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https://www.readbyqxmd.com/read/29909236/antiepileptic-drugs-as-analgesics-adjuvants-in-inflammatory-pain-current-preclinical-evidence
#1
REVIEW
Tomić Maja, Pecikoza Uroš, Micov Ana, Vučković Sonja, Stepanović-Petrović Radica
Inflammatory pain is the most common type of pain that is treated clinically. The use of currently available treatments (classic analgesics - NSAIDs, paracetamol and opioids) is limited by insufficient efficacy and/or side effects/tolerance development. Antiepileptic drugs (AEDs) are widely used in neuropathic pain treatment, but there is substantial preclinical evidence on their efficacy against inflammatory pain, too. In this review we focus on gabapentinoids (gabapentin and pregabalin) and dibenzazepine AEDs (carbamazepine, oxcarbazepine, and recently introduced eslicarbazepine acetate) and their potential for relieving inflammatory pain...
June 15, 2018: Pharmacology & Therapeutics
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/29903752/what-place-is-there-for-tramadol-dexketoprofen
#3
(no author information available yet)
No single analgesic provides effective pain relief in all patients and increasing the dose of an analgesic may increase its unwanted effects.1 In addition, pain frequently results from multiple mechanisms that may respond to different pharmacological interventions.2 One suggested approach is to combine analgesics with different modes of action, with the aim of delivering better analgesia using lower doses of each drug.1 Skudexa (A. Menarini Farmaceutica Internazionale SRL), a combination of tramadol hydrochloride (a synthetic opioid analgesic that is a partial agonist at the μ, δ and κ opioid receptors) and dexketoprofen (a NSAID), is licensed for short term treatment of moderate to severe acute pain in adults...
June 2018: Drug and Therapeutics Bulletin
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
#4
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
#5
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/29861097/a-model-of-%C3%AE-9-tetrahydrocannabinol-self-administration-and-reinstatement-that-alters-synaptic-plasticity-in-nucleus-accumbens
#6
Sade Spencer, Daniela Neuhofer, Vivian C Chioma, Constanza Garcia-Keller, Danielle J Schwartz, Nicholas Allen, Michael D Scofield, Tara Ortiz-Ithier, Peter W Kalivas
BACKGROUND: Cannabis is the most widely used illicit drug, but knowledge of the neurological consequences of cannabis use is deficient. Two primary components of cannabis are Δ9 -tetrahydrocannabinol (THC) and cannabidiol (CBD). We established a THC+CBD model of self-administration and reinstated drug seeking to determine if, similar to other addictive drugs, cannabis produces enduring synaptic changes in nucleus accumbens core (NAcore) thought to contribute vulnerability to drug reinstatement...
May 3, 2018: Biological Psychiatry
https://www.readbyqxmd.com/read/29858921/perioperative-antiemetic-efficacy-of-dexamethasone-versus-5-ht3-receptor-antagonists-a-meta-analysis-and-trial-sequential-analysis-of-randomized-controlled-trials
#7
REVIEW
Preet Mohinder Singh, Anuradha Borle, Rajesh Panwar, Jeetinder Kaur Makkar, Ian McGrath, Anjan Trikha, Ashish Sinha
BACKGROUND: Dexamethasone has many desirable pharmacologic properties for perioperative use. Its antiemetic potential has been a focus of many recent trials. METHODS: Trials comparing dexamethasone to 5-HT3-receptor antagonists (5HT3-RA) for 24 h postoperative vomiting incidences published till August 2017 were searched in the medical database. Comparisons for antiemetic efficiency variables (vomiting incidence, nausea incidence, rescue antiemetic need, and patients with complete response) during early (until 6 h) and late postoperative phase were made...
June 1, 2018: European Journal of Clinical 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
#8
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/29781560/conditioned-reward-of-opioids-but-not-psychostimulants-is-impaired-in-gaba-a-receptor-%C3%AE-subunit-knockout-mice
#9
Milo S Siivonen, Elena de Miguel, Juho Aaltio, Aino K Manner, Mikko Vahermo, Jari Yli-Kauhaluoma, Anni-Maija Linden, Teemu Aitta-Aho, Esa R Korpi
Extrasynaptic δ subunit-containing γ-aminobutyric acid type A receptors (δ-GABAA Rs) are emerging as targets for a number of neuropsychopharmacological drugs, including the direct GABA-site agonist gaboxadol and neuroactive steroids. Among other regions, these δ-GABAA Rs are functionally expressed in the ventral tegmental area (VTA), the cell body region of mesocorticolimbic dopamine (DA) system important for motivated behaviors, and in the target region, the nucleus accumbens. Gaboxadol and neurosteroids induce VTA DA neuron plasticity ex vivo, by inhibiting the VTA GABA neurons, and aversive place conditioning, which are absent in the δ-GABAA R knockout mice (δ-KO)...
May 21, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29778745/phytohormone-abscisic-acid-elicits-antinociceptive-effects-in-rats-through-the-activation-of-opioid-and-peroxisome-proliferator-activated-receptors-%C3%AE-%C3%AE
#10
Mahtab Mollashahi, Mehdi Abbasnejad, Saeed Esmaeili-Mahani
The phytohormone abscisic acid exists in animal tissues particularly in the brain. However, its neurophysiological effects have not yet been fully clarified. This study was designed to evaluate the possible antinociceptive effects of abscisic acid on animal models of pain and determine its possible signaling mechanism. Tail-flick, hot-plate and formalin tests were used to assess the nociceptive threshold. All experiments were carried out on male Wistar rats. To determine the role of Peroxisome proliferator-activated receptor β/δ (PPARβ/δ) and opioid receptors on the induction of abscisic acid antinociception, specific antagonists were injected 15min before abscisic acid...
May 17, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29768254/neuroprotection-against-hypoxic-ischemic-injury-%C3%AE-opioid-receptors-and-bdnf-trkb-pathway
#11
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
#12
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
#13
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
#14
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/29686743/antinociceptive-activity-of-methanolic-extract-of-clinacanthus-nutans-leaves-possible-mechanisms-of-action-involved
#15
Zainul Amiruddin Zakaria, Mohammad Hafiz Abdul Rahim, Rushduddin Al Jufri Roosli, Mohd Hijaz Mohd Sani, Maizatul Hasyima Omar, Siti Farah Mohd Tohid, Fezah Othman, Siew Mooi Ching, Arifah Abdul Kadir
Methanolic extract of Clinacanthus nutans Lindau leaves (MECN) has been proven to possess antinociceptive activity that works via the opioid and NO-dependent/cGMP-independent pathways. In the present study, we aimed to further determine the possible mechanisms of antinociception of MECN using various nociceptive assays. The antinociceptive activity of MECN was (i) tested against capsaicin-, glutamate-, phorbol 12-myristate 13-acetate-, bradykinin-induced nociception model; (ii) prechallenged against selective antagonist of opioid receptor subtypes ( β -funaltrexamine, naltrindole, and nor-binaltorphimine); (iii) prechallenged against antagonist of nonopioid systems, namely, α 2 -noradrenergic (yohimbine), β -adrenergic (pindolol), adenosinergic (caffeine), dopaminergic (haloperidol), and cholinergic (atropine) receptors; (iv) prechallenged with inhibitors of various potassium channels (glibenclamide, apamin, charybdotoxin, and tetraethylammonium chloride)...
2018: Pain Research & Management: the Journal of the Canadian Pain Society
https://www.readbyqxmd.com/read/29669290/non-canonical-opioid-signaling-inhibits-itch-transmission-in-the-spinal-cord-of-mice
#16
Admire Munanairi, Xian-Yu Liu, Devin M Barry, Qianyi Yang, Jun-Bin Yin, Hua Jin, Hui Li, Qing-Tao Meng, Jia-Hang Peng, Zhen-Yu Wu, Jun Yin, Xuan-Yi Zhou, Li Wan, Ping Mo, Seungil Kim, Fu-Quan Huo, Joseph Jeffry, Yun-Qing Li, Rita Bardoni, Michael R Bruchas, Zhou-Feng Chen
Chronic itch or pruritus is a debilitating disorder that is refractory to conventional anti-histamine treatment. Kappa opioid receptor (KOR) agonists have been used to treat chronic itch, but the underlying mechanism remains elusive. Here, we find that KOR and gastrin-releasing peptide receptor (GRPR) overlap in the spinal cord, and KOR activation attenuated GRPR-mediated histamine-independent acute and chronic itch in mice. Notably, canonical KOR-mediated Gαi signaling is not required for desensitizing GRPR function...
April 17, 2018: Cell Reports
https://www.readbyqxmd.com/read/29659201/evaluation-of-eluxadoline-effect-on-cardiac-repolarization
#17
Laura Bonifacio, Thomas L Hunt, Gail McIntyre, Leonard S Dove, Paul S Covington
This study evaluated the effects of eluxadoline, a mixed μ-opioid receptor (OR) and κ-OR agonist and δ-OR antagonist, on cardiac repolarization. This evaluator-blinded, placebo- and positive-controlled, 4-period crossover study randomized healthy men and women to single oral doses of eluxadoline (therapeutic dose 100 mg or supratherapeutic dose 1000 mg), moxifloxacin 400 mg, or placebo. QT data were corrected using individual custom correction (QTcI). The primary endpoint was the change from baseline in QTcI intervals (ΔQTcI) between eluxadoline and placebo (ΔΔQTcI)...
April 16, 2018: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29649035/pharmacological-characterization-of-levorphanol-a-g-protein-biased-opioid-analgesic
#18
Valerie Le Rouzic, Ankita Narayan, Amanda Hunkle, Gina F Marrone, Zhigang Lu, Susruta Majumdar, Jin Xu, Ying-Xian Pan, Gavril W Pasternak
BACKGROUND: Levorphanol is a potent analgesic that has been used for decades. Most commonly used for acute and cancer pain, it also is effective against neuropathic pain. The recent appreciation of the importance of functional bias and the uncovering of multiple µ opioid receptor splice variants may help explain the variability of patient responses to different opioid drugs. METHODS: Here, we evaluate levorphanol in a variety of traditional in vitro receptor binding and functional assays...
April 11, 2018: Anesthesia and Analgesia
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
#19
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
#20
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
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