DOPA-induced dyskinesia (LID) remains a significant problem in the management of Parkinson's disease (PD). In rodent and macaque models of PD, delta opioid receptor agonists have anti-parkinsonian actions while mu opioid antagonists can reduce the expression of LID. DPI-289 is a novel molecule with a unique combination of opioid receptor DAMA actions: delta agonist (Ki: 0.73 nM); mu antagonist (Ki: 12 nM). We demonstrated that DPI-289 has oral bioavailability and established its pharmacokinetic profile in both rat and primate...
November 29, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29163008/antioxidative-and-antiapoptotic-effects-of-delta-opioid-peptide-d-ala-2-d-leu-5-enkephalin-on-spinal-cord-ischemia-reperfusion-injury-in-rabbits
#19
Danyun Fu, Haitong Liu, Shitong Li, Lianhua Chen, Junyan Yao
Background: In our previous study, we found that regional administration of delta-opioid peptide [D-Ala(2), D-Leu(5)] enkephalin (DADLE) could provide dose-dependent protection on spinal cord ischemia-reperfusion (I/R) injury in rabbits. However, the relative protective molecular mechanisms underlying this neuroprotection remain unclear. The purpose of this study was to investigate whether DADLE provided the protection in spinal cord I/R injury through its antioxidant property by decreasing malondialdehyde (MDA) and nitric oxide (NO) levels and increasing glutathione peroxidase (GSH-Px) and superoxide dismutase (SOD) levels and through its antiapoptotic capacity by inhibiting caspase-3 and p53 expression...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/29156533/serotonin-induces-peripheral-antinociception-via-the-opioidergic-system
#20
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
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