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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
#1
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
#2
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
#3
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/29624527/dezocine-alleviates-morphine-induced-dependence-in-rats
#4
Fei-Xiang Wu, Hasan Babazada, Hao Gao, Xi-Ping Huang, Chun-Hua Xi, Chun-Hua Chen, Jin Xi, Wei-Feng Yu, Renyu Liu
BACKGROUND: Opioid dependence is a major public health issue without optimal therapeutics. This study investigates the potential therapeutic effect of dezocine, a nonaddictive opioid, in opioid dependence in rat models. METHODS: Dezocine was administered intraperitoneally to a morphine-dependent rat model to investigate its effect on withdrawal and conditioned place preference (CPP). Effect of dezocine on morphine withdrawal syndrome and CPP was analyzed using 2-way analysis of variance (ANOVA) followed by Tukey's post hoc test...
April 5, 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
#5
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/29575372/radar-plots-a-novel-modality-for-displaying-disparate-data-on-the-efficacy-of-eluxadoline-for-the-treatment-of-irritable-bowel-syndrome-with-diarrhea
#6
D M Brenner, L S Dove, D A Andrae, P S Covington, C Gutman, W D Chey
BACKGROUND: Patients with irritable bowel syndrome with diarrhea (IBS-D) experience a range of abdominal and bowel symptoms; successful management requires alleviation of this constellation of symptoms. Eluxadoline, a locally active mixed μ- and κ-opioid receptor agonist and δ-opioid receptor antagonist, is approved for the treatment of IBS-D in adults based on the results of 2 Phase 3 studies. Radar plots can facilitate comprehensive, visual evaluation of diverse but interrelated efficacy endpoints...
March 25, 2018: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/29556136/secondary-metabolites-isolated-from-pinus-roxburghii-and-interpretation-of-their-cannabinoid-and-opioid-binding-properties-by-virtual-screening-and-in-vitro-studies
#7
Rola M Labib, Radhakrishnan Srivedavyasasri, Fadia S Youssef, Samir A Ross
Pinus roxburghii is highly popular as a potent analgesic and anti-inflammatory agent; however its exact mechanism of action was not fully elucidated. We aimed to interpret the analgesic and anti-inflammatory activity of the total ethanol extract of Pinus roxburghii bark (PRE) and its isolated compounds by both in silico molecular modelling and in-vitro cannabinoid and opioid binding activities evaluation for the first time. Comprehensive phytochemical investigation of PRE resulted in the isolation of sixteen compounds that were fully elucidated using1 H NMR and13 C NMR...
March 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/29552078/isolation-and-biological-evaluation-of-prenylated-flavonoids-from-maclura-pomifera
#8
Yerkebulan Orazbekov, Mohamed A Ibrahim, Serjan Mombekov, Radhakrishnan Srivedavyasasri, Ubaidilla Datkhayev, Bauyrzhan Makhatov, Narayan D Chaurasiya, Babu L Tekwani, Samir A Ross
Phytochemical analysis of the ethanolic extract of Maclura pomifera fruits yielded four new compounds ( I - IV ) along with eleven known compounds ( V - XV ). The crude extract exhibited significant activity towards cannabinoid receptors (CB1: 103.4% displacement; CB2: 68.8% displacement) and possibly allosteric interaction with δ and μ opioid receptors (-49.7 and -53.8% displacement, resp.). Compound I was found to be possibly allosteric for κ and μ opioid receptors (-88.4 and -27.2% displacement, resp...
2018: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29501769/the-efficacy-of-a-lectin-from-abelmoschus-esculentus-depends-on-central-opioid-receptor-activation-to-reduce-temporomandibular-joint-hypernociception-in-rats
#9
Shirley Moreira Alves, Raul Sousa Freitas, Danielle Rocha do Val, Lorena Vasconcelos Vieira, Ellen Lima de Assis, Francisco Isaac Fernandes Gomes, Carlos Alberto de Almeida Gadelha, Tatiane Santi Gadelha, José Thalles Jocelino Gomes de Lacerda, Juliana Trindade Clemente-Napimoga, Vicente de Paulo Teixeira Pinto, Gerardo Cristino Filho, Mirna Marques Bezerra, Hellíada Vasconcelos Chaves
Abelmoschus esculentus is largely cultivated in Northeastern Brazil for medicinal purposes, e.g. inflammatory conditions. This study aimed to evaluate the efficacy of Abelmoschus esculentus lectin (AEL) in reducing formalin-induced temporomandibular joint inflammatory hypernociception in rats. The behavioral experiments were performed in male Wistar rats (180-240 g). Rats were pre-treated (i.v.) with AEL (0.001, 0.01 or 0.1 mg/kg) 30 min before formalin injection (i.art.). To analyze the possible effect of opioid pathways on AEL efficacy, animals were pre-treated with naloxone or CTOP (μ opioid receptor antagonist), naltrindole (δ opioid receptor antagonist) or nor-binaltorphimine (κ opioid receptor antagonist) (i...
March 1, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29499274/role-of-dorsal-hippocampus-%C3%AE%C2%BA-opioid-receptors-in-contextual-aversive-memory-consolidation-in-rats
#10
Felipe Vanz, Maíra Assunção Bicca, Vagner Fagnani Linartevichi, Marcelo Giachero, Leandro José Bertoglio, Thereza C Monteiro de Lima
The main κ opioid receptors (κORs) subtypes already described (κ1 ORs and κ2 ORs) are expressed in brain regions involved in aversive memory consolidation, including the dorsal hippocampus (DH). However, the role of DH κORs in consolidation of aversive memories with varied intensity and specificity is still uncertain. The present study aimed to investigate this question using pharmacological agents in rats subjected to a weak, moderate or strong contextual aversive conditioning (CAC) protocol. Antagonizing DH κORs with nor-binaltorphimine (nor-BNI), immediately after, but not 6 h later, a moderate CAC leads to intensified freezing behavior in the re-exposure to the paired context...
February 27, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29496478/non-pharmacological-treatment-affects-neuropeptide-expression-in-neuropathic-pain-model
#11
Fabio Martinez Santos, Joyce Teixeira Silva, Igor Rafael Correia Rocha, Daniel Oliveira Martins, Marucia Chacur
Chronic constriction injury (CCI) of the sciatic nerve elicits changes in neuropeptide expression on the dorsal root ganglia (DRG). The neural mobilization (NM) technique is a noninvasive method that has been proven clinically effective in reducing pain. The aim of this study was to analyze the expression of substance P, transient receptor potential vanilloid 1 (TRPV1) and opioid receptors in the DRG of rats with chronic constriction injury and to compare it to animals that received NM treatment. CCI was performed on adult male rats...
May 15, 2018: Brain Research
https://www.readbyqxmd.com/read/29492614/the-%C3%AE%C2%BA-opioid-receptor-antagonist-jdtic-decreases-ethanol-intake-in-alcohol-preferring-aa-rats
#12
Johanna Uhari-Väänänen, Atso Raasmaja, Pia Bäckström, Ville Oinio, F Ivy Carroll, Mikko Airavaara, Kalervo Kiianmaa, Petteri Piepponen
RATIONALE: Studies suggest that the κ-opioidergic system becomes overactivated as ethanol use disorders develop. Nalmefene, a currently approved treatment for ethanol use disorders, may also elicit some of its main effects via the κ-opioidergic system. However, the exact role of κ-opioid receptors on regulating ethanol intake and contribution to the development of ethanol addiction remains to be elucidated. OBJECTIVES: The aim of the present study was to clarify the role of accumbal κ-opioid receptors in controlling ethanol intake in alcohol-preferring Alko Alcohol (AA) rats...
February 28, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29479731/severe-central-sleep-apnoea-associated-with-nalmefene-a-case-report
#13
Charles Khouri, François Arbib, Bruno Revol, Jean-Louis Pepin, Renaud Tamisier
Nalmefene, an opioid antagonist, has recently been approved for the treatment of alcohol dependence. We describe here the first case of a 52-year-old woman who developed a severe central sleep apnoea (CSA) 5 months after initiation of nalmefene. Scoring of ventilation during sleep recording revealed an apnoea-hypopnoea index of 67/h with 98.7% of central events and an apnoea index of 65/h. Nalmefene was withdrawn and a new polysomnography was performed which concluded that CSA has disappeared. Pathophysiology is still unclear but could involve the κ-opioid receptors...
February 26, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29467000/ginsenoside-re-protects-methamphetamine-induced-dopaminergic-neurotoxicity-in-mice-via-upregulation-of-dynorphin-mediated-%C3%AE%C2%BA-opioid-receptor-and-downregulation-of-substance-p-mediated-neurokinin-1-receptor
#14
Duy-Khanh Dang, Eun-Joo Shin, Dae-Joong Kim, Hai-Quyen Tran, Ji Hoon Jeong, Choon-Gon Jang, Seung-Yeol Nah, Jung Hwan Jeong, Jae Kyung Byun, Sung Kwon Ko, Guoying Bing, Jau-Shyong Hong, Hyoung-Chun Kim
BACKGROUND: We previously reported that ginsenoside Re (GRe) attenuated against methamphetamine (MA)-induced neurotoxicity via anti-inflammatory and antioxidant potentials. We also demonstrated that dynorphin possesses anti-inflammatory and antioxidant potentials against dopaminergic loss, and that balance between dynorphin and substance P is important for dopaminergic neuroprotection. Thus, we examined whether GRe positively affects interactive modulation between dynorphin and substance P against MA neurotoxicity in mice...
February 21, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29441714/time-dependent-regional-brain-distribution-of-methadone-and-naltrexone-in-the-treatment-of-opioid-addiction
#15
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/29430855/dynorphinergic-system-alterations-in-the-corticostriatal-circuitry-of-neuropathic-mice-support-its-role-in-the-negative-affective-component-of-pain
#16
M Palmisano, F F Caputi, D Mercatelli, P Romualdi, S Candeletti
The dynorphinergic system is involved in pain transmission at spinal level, where dynorphin exerts antinociceptive or pronociceptive effects, based on its opioid or non-opioid actions. Surprisingly, little evidence is currently available concerning the supraspinal role of the dynorphinergic system in pain conditions. The present study aimed to investigate whether neuropathic pain is accompanied by prodynorphin (Pdyn) and κ-opioid receptor (Oprk1) gene expression alterations in selected mouse brain areas. To this end, mice were subjected to chronic constriction injury of the right sciatic nerve and neuropathic pain behavioral signs were ascertained after 14 days...
February 12, 2018: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/29427652/evaluating-the-abuse-potential-of-psychedelic-drugs-for-medical-use-in-humans
#17
REVIEW
David J Heal, Jane Gosden, Sharon L Smith
Psychedelics comprise drugs come from various pharmacological classes including 5-HT 2A agonists, indirect 5-HT agonists, e.g. MDMA, NMDA antagonists and κ-opioid receptor agonists. There is resurgence in developing psychedelics to treat psychiatric disorders with high unmet clinical need. Many, but not all, psychedelics are schedule 1 controlled drugs (CDs), i.e. no approved medical use. For existing psychedelics in development, regulatory approval will require a move from schedule 1 to a CD schedule for drugs with medical use, i...
February 7, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29391822/post-marketing-surveillance-study-of-the-safety-and-efficacy-of-nalfurafine-hydrochloride-remitch%C3%A2-capsules-2-5-%C3%AE-g-in-3-762-hemodialysis-patients-with-intractable-pruritus
#18
Hideki Kozono, Hiroshi Yoshitani, Ryoko Nakano
Background: Intractable pruritus in hemodialysis patients can significantly decrease their quality of life and is also associated with poor vital prognosis. Although combined multiple causes of intractable pruritus in these patients have been identified, no existing treatments are proven to be sufficiently effective. We conducted a post-marketing surveillance to follow-up and assess the safety and efficacy of nalfurafine, a selective κ-opioid receptor agonist, for the treatment of intractable pruritus in patients undergoing hemodialysis...
2018: International Journal of Nephrology and Renovascular Disease
https://www.readbyqxmd.com/read/29383684/dynorphin-and-%C3%AE%C2%BA-opioid-receptor-dysregulation-in-the-dopaminergic-reward-system-of-human-alcoholics
#19
Igor Bazov, Daniil Sarkisyan, Olga Kononenko, Hiroyuki Watanabe, Tatiana Yakovleva, Anita C Hansson, Wolfgang H Sommer, Rainer Spanagel, Georgy Bakalkin
Molecular changes induced by excessive alcohol consumption may underlie formation of dysphoric state during acute and protracted alcohol withdrawal which leads to craving and relapse. A main molecular addiction hypothesis is that the upregulation of the dynorphin (DYN)/κ-opioid receptor (KOR) system in the nucleus accumbens (NAc) of alcohol-dependent individuals causes the imbalance in activity of D1- and D2 dopamine receptor (DR) expressing neural circuits that results in dysphoria. We here analyzed post-mortem NAc samples of human alcoholics to assess changes in prodynorphin (PDYN) and KOR (OPRK1) gene expression and co-expression (transcriptionally coordinated) patterns...
January 30, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29379300/the-effects-of-naloxone-on-human-breast-cancer-progression-in-vitro-and-in-vivo-studies-on-mda-mb231-cells
#20
Sabrina Bimonte, Antonio Barbieri, Marco Cascella, Domenica Rea, Giuseppe Palma, Vitale Del Vecchio, Cira Antonietta Forte, Francesco Del Prato, Claudio Arra, Arturo Cuomo
Background: Naloxone is viewed as a specific competitive opioid antagonist acting at the level of opioid receptors (μ, δ, and κ) with blended agonist-adversary or agonist action. The role of naloxone in tumor cell growth has been poorly studied in human cancer cell lines. Materials and methods: In the present study, we report findings from in vitro and in vivo experiments performed to evaluate the effects of naloxone on human breast cancer cell growth and progression...
2018: OncoTargets and Therapy
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