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https://www.readbyqxmd.com/read/29926144/lappaconitine-a-c18-diterpenoid-alkaloid-exhibits-antihypersensitivity-in-chronic-pain-through-stimulation-of-spinal-dynorphin-a-expression
#1
Ming-Li Sun, Jun-Ping Ao, Yi-Rui Wang, Qian Huang, Teng-Fei Li, Xin-Yan Li, Yong-Xiang Wang
Lappaconitine is a representative C18-diterpenoid alkaloid extracted from Aconitum sinomontanum Nakai and has been prescribed as a pain relief medicine in China for more than 30 years. This study evaluated its antihypersensitivity activity in the rat models of neuropathic and cancer pains and explored its underlying mechanisms. Subcutaneous injection of cumulative doses of lappaconitine produced dose-dependent mechanical antiallodynia and thermal antihyperalgesia in spinal nerve ligation-induced neuropathic rats...
June 20, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29911992/motivational-valence-is-determined-by-striatal-melanocortin-4-receptors
#2
Anna Mathia Klawonn, Michael Fritz, Anna Nilsson, Jordi Bonaventura, Kiseko Shionoya, Elahe Mirrasekhian, Urban Karlsson, Maarit Jaarola, Björn Granseth, Anders Blomqvist, Michael Michaelides, David Engblom
It is critical for survival to assign positive or negative valence to salient stimuli in a correct manner. Accordingly, harmful stimuli and internal states characterized by perturbed homeostasis are accompanied by discomfort, unease, and aversion. Aversive signaling causes extensive suffering during chronic diseases, including inflammatory conditions, cancer, and depression. Here, we investigated the role of melanocortin 4 receptors (MC4Rs) in aversive processing using genetically modified mice and a behavioral test in which mice avoid an environment that they have learned to associate with aversive stimuli...
June 18, 2018: Journal of Clinical Investigation
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/29901392/constraining-endomorphin-1-by-%C3%AE-%C3%AE-hybrid-dipeptide-heterocycle-scaffolds-identification-of-a-novel-%C3%AE%C2%BA-opioid-receptor-selective-partial-agonist
#4
Rossella De Marco, Andrea Bedini, Santi Mario Spampinato, Lorenzo Comellini, Junwei Zhao, Roberto Artali, Luca Gentilucci
Herein we present the expedient synthesis of endomorphin-1 analogues containing stereoisomeric β2 -homo-Freidinger lactam-like scaffolds ([Amo2 ]EM), and we discuss opioid receptor (OR) affinity, enzymatic stability, functional activity, in vivo antinociceptive effects, and conformational and molecular docking analysis. Hence, H-Tyr-Amo-Trp-PheNH2 resulted to be a new chemotype of highly stable, selective, partial KOR agonist inducing analgesia, therefore displaying great potential interest as a painkiller possibly with reduced harmful side effects...
June 14, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29878268/the-protein-status-of-rats-affects-the-rewarding-value-of-meals-due-to-their-protein-content
#5
Catherine Chaumontet, Isidra Recio, Gilles Fromentin, Simon Benoit, Julien Piedcoq, Nicolas Darcel, Daniel Tomé
Background: Protein status is controlled by the brain, which modulates feeding behavior to prevent protein deficiency. Objective: This study tested in rats whether protein status modulates feeding behavior through brain reward pathways. Methods: Experiments were conducted in male Wistar rats (mean ± SD weight; 230 ± 16 g). In experiment 1, rats adapted for 2 wk to a low-protein (LP; 6% of energy) or a normal-protein (NP; 14% of energy) diet were offered a choice between 3 cups containing high-protein (HP; 50% of energy), NP, or LP feed; their intake was measured for 24 h...
June 1, 2018: Journal of Nutrition
https://www.readbyqxmd.com/read/29863085/kappa-opioid-receptor-agonist-administration-in-olfactory-bulbectomized-mice-restores-cognitive-impairment-through-cholinergic-neuron-activation
#6
Kohei Takahashi, Osamu Nakagawasai, Masae Sugawara, Atsushi Sato, Wataru Nemoto, Takeshi Tadano, Koichi Tan-No
Olfactory bulbectomized (OBX) mice are characterized by impaired performance in the passive avoidance test and decreased number of cholinergic neurons in the hippocampus. Several studies have reported that κ-opioid receptor agonists improve cognitive function in mice. However, their influence on OBX-induced cognitive dysfunction remains unclear. To address this question, we evaluated the effects of the endogenous κ-opioid receptor agonist dynorphin A (Dyn A) and the selective agonist trans-(-)-U-50488 on the behavior of OBX mice in the passive avoidance test...
2018: Biological & Pharmaceutical Bulletin
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
#7
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/29852138/differential-effects-of-left-and-right-neuropathy-on-opioid-gene-expression-in-lumbar-spinal-cord
#8
Olga Kononenko, Irina Mityakina, Vladimir Galatenko, Hiroyuki Watanabe, Igor Bazov, Anna Gerashchenko, Daniil Sarkisyan, Anna Iatsyshyna, Tatiana Yakovleva, Alex Tonevitsky, Niklas Marklund, Michael H Ossipov, Georgy Bakalkin
The endogenous opioid system (EOS) controls the processing of nociceptive stimuli and is a pharmacological target for opioids. Alterations in expression of the EOS genes under neuropathic pain condition may account for low efficacy of opioid drugs. We here examined whether EOS expression patterns are altered in the lumbar spinal cord of the rats with spinal nerve ligation (SNL) as a neuropathic pain model. Effects of the left- and right-side SNL on expression of EOS genes in the ipsi- and contralateral spinal domains were analysed...
May 28, 2018: Brain Research
https://www.readbyqxmd.com/read/29791013/frontline-science-buprenorphine-decreases-ccl2-mediated-migration-of-cd14-cd16-monocytes
#9
Matias Jaureguiberry-Bravo, Lillie Lopez, Joan W Berman
HIV infection of the CNS causes neuroinflammation and damage that contributes to the development of HIV-associated neurocognitive disorders (HAND) in greater than 50% of HIV-infected individuals, despite antiretroviral therapy (ART). Opioid abuse is a major risk factor for HIV infection. It has been shown that opioids can contribute to increased HIV CNS pathogenesis, in part, by modulating the function of immune cells. HIV enters the CNS within two weeks after peripheral infection by transmigration of infected monocytes across the blood brain barrier (BBB)...
May 23, 2018: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/29782857/quaternary-ammonium-salt-of-u50-488h-elicits-protective-effects-against-hypoxic-pulmonary-hypertension
#10
Yaguang Zhou, Xin Tian, Xueying Wang, Yuanbo Wang, Rong Fan, Yuemin Wang, Na Feng, Shumiao Zhang, Haitao Guo, Xiaoming Gu, Min Jia, Wen Yin, Zuoxu Hou, Juan Li, Jianming Pei
The present study aimed to investigate the role of quaternary ammonium salt of U50,488H (Q-U50,488H) in hypoxic pulmonary hypertension (HPH) and underlying mechanisms involved. A HPH animal model was established in rats under hypoxia and the mean pulmonary arterial pressure (mPAP) and right ventricular pressure (RVP) were measured. Relaxation of the pulmonary artery in response to Q-U50,488H was determined. In addition, expression and activity of endothelial nitric oxide (NO) synthase (eNOS) and inducible NO synthase (iNOS) with NO content, Akt expression, total antioxidant capacity (T-AOC), and gp91phox were evaluated...
May 18, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29782380/negative-modulation-of-spinal-%C3%AE%C2%BA-opioid-receptor-mediated-antinociception-by-the-%C3%A2%C2%B5-opioid-receptor-at-selective-doses-of-pentazocine
#11
Douglas L Robinson, Subodh Nag, Sukhbir S Mokha
The mixed-action κ-opioid receptor (KOR) agonist, pentazocine, binds to both KOR and the µ-opioid receptor (MOR). Racemic (±)-pentazocine and (-)-pentazocine, each administered systemically, have been shown to produce antinociception in various animal models. In contrast, racemic (±)-pentazocine failed to produce antinociception when administered intrathecally (i.t.). However, whether spinal activation of KOR and MOR by (-)-pentazocine produces antinociception and the relative contribution of KOR and MOR in mediating antinociception remain unknown...
May 18, 2018: Neuroreport
https://www.readbyqxmd.com/read/29743920/electroacupuncture-alleviates-pain-responses-and-inflammation-in-a-rat-model-of-acute-gout-arthritis
#12
Wenxin Chai, Yan Tai, Xiaomei Shao, Yi Liang, Guo-Qing Zheng, Ping Wang, Jianqiao Fang, Boyi Liu
Acute gout arthritis is one of the most painful inflammatory conditions. Treatments for gout pain are limited to colchicine, nonsteroidal anti-inflammatory drugs, and corticosteroids, which oftentimes result in severe adverse effects. Electroacupuncture (EA) has been proved to be effective in relieving many inflammatory pain conditions with few side effects. Here, we aim to investigate the therapeutic potentials of EA on pain and inflammation of a rat model of acute gout arthritis and underlying mechanisms...
2018: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29733100/does-nalbuphine-have-a-niche-in-managing-pain
#13
Mellar P Davis, Carlos Fernandez, Sally Regel, Mary Lynn McPherson
Nalbuphine has been commercially available for 40 years for the treatment of acute pain; few studies have centered on management of chronic pain. Nalbuphine unique pharmacology is an advantage in pain management. It is µ antagonist, partial κ agonist for G-proteins and beta-arrestin-2. Benefits are related to G-protein interactions resulting in less nausea, pruritus, and respiratory depression than morphine. At low doses, nalbuphine reduces side effects particularly respiratory depression without loss of analgesia when combined with potent opioids...
March 2018: Journal of Opioid Management
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
#14
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/29705547/nociceptin-orphanin-fq-receptors-modulate-the-discriminative-stimulus-effects-of-oxycodone-in-c57bl-6-mice
#15
D Matthew Walentiny, Jason M Wiebelhaus, Patrick M Beardsley
BACKGROUND: Nociceptin/orphanin FQ (NOP) receptor ligands have shown efficacy as putative analgesics and can modulate the abuse-related effects of opioids, suggesting therapeutic applications. The discriminative stimulus effects of a drug are related to their subjective effects, a predictor of abuse potential. To determine whether activation of NOP receptors could alter the subjective effects of an abused opioid analgesic, a novel oxycodone discrimination was established in mice, characterized with positive and negative controls, and its expression evaluated with a NOP receptor agonist...
June 1, 2018: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29686743/antinociceptive-activity-of-methanolic-extract-of-clinacanthus-nutans-leaves-possible-mechanisms-of-action-involved
#16
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/29678771/prenatal-ethanol-induces-an-anxiety-phenotype-and-alters-expression-of-dynorphin-nociceptin-orphanin-fq-genes
#17
Aranza Wille-Bille, Roberto Sebastián Miranda-Morales, Mariangela Pucci, Fabio Bellia, Claudio D'Addario, Ricardo Marcos Pautassi
Animal models have suggested that prenatal ethanol exposure (PEE) alters the κ opioid receptor system. The present study investigated the brain expression of dynorphin and nociceptin/orphanin FQ related genes and assessed anxiety-like behavior in the light-dark box (LDB), shelter-seeking and risk-taking behaviors in the concentric square field (CSF) test, and ethanol-induced locomotion in the open field (OF), in infant or adolescent Wistar rats that were exposed to PEE (0.0 or 2.0 g/kg, intragastrically, gestational days 17-20)...
July 13, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29663077/is-patient-reported-outcome-improved-by-nalfurafine-hydrochloride-in-patients-with-primary-biliary-cholangitis-and-refractory-pruritus-a-post-marketing-single-arm-prospective-study
#18
Minami Yagi, Atsushi Tanaka, Tadashi Namisaki, Atsushi Takahashi, Masanori Abe, Akira Honda, Yasushi Matsuzaki, Hiromasa Ohira, Hitoshi Yoshiji, Hajime Takikawa
BACKGROUND: Patients with primary biliary cholangitis (PBC) frequently suffer from pruritus, which can severely impair their health-related quality of life (HRQOL). Nalfurafine hydrochloride, a selective κ-opioid receptor agonist, was recently approved in Japan for refractory pruritus in patients with chronic liver diseases, but it still remains unclear whether this treatment improves the patient-reported outcome (PRO) in PBC patients with refractory pruritus. Herein, we conducted a multicenter, post-marketing, single-arm prospective study to investigate the efficacy of nalfurafine in terms of PRO, and the associations of the efficacy with any clinical characteristics...
April 16, 2018: Journal of Gastroenterology
https://www.readbyqxmd.com/read/29659201/evaluation-of-eluxadoline-effect-on-cardiac-repolarization
#19
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
#20
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
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