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https://www.readbyqxmd.com/read/28877966/t-cell-mediation-of-pregnancy-analgesia-affecting-chronic-pain-in-mice
#1
Sarah F Rosen, Boram Ham, Shannon Drouin, Nadia Boachie, Anne-Julie Chabot-Dore, Jean-Sebastien Austin, Luda Diatchenko, Jeffrey S Mogil
It has been consistently reported that many female chronic pain sufferers have an attenuation of symptoms during pregnancy. Rats display increased pain tolerance during pregnancy, due to an increase in opioid receptors in the spinal cord. These past studies did not consider the role of non-neuronal cells, now appreciated to play an important role in chronic pain processing. Using an inflammatory (complete Freund's adjuvant) or neuropathic (spared nerve injury) model of persistent pain, we observe that young adult female mice in early pregnancy switch from a micgrolia-independent to a microglia-dependent pain hypersensitivity mechanism...
September 6, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28857657/opioid-system-contribution-to-the-antidepressant-like-action-of-m-trifluoromethyl-diphenyl-diselenide-in-mice-a-compound-devoid-of-tolerance-and-withdrawal-syndrome
#2
Suzan G Rosa, Ana P Pesarico, Carolina F Tagliapietra, Sônia C A da Luz, Cristina W Nogueira
Animal and clinical researches indicate that the opioid system exerts a crucial role in the etiology of mood disorders and is a target for intervention in depression treatment. This study investigated the contribution of the opioid system to the antidepressant-like action of acute or repeated m-trifluoromethyl-diphenyl diselenide administration to Swiss mice. m-Trifluoromethyl-diphenyl diselenide (50 mg/kg, intragastric) produced an antidepressant-like action in the forced swimming test from 30 min to 24 h after treatment...
August 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28844215/antinociceptive-and-anti-inflammatory-activities-of-leaf-extracts-from-annona-tomentosa-r-e-fr
#3
Lilian Uchoa Carneiro, Ilna Gomes da Silva, Mirian Eliza Alves de Souza, Wellington da Silva Côrtes, Mário Geraldo de Carvalho, Bruno Guimarães Marinho
OBJECTIVE: Annona tomentosa R.E.Fr is a species not endemic to Brazil that belongs to the phytogeographic areas of the Amazon, Cerrado and Pantanal. Popularly known as "araticum rasteiro" or "araticum de moita", A. tomentosa is edible and tea made from the leaves has been used as an anti-inflammatory by native communities. There is no scientific evidence for these uses of A. tomentosa, especially those related to the control of pain and inflammation. For this reason, in the present study we evaluated the antinociceptive and anti-inflammatory activities of partitions from the methanolic extract of A...
September 2017: Journal of Integrative Medicine
https://www.readbyqxmd.com/read/28819330/synthesis-and-investigation-of-mixed-%C3%AE-opioid-and-%C3%AE-opioid-agonists-as-possible-bivalent-ligands-for-treatment-of-pain
#4
Ruben S Vardanyan, James P Cain, Saghar Mowlazadeh Haghighi, Vlad K Kumirov, Mary I McIntosh, Alexander J Sandweiss, Frank Porreca, Victor J Hruby
Several studies have suggested functional association between μ-opioid and δ-opioid receptors and showed that μ-activity could be modulated by δ-ligands. The general conclusion is that agonists for the δ-receptor can enhance the analgesic potency and efficacy of μ-agonists. Our preliminary investigations demonstrate that new bivalent ligands constructed from the μ-agonist fentanyl and the δ-agonist enkephalin-like peptides are promising entities for creation of new analgesics with reduced side effects for treatment of neuropathic pain...
March 2017: Journal of Heterocyclic Chemistry
https://www.readbyqxmd.com/read/28806211/the-opiorphin-analog-str-324-decreases-sensory-hypersensitivity-in-a-rat-model-of-neuropathic-pain
#5
Alain Van Elstraete, Philippe Sitbon, Leila Hamdi, Victor Juarez-Perez, Jean-Xavier Mazoit, Dan Benhamou, Catherine Rougeot
BACKGROUND: Neuropathic pain represents a therapeutic challenge, and treatments with increased efficacy and tolerability still need to be developed. Opiorphin protects endogenous enkephalins from degradation, potentiating enkephalin-dependent analgesia via the activation of opioid pathways. Enkephalins are natural ligands of opioid receptors, with strong affinity for δ-opioid receptors. Expression of functional δ-opioid receptors increases in sensory neurons after peripheral nerve injury in neuropathic pain models...
August 10, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28781901/enkephalins-endogenous-analgesics-with-an-emerging-role-in-stress-resilience
#6
REVIEW
Mathilde S Henry, Louis Gendron, Marie-Eve Tremblay, Guy Drolet
Psychological stress is a state of mental or emotional strain or tension that results from adverse or demanding circumstances. Chronic stress is well known to induce anxiety disorders and major depression; it is also considered a risk factor for Alzheimer's disease. Stress resilience is a positive outcome that is associated with preserved cognition and healthy aging. Resilience presents psychological and biological characteristics intrinsic to an individual conferring protection against the development of psychopathologies in the face of adversity...
2017: Neural Plasticity
https://www.readbyqxmd.com/read/28758123/peripheral-antinociception-induced-by-aripiprazole-is-mediated-by-the-opioid-system
#7
Renata Cristina Mendes Ferreira, Ana Flávia Almeida-Santos, Igor Dimitri Gama Duarte, Daniele C Aguiar, Fabricio A Moreira, Thiago Roberto Lima Romero
BACKGROUND: Aripiprazole is an antipsychotic drug used to treat schizophrenia and related disorders. Our previous study showed that this compound also induces antinociceptive effects. The present study aimed to assess the participation of the opioid system in this effect. METHODS: Male Swiss mice were submitted to paw pressure test and hyperalgesia was induced by intraplantar injection of prostaglandin E2 (PGE2, 2 μg). Aripiprazole was injected 10 min before the measurement...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28740609/simple-tetrahydroisoquinolines-are-potent-and-selective-kappa-opioid-receptor-antagonists
#8
Chad M Kormos, Pauline W Ondachi, Scott P Runyon, James B Thomas, S Wayne Mascarella, Ann M Decker, Hernán A Navarro, F Ivy Carroll
Potent and selective κ opioid receptor antagonists have been derived from the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of pure opioid receptor antagonists. In order to determine if the 3-hydroxyphenyl and/or the piperidine amino groups are required for obtaining the pure opioid antagonists, (3R)-7-hydroxy-N-[(1S)-2-methyl-1-(piperidine-1-ylmethyl)propyl]-1,2,3,4-tetrahydroiosquinoline-3-carboxamide (1), which does not have a 4-(3-hydroxyphenyl) group, and (3R)-N-(1R)-1-(cyclohexylmethyl)-2-methylpropyl]-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (2), which does not have a 4-hydroxylphenyl or a piperidine amino group, were synthesized and evaluated for their [(35)S]GTPγS binding properties at the μ, δ, and κ opioid receptors...
July 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28726190/effect-of-peripheral-%C3%AE-%C3%AE-and-%C3%AE%C2%BA-opioid-ligands-on-the-development-of-tolerance-to-ethanol-induced-analgesia
#9
S K Sudakov, E V Alekseeva, G A Nazarova
We studied the rate of development of tolerance to the ethanol-induced analgesia under the effect of μ-, δ-, and κ-opioid agonists and antagonists not crossing the blood-brain barrier and rapidly inactivated by gastric and duodenal proteolytic enzymes. Activation of gastric κ-opioid receptors eliminated the analgesic effect of ethanol and accelerated the development of tolerance to ethanol-induced analgesia. In contrast, activation of gastric μ-opioid receptors decelerated the development of this tolerance...
June 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28700700/the-induction-of-the-transcription-factor-nrf2-enhances-the-antinociceptive-effects-of-delta-opioid-receptors-in-diabetic-mice
#10
Christina McDonnell, Sergi Leánez, Olga Pol
The involvement of heme oxygenase 1 (HO-1) in the modulation of the antinociceptive effects of opioids in type 1 diabetes has been demonstrated but the role played by the transcription factor Nrf2 in the regulation of painful neuropathy and in the effects and expression of δ-opioid receptors (DOR) in type 2 diabetes, has not been studied. In male BKS.Cg-m+/+Leprdb/J (db/db) mice, the anti-allodynic effects produced by a Nrf2 transcription factor activator, sulforaphane (SFN) administered alone and combined with two DOR agonists, [d-Pen(2),d-Pen(5)]-Enkephalin (DPDPE) and (+)-4-[(αR)-α-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N diethylbenzamide (SNC-80), were evaluated...
2017: PloS One
https://www.readbyqxmd.com/read/28662966/antitrichomonal-activity-of-%C3%AE-opioid-receptor-antagonists-7-benzylidenenaltrexone-derivatives
#11
Noriki Kutsumura, Yasuaki Koyama, Yasuyuki Nagumo, Ryo Nakajima, Yoshiyuki Miyata, Naoshi Yamamoto, Tsuyoshi Saitoh, Naoko Yoshida, Satoshi Iwata, Hiroshi Nagase
The 7-benzylidenenaltrexone (BNTX) derivatives 2a-v, 3a-c, 13a-c, and 14a were synthesized from naltrexone (1) and evaluated for their antitrichomonal activity. The structure-activity-relationship studies found that 4-iodo-BNTX (2g) showed the highest activity (IC50=10.5µM) and the affinity for the opioid receptor was less important for antitrichomonal activity against Trichomonas vaginalis. The morphinan skeleton bearing both the double bond for a Michael acceptor and the phenolic hydroxy group would be a specific template for development of antitrichomonal agents...
August 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28647729/analgesic-effects-of-diluted-bee-venom-acupuncture-mediated-by-%C3%AE-opioid-and-%C3%AE-2-adrenergic-receptors-in-osteoarthritic-rats
#12
Jeong-Eun Huh, Byung-Kwan Seo, Jung-Woo Lee, Chanyoung Kim, Yeon-Cheol Park, Jae-Dong Lee, Yong-Hyeon Baek
Context • Pain from osteoarthritis is associated with peripheral nociception and central pain processing. Given the unmet need for innovative, effective, and well-tolerated therapies, many patients, after looking for more satisfactory alternatives, decide to use complementary and alternative modalities. The analgesic mechanism of subcutaneous injections of diluted bee venom into an acupoint is thought to be part of an anti-inflammatory effect and the central modulation of pain processing. Objectives • Using the rat model of collagenase-induced osteoarthritis (CIOA), the study intended to investigate the analgesic effects of bee venom acupuncture (BVA) as they are related to the acupuncture points and dosage used and to determine whether the analgesic mechanisms of BVA for pain were mediated by opioid or adrenergic receptors...
June 23, 2017: Alternative Therapies in Health and Medicine
https://www.readbyqxmd.com/read/28647372/delta-opioid-receptor-agonist-attenuates-lipopolysaccharide-induced-myocardial-injury-by-regulating-autophagy
#13
Pin Zhao, Jianke Kuai, Jinjian Gao, Li Sun, Yan Wang, Linong Yao
BACKGROUND: Previous studies have described the protective effects of DADLE on myocardial injury in sepsis. Recently, autophagy has been shown to be an innate defense mechanism in sepsis-related myocardial injury. However, whether DADLE has an pro-autophagic effect is yet to be elucidated. The present study aimed to investigate the effect of DADLE on the regulation of autophagy during sepsis. METHODS: Male mice were subjected to LPS or vehicle intraperitoneal injection...
October 7, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28645007/activation-of-the-pi3k-akt-pathway-promotes-neuroprotection-of-the-%C3%AE-opioid-receptor-agonist-against-cerebral-ischemia-reperfusion-injury-in-rat-models
#14
Mei-Rong Lv, Bin Li, Ming-Guang Wang, Fan-Guo Meng, Jian-Jun Yu, Feng Guo, Ye Li
The central objective was to identify the role of the PI3K-Akt activation pathway on the neuroprotection of δ-opioid receptor agonist (DADLE) against cerebral ischemia-reperfusion (I/R) injury in a rat model. Fifty-five male Sprague-Dawley (SD) rats were included to establish a middle cerebral artery occlusion (MCAO) model which were then divided into the sham, MCAO, LY294002 (MCAO+DADLE+LY294002 [inhibitor of PI3K-Akt pathway]), DADLE (MCAO+DADLE) and DMSO (MCAO+DADLE+DMSO [dimethyl sulphoxide]) groups. The cerebral infarction (CI) volume and nerve cell apoptosis was determined using TTC and TUNEL staining...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28640078/prospective-observational-pharmacogenetic-study-of-side-effects-induced-by-intravenous-morphine-for-postoperative-analgesia
#15
Li-Kuei Chen, Mao-Hsien Wang, Hong-Jyh Yang, Shou-Zen Fan, Shiou-Sheng Chen
Nausea and vomiting are probably the most unpleasant side effects that occur when morphine used. A number of studies have investigated the effect on pain relief of single nucleotide polymorphisms (SNPs) in genes involved in morphine's metabolism, distribution, binding, and cellular action. The mechanism through which morphine causes nausea and vomiting has not been elucidated clearly. We examined all the reported SNPs which are associated with the complications of morphine, including SNPs in genes for phase I and phase II metabolic enzymes, ABC binding cassette drug transporters, κ and δ opioid receptors, and ion channels implicated in the postreceptor action of morphine...
June 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28620922/supraspinal-inhibitory-effects-of-chimeric-peptide-mcrt-on-gastrointestinal-motility-in-mice
#16
Chunbo He, Hailan Li, Jing Zhang, Yanping Kang, Fang Jia, Shouliang Dong, Lanxia Zhou
OBJECTIVES: Chimeric peptide MCRT, based on morphiceptin and PFRTic-NH2 , was a bifunctional ligand of μ- and δ-opioid receptors (MOR-DOR) and produced potent analgesia in tail-withdrawal test. The study focused on the supraspinal effects of morphiceptin, PFRTic-NH2 and MCRT on gastrointestinal motility. Moreover, opioid receptor antagonists, naloxone (non-selective), cyprodime (MOR selective) and naltrindole (DOR selective) were utilized to explore the mechanisms. METHODS: Intracerebroventricular administration was achieved via the implanted cannula...
June 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28602640/design-and-synthesis-of-novel-%C3%AE-opioid-receptor-agonists-with-an-azatricyclodecane-skeleton-for-improving-blood-brain-barrier-penetration
#17
Yoshikazu Watanabe, Kohei Hayashida, Daisuke Saito, Toshihiro Takahashi, Junichi Sakai, Eriko Nakata, Takashi Kanda, Takashi Iwai, Shigeto Hirayama, Hideaki Fujii, Tomio Yamakawa, Hiroshi Nagase
We designed and synthesized novel δ opioid receptor (DOR) agonists 3a-i with an azatricyclodecane skeleton, which was a novel structural class of DOR agonists. Among them, 3b exhibited high values of binding affinity and potent agonistic activity for the DOR that were approximately equivalent to those of 2 which bore an oxazatricyclodecane skeleton. In vitro assays using the blood-brain barrier (BBB) permeability test kit supported the idea that 3b achieved an excellent BBB permeability by converting an oxygen atom of 2 to a carbon atom (methylene group) in the core skeleton...
August 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28596506/by-up-regulating-%C3%AE-and-%C3%AE-opioid-receptors-neuron-restrictive-silencer-factor-knockdown-promotes-neurological-recovery-after-ischemia
#18
Hui-Min Liang, Li-Jiao Geng, Xiao-Yan Shi, Chao-Gang Zhang, Shu-Yan Wang, Guang-Ming Zhang
We investigated the effects of neuron-restrictive silencer factor (NRSF) on proliferation of endogenous nerve stem cells (NSCs) and on μ- and δ-opioid receptor (MOR/DOR) expression in rats after cerebral ischemia. Among 100 rats subjected to cerebral ischemia, 20 rats were transfected with NRSF shRNA, and the remaining 80 were randomly assigned to normal, sham, model, and negative control (NC) groups. On days 7, 14, and 28 after ischemia and reperfusion, neurological function scores were assigned and a step-down passive avoidance test was conducted...
May 23, 2017: Oncotarget
https://www.readbyqxmd.com/read/28590304/antinociceptive-effect-of-epicatechin-in-inflammatory-and-neuropathic-pain-in-rats
#19
Geovanna N Quiñonez-Bastidas, Jorge B Pineda-Farias, Francisco J Flores-Murrieta, Juan Rodríguez-Silverio, Juan G Reyes-García, Beatriz Godínez-Chaparro, Vinicio Granados-Soto, Héctor I Rocha-González
The aim of this study was to investigate the antinociceptive potential of (-)-epicatechin and the possible mechanisms of action involved in its antinociceptive effect. The carrageenan and formalin tests were used as inflammatory pain models. A plethysmometer was used to measure inflammation and L5/L6 spinal nerve ligation as a neuropathic pain model. Oral (-)-epicatechin reduced carrageenan-induced inflammation and nociception by about 59 and 73%, respectively, and reduced formalin- induced and nerve injury-induced nociception by about 86 and 43%, respectively...
June 5, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28566554/pi3k-class-ii-%C3%AE-regulates-%C3%AE-opioid-receptor-export-from-the-trans-golgi-network
#20
Daniel J Shiwarski, Marlena Darr, Cheryl A Telmer, Marcel P Bruchez, Manojkumar A Puthenveedu
The interplay between signaling and trafficking by G protein-coupled receptors (GPCRs) has focused mainly on endocytic trafficking. Whether and how surface delivery of newly synthesized GPCRs is regulated by extracellular signals is less understood. Here we define a signaling-regulated checkpoint at the trans-Golgi network (TGN) that controls the surface delivery of the delta opioid receptor (δR). In PC12 cells, inhibition of phosphoinositide-3 kinase (PI3K) activity blocked export of newly synthesized δR from the Golgi and delivery to the cell surface, similar to treatment with nerve growth factor (NGF)...
August 1, 2017: Molecular Biology of the Cell
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