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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
#1
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...
January 5, 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
#2
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...
December 28, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28050773/the-effect-of-chronic-intermittent-hypoxia-on-respiratory-sensitivity-to-morphine-in-rats
#3
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
#4
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
#5
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
#6
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...
January 2, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/27922029/safety-of-eluxadoline-in-patients-with-irritable-bowel-syndrome-with-diarrhea
#7
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...
December 6, 2016: 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
#8
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
https://www.readbyqxmd.com/read/27799813/local-analgesic-effect-of-tramadol-is-mediated-by-opioid-receptors-in-late-postoperative-pain-after-plantar-incision-in-rats
#9
José Oswaldo de Oliveira Junior, Milena Fernandes de Freitas, Carolina Bullara de Andrade, Marucia Chacur, Hazem Adel Ashmawi
Tramadol is a drug used to treat moderate to severe pain. It is known to present a peripheral effect, but the local mechanisms underlying its actions remain unclear. The role of peripheral opioid receptors in postoperative pain is not well understood. In the present study, we examined the peripheral opioid receptors to determine the local effect of tramadol in a plantar incision pain model. Rats were subjected to plantar incision and divided into four groups on postoperative day (POD) 1: SF_SF, 0.9% NaCl injected into the right hindpaw; SF_TraI, 0...
2016: Journal of Pain Research
https://www.readbyqxmd.com/read/27778232/a-computational-systems-biology-approach-for-identifying-candidate-drugs-for-repositioning-for-cardiovascular-disease
#10
Alvin Z Yu, Stephen A Ramsey
We report an in silico method to screen for receptors or pathways that could be targeted to elicit beneficial transcriptional changes in a cellular model of a disease of interest. In our method, we integrate: (1) a dataset of transcriptome responses of a cell line to a panel of drugs; (2) two sets of genes for the disease; and (3) mappings between drugs and the receptors or pathways that they target. We carried out a gene set enrichment analysis (GSEA) test for each of the two gene sets against a list of genes ordered by fold-change in response to a drug in a relevant cell line (HL60), with the overall score for a drug being the difference of the two enrichment scores...
October 24, 2016: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/27775047/repetitive-electroacupuncture-attenuates-cold-induced-hypertension-through-enkephalin-in-the-rostral-ventral-lateral-medulla
#11
Min Li, Stephanie C Tjen-A-Looi, Zhi-Ling Guo, John C Longhurst
Acupuncture lowers blood pressure (BP) in hypertension, but mechanisms underlying its action are unclear. To simulate clinical studies, we performed electroacupuncture (EA) in unanesthetized rats with cold-induced hypertension (CIH) induced by six weeks of cold exposure (6 °C). EA (0.1 - 0.4 mA, 2 Hz) was applied at ST36-37 acupoints overlying the deep peroneal nerve for 30 min twice weekly for five weeks while sham-EA was conducted with the same procedures as EA except for no electrical stimulation...
October 24, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27744679/identification-of-the-first-marine-derived-opioid-receptor-balanced-agonist-with-a-signaling-profile-that-resembles-the-endorphins
#12
Tyler A Johnson, Laura Milan-Lobo, Tao Che, Madeline Ferwerda, Eptisam Lambo, Nicole L McIntosh, Fei Li, Li He, Nicholas Lorig-Roach, Phillip Crews, Jennifer Lynne Whistler
Opioid therapeutics are excellent analgesics, whose utility is compromised by dependence. Morphine (1) and its clinically relevant derivatives such as OxyContin® (4), Vicodin® (5) and Dilaudid® (6) are "biased" agonists at the µ opioid receptor (OR), wherein they engage G-protein signaling but poorly engage β-arrestin and the endocytic machinery. In contrast, the endorphins, met-enkephalin (14) and β-endorphin (15), endogenous peptide agonists for ORs, are more potent analgesics then 1, show reduced liability for tolerance and dependence, and engage both G-protein and β-arrestin pathways as "balanced" agonists...
October 17, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27734456/-opioidergic-postconditioning-of-heart-muscle-during-ischemia-reperfusion-injury
#13
Marcin Kunecki, Wojciech Płazak, Tomasz Roleder, Jolanta Biernat, Tomasz Oleksy, Piotr Podolec, Krzysztof Stanisław Gołba
BACKGROUND: Ischemic preconditioning (IPC) and postconditioning (POC) are the novel strategies of attaining cardioprotection against ischemia/reperfusion (I/R) injury. Previous studies suggested the role of opioid pathway, however the class of opioid receptors responsible for this effect in humans remains unknown. The aim of the study was to assess the influence of opioids on simulated I/R injury outcomes in the human myocardium. METHODS: Trabeculae of the human right atrium were electrically driven in organ bath and subjected to simulated I/R injury...
October 13, 2016: Cardiology Journal
https://www.readbyqxmd.com/read/27729853/feasibility-of-non-invasive-brain-modulation-for-management-of-pain-related-to-chemoradiotherapy-in-patients-with-advanced-head-and-neck-cancer
#14
Xiao-Su Hu, Clayton A Fisher, Stephanie M Munz, Rebecca L Toback, Thiago D Nascimento, Emily L Bellile, Laura Rozek, Avraham Eisbruch, Francis P Worden, Theodora E Danciu, Alexandre F DaSilva
Patients with head and neck cancer often experience a significant decrease in their quality of life during chemoradiotherapy (CRT) due to treatment-related pain, which is frequently classified as severe. Transcranial direct current stimulation (tDCS) is a method of non-invasive brain stimulation that has been frequently used in experimental and clinical pain studies. In this pilot study, we investigated the clinical impact and central mechanisms of twenty primary motor cortex (M1) stimulation sessions with tDCS during 7 weeks of CRT for head and neck cancer...
2016: Frontiers in Human Neuroscience
https://www.readbyqxmd.com/read/27670390/allostatic-mechanisms-of-opioid-tolerance-beyond-desensitization-and-downregulation
#15
REVIEW
Catherine M Cahill, Wendy Walwyn, Anna M W Taylor, Amynah A A Pradhan, Christopher J Evans
Mechanisms of opioid tolerance have focused on adaptive modifications within cells containing opioid receptors, defined here as cellular allostasis, emphasizing regulation of the opioid receptor signalosome. We review additional regulatory and opponent processes involved in behavioral tolerance, and include mechanistic differences both between agonists (agonist bias), and between μ- and δ-opioid receptors. In a process we will refer to as pass-forward allostasis, cells modified directly by opioid drugs impute allostatic changes to downstream circuitry...
November 2016: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/27665747/upregulation-and-activation-of-%C3%AE-%C3%A2-opioid-receptors-promotes-the-progression-of-human-breast-cancer
#16
Yang-Chao Wei, Bin Zhang, Xuan Li, Xiao-Meng Liu, Jing Zhang, Biao Lei, Bo Li, Run Zhai, Qian Chen, Yang Li
δ‑opioid receptor (DOR) belongs to the family of G protein‑coupled receptors (GPCRs). Numerous studies have shown that DOR is widely distributed in human peripheral tissues and is closely related to the development and progression of certain malignant tumours. However, there is controversy in the literature regarding whether DOR has an impact on the development and progression of human breast cancer. The present study comprehensively elaborates on the biological functions of DOR by determining the distribution of DOR expression in breast cancer tissues and cells and by further verifying the effects of DOR on breast cancer progression...
November 2016: Oncology Reports
https://www.readbyqxmd.com/read/27647873/abuse-potential-and-pharmacodynamic-characteristics-of-oral-and-intranasal-eluxadoline-a-mixed-%C3%AE-and-%C3%AE%C2%BA-opioid-receptor-agonist-and-%C3%AE-opioid-receptor-antagonist
#17
N Levy-Cooperman, G McIntyre, L Bonifacio, M McDonnell, J M Davenport, P S Covington, L S Dove, E M Sellers
Drugs with μ-opioid receptor (OR) activity can be associated with abuse and misuse. The peripherally acting mixed μ-OR and κ-OR agonist and δ-OR antagonist eluxadoline is approved in the United States for the treatment of irritable bowel syndrome with diarrhea. In two separate crossover studies, we evaluated the oral and intranasal abuse potential of eluxadoline versus placebo and the active control oxycodone. Healthy recreational opioid users received eluxadoline 100, 300, and 1000 mg, oxycodone 30 and 60 mg, and placebo (oral study), or eluxadoline 100 and 200 mg, oxycodone 15 and 30 mg, and placebos matched to eluxadoline and oxycodone (intranasal study)...
December 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27646288/histone-deacetylase-inhibitor-induced-emergence-of-synaptic-%C3%AE-opioid-receptors-and-behavioral-antinociception-in-persistent-neuropathic-pain
#18
Wenjuan Tao, Wenjie Zhou, Yuping Wang, Tingting Sun, Haitao Wang, Zhi Zhang, Yan Jin
The efficacy of opioids in patients with chronic neuropathic pain remains controversial. Although activation of δ-opioid receptors (DORs) in the brainstem reduces inflammation-induced persistent hyperalgesia, it is not effective under persistent neuropathic pain conditions and these clinical problems remain largely unknown. In this study, by using a chronic constriction injury (CCI) of the sciatic nerve in rats, we found that in the brainstem nucleus raphe magnus (NRM), DORs emerged on the surface membrane of central synaptic terminals on day 3 after CCI surgery and disappeared on day 14...
December 17, 2016: Neuroscience
https://www.readbyqxmd.com/read/27614546/an-optimised-phylogenetic-method-sheds-more-light-on-the-main-branching-events-of-rhodopsin-like-superfamily
#19
Michel E Mickael, Ashish Rajput, Jannetta Steyn, Lyle Wiemerslage, Thomas Bürglin
The comparative genomics between different rhodopsin-like family groups (α, β, γ and δ) is not well studied. We used a combination of phylogenetic analysis and statistical genomic methods to compare rhodopsin-like family proteins in species likely symbolic of this family's evolutionary progression. For intra-cluster relationships, we applied mathematical optimisation to enhance the tree search produced by the neighbour joining method (NJ) and compared it with maximum likelihood (ML) method. To infer inter-clusters relationships, we used Needleman-Wunsch analysis (NW), HHsearch, ancestral sequence reconstruction and phylogenetic network analysis...
September 3, 2016: Comparative Biochemistry and Physiology. Part D, Genomics & Proteomics
https://www.readbyqxmd.com/read/27607020/versatile-picklocks-to-access-all-opioid-receptors-tuning-the-selectivity-and-functional-profile-of-the-cyclotetrapeptide-c-phe-d-pro-phe-trp-cj-15-208
#20
Rossella De Marco, Andrea Bedini, Santi Spampinato, Lorenzo Cavina, Edoardo Pirazzoli, Luca Gentilucci
Recently, the tryptophan-containing noncationizable opioid peptides emerged with atypical structure and unexpected in vivo activity. Herein, we describe analogs of the naturally occurring mixed κ/μ-ligand c[Phe-d-Pro-Phe-Trp] 1 (CJ-15,208). Receptor affinity, selectivity, and agonism/antagonism varied upon enlarging macrocycle size, giving the μ-agonist 9 or the δ-antagonist 10 characterized by low nanomolar affinity. In particular, the μ-agonist c[β-Ala-d-Pro-Phe-Trp] 9 was shown to elicit potent antinociception in a mouse model of visceral pain upon systemic administration...
October 13, 2016: Journal of Medicinal Chemistry
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