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https://www.readbyqxmd.com/read/29441714/time-dependent-regional-brain-distribution-of-methadone-and-naltrexone-in-the-treatment-of-opioid-addiction
#1
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-supports-its-role-in-the-negative-affective-component-of-pain
#2
Palmisano Martina, Caputi Francesca Felicia, Mercatelli Daniela, Romualdi Patrizia, Candeletti Sanzio
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
#3
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
#4
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
#5
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
#6
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
https://www.readbyqxmd.com/read/29367258/identifying-functional-hotspot-residues-for-biased-ligand-design-in-g-protein-coupled-receptors
#7
Anita Nivedha, Christofer Tautermann, Supriyo Bhattacharya, Sangbae Lee, Paola Casarosa, Ines Kollak, Tobias Kiechle, Nagarajan Vaidehi
G-protein-coupled receptors (GPCRs) mediate multiple signaling pathways in the cell depending on the agonist that activates the receptor and multiple cellular factors. Agonists that show higher potency to specific signaling pathways over others are known as "biased agonists" and have been shown to have better therapeutic index. Although biased agonists are desirable, their design poses several challenges to date. The number of assays to identify biased agonists seems expensive and tedious. Therefore, computational methods that can reliably calculate the possible bias of various ligands ahead of experiments and provide guidance will be both cost and time effective...
January 24, 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29361112/what-is-new-in-pain-modification-in-osteoarthritis
#8
Rachel E Miller, Joel A Block, Anne-Marie Malfait
There is a big need for the development of novel therapies for the safe management of chronic pain associated with OA. Here we reviewed PubMed (2015 onward) and ClinicalTrials.gov for ongoing and recently completed trials where pain in OA is the primary outcome measure. Three broad categories were identified: biological therapies, small molecules and cryoneurolysis. The most promising new strategy is blockade of nerve growth factor with antibodies. Two anti-nerve growth factor antibodies, tanuzemab and fasinumab, are in active development after the 2010 hold on trials was lifted in 2015...
January 17, 2018: Rheumatology
https://www.readbyqxmd.com/read/29354941/-new-thoughts-in-mechanism-research-of-acupuncture-for-myocardial-stunning-from-%C3%AE%C2%BA-opioid-receptor-signaling-pathway
#9
Yuanyuan Wang, Qun Liu, Fengyan Lu, Juanjuan Xin, Qiufu Dai, Shuyang Wu, Yuxue Zhao, Junhong Gao, Xiaochun Yu
By reviewing the literature regarding the development mechanism of myocardial stunning, effects of acupuncture on myocardial ischemic injury, and correlation between acupuncture and κ-opioid receptor, it was suggested that acupuncture was highly likely to act on κ-opioid receptor in myocardial cells, and directly treated myocardial malfunction induced by myocardial stunning through κ-opioid receptor and its signaling pathway. In addition, acupuncture could inhabit the signaling pathway of adrenoceptor β1, one of the main functional receptors, to indirectly improve myocardial ischemic injury...
January 12, 2018: Zhongguo Zhen Jiu, Chinese Acupuncture & Moxibustion
https://www.readbyqxmd.com/read/29342943/the-peptide-pnpp-19-a-spider-toxin-derivative-activates-%C3%AE-opioid-receptors-and-modulates-calcium-channels
#10
Ana C N Freitas, Steve Peigneur, Flávio H P Macedo, José E Menezes-Filho, Paul Millns, Liciane F Medeiros, Maria A Arruda, Jader Cruz, Nicholas D Holliday, Jan Tytgat, Gareth Hathway, Maria E de Lima
The synthetic peptide PnPP-19 comprehends 19 amino acid residues and it represents part of the primary structure of the toxin δ-CNTX-Pn1c (PnTx2-6), isolated from the venom of the spider Phoneutria nigriventer. Behavioural tests suggest that PnPP-19 induces antinociception by activation of CB1, μ and δ opioid receptors. Since the peripheral and central antinociception induced by PnPP-19 involves opioid activation, the aim of this work was to identify whether this synthetic peptide could directly activate opioid receptors and investigate the subtype selectivity for μ-, δ- and/or κ-opioid receptors...
January 15, 2018: Toxins
https://www.readbyqxmd.com/read/29311142/regulation-of-lateral-hypothalamic-orexin-activity-by-local-gabaergic-neurons
#11
Loris L Ferrari, Daniel Park, Lin Zhu, Matthew R Palmer, Rebecca Y Broadhurst, Elda Arrigoni
Orexin (also known as hypocretin) neurons are considered a key component of the ascending arousal system. They are active during wakefulness, at which time they drive and maintain arousal, and are silent during sleep. Their activity is controlled by long-range inputs from many sources, as well as by more short-range inputs, including from presumptive GABAergic neurons in the lateral hypothalamus/perifornical region (LH/PF). To characterize local GABAergic input to orexin neurons we employed channelrhodopsin-2 (ChR2)-assisted-circuit-mapping in brain slices...
January 8, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29296674/dynamic-strategic-bond-analysis-yields-a-ten-step-synthesis-of-20-nor-salvinorin-a-a-potent-%C3%AE%C2%BA-or-agonist
#12
Jeremy J Roach, Yusuke Sasano, Cullen L Schmid, Saheem Zaidi, Vsevolod Katritch, Raymond C Stevens, Laura M Bohn, Ryan A Shenvi
Salvinorin A (SalA) is a plant metabolite that agonizes the human kappa-opioid receptor (κ-OR) with high affinity and high selectivity over mu- and delta-opioid receptors. Its therapeutic potential has stimulated extensive semisynthetic studies and total synthesis campaigns. However, structural modification of SalA has been complicated by its instability, and efficient total synthesis has been frustrated by its dense, complex architecture. Treatment of strategic bonds in SalA as dynamic and dependent on structural perturbation enabled the identification of an efficient retrosynthetic pathway...
December 27, 2017: ACS Central Science
https://www.readbyqxmd.com/read/29273415/design-synthesis-and-opioid-activity-of-arodyn-analogs-cyclized-by-ring-closing-metathesis-involving-tyr-allyl
#13
Wei-Jie Fang, Thomas F Murray, Jane V Aldrich
Kappa (κ) opioid receptor selective antagonists are useful pharmacological tools in studying κ opioid receptors and have potential to be used as therapeutic agents for the treatment of a variety of diseases including mood disorders and drug addiction. Arodyn (Ac[Phe1-3,Arg4,d-Ala8]Dyn A-(1-11)NH2) is a linear acetylated dynorphin A (Dyn A) analog that is a potent and selective κ opioid receptor antagonist (Bennett et al. J Med Chem 2002;45:5617-5619) and prevents stress-induced reinstatement of cocaine-seeking behavior following central administration (Carey et al...
November 21, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29233847/pharmacological-evidence-for-a-putative-conserved-allosteric-site-on-opioid-receptors
#14
Kathryn E Livingston, M Alexander Stanczyk, Neil Burford, Andrew Alt, Merixtell Canals, John R Traynor
Allosteric modulators of G protein-coupled receptors (GPCRs), including opioid receptors, have been proposed as possible therapeutic agents with enhanced selectivity. BMS-986122 is a positive allosteric modulator (PAM) of the mu-opioid receptor (μ-OR). BMS-986187 is a structurally distinct PAM for the delta-opioid receptor (δ-OR) that has been reported to show 100-fold selectivity in promoting δ-OR over μ-OR agonism. Here we use ligand binding and second messenger assays to show that BMS-986187 is actually an effective PAM at μ-OR and at the kappa opioid receptor (κ-OR), but is ineffective at the nociceptin receptor (NOPR)...
December 12, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29224002/the-protective-effects-of-%C3%AE-opioid-receptor-stimulation-in-hypoxic-pulmonary-hypertension-involve-inhibition-of-autophagy-through-the-ampk-mtor-pathway
#15
Yaguang Zhou, Yuanbo Wang, Xu Wang, Xin Tian, Shumiao Zhang, Fan Yang, Haitao Guo, Rong Fan, Na Feng, Min Jia, Xiaoming Gu, Yuemin Wang, Juan Li, Jianming Pei
BACKGROUND/AIMS: In a previous study, we showed that κ-opioid receptor stimulation with the selective agonist U50,488H ameliorated hypoxic pulmonary hypertension (HPH). However, the roles that pulmonary arterial smooth muscle cell (PASMC) proliferation, apoptosis, and autophagy play in κ-opioid receptor-mediated protection against HPH are still unknown. The goal of the present study was to investigate the role of autophagy in U50,488H-induced HPH protection and the underlying mechanisms...
December 8, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29202454/fentanyl-related-designer-drugs-w-18-and-w-15-lack-appreciable-opioid-activity-in-vitro-and-in-vivo
#16
Xi-Ping Huang, Tao Che, Thomas J Mangano, Valerie Le Rouzic, Ying-Xian Pan, Michael D Cameron, Michael H Baumann, Gavril W Pasternak, Bryan L Roth
W-18 (4-chloro-N-[1-[2-(4-nitrophenyl)ethyl]-2-piperidinylidene]-benzenesulfonamide) and W-15 (4-chloro-N-[1-(2-phenylethyl)-2-piperidinylidene]-benzenesulfonamide) represent two emerging drugs of abuse chemically related to the potent opioid agonist fentanyl (N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylpropanamide). Here, we describe the comprehensive pharmacological profiles of W-18 and W-15, as examination of their structural features predicted that they might lack opioid activity. We found W-18 and W-15 to be without detectible activity at μ, δ, κ, and nociception opioid receptors in a variety of assays...
November 16, 2017: JCI Insight
https://www.readbyqxmd.com/read/29174974/m-trifluoromethyl-diphenyl-diselenide-promotes-resilience-to-social-avoidance-induced-by-social-defeat-stress-in-mice-contribution-of-opioid-receptors-and-mapks
#17
Suzan Gonçalves Rosa, Ana Paula Pesarico, Cristina Wayne Nogueira
Depressive symptoms precipitated by stress are prevalent in population. In experimental models of social stress, endogenous opioids mediate different aspects of defensive and submissive behaviors. The present study investigated the opioid receptors, mitogen-activated protein kinase (MAPKs) and protein kinase B (Akt) contribution to m-trifluoromethyl-diphenyl diselenide [(m-CF3-PhSe)2] effects on social avoidance induced by social defeat stress (SDS). Adult Swiss mice were subjected to SDS and treated with (m-CF3-PhSe)2 (5 to 25mg/kg) for 7days...
November 23, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29131554/the-pathophysiology-incidence-impact-and-treatment-of-opioid-induced-nausea-and-vomiting
#18
Theresa Mallick-Searle, Mechele Fillman
PURPOSE: Opioid medications are integral in managing acute moderate-to-severe pain. Opioid analgesics bind to μ (mu), κ (kappa), or δ (delta) opioid receptors in the brain, spinal cord, and digestive tract. However, opioids cause adverse effects that may interfere with their therapeutic use. Some adverse effects wane over time, but patients using opioids for acute pain struggle with opioid-induced nausea and vomiting (OINV) the entire time they take the opioid. This article discusses the underlying mechanisms, clinical implications, and treatment strategies of OINV...
November 2017: Journal of the American Association of Nurse Practitioners
https://www.readbyqxmd.com/read/29121571/high-throughput-%C3%AE-spe-based-elution-coupled-with-uplc-ms-ms-for-determination-of-eluxadoline-in-plasma-sample-application-in-pharmacokinetic-characterization-of-plga-nanoparticle-formulations-in-rats
#19
Muzaffar Iqbal, Essam Ezzeldin, Khalid A Al-Rashood, Ramadan Al-Shdefat, Md Khalid Anwer
Eluxadoline is a novel μ- and κ-opioid receptor (OR) agonist and δ-OR antagonist, recently approved as a first line therapy for the treatment of irritable bowel syndrome. Due to abuse potential, poor bioavailability and high intersubject variability, a sensitive and reliable assay is prerequisite for its determination in biological samples. This work first time report the development and validation of UPLC-MS/MS assay for determination of eluxadoline in rat plasma sample using risperidone as an internal standard (IS)...
October 28, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29119401/role-of-endogenous-agonists-of-opioid-receptors-in-the-regulation-of-heart-resistance-to-postischemic-reperfusion-injury
#20
A S Gorbunov, O E Vaizova, M V Belousov, S V Pozdnyakova, E A Nesterov, P G Madonov
Intravenous injection of nonselective antagonists of opioid receptors (OR) naltrexone (5 mg/kg) and naloxone methiodide (5 mg/kg), selective δ1-OR antagonist BNTX (0.7 mg/kg), selective δ2-OR blocker naltriben (0.3 mg/kg), selective κ-OR antagonist norbinaltorphimine (2 mg/kg), and selective blocker of ORL1 opioid receptors JTC-801 (0.1 mg/kg) produced no effect on reperfusion injury to the heart in rats narcotized with α-chloralose. In contrast, selective μ-OR antagonist CTAP (1 mg/kg) limited the infarct size, although this effect was not observed at a lower CTAP concentration of 0...
November 9, 2017: Bulletin of Experimental Biology and Medicine
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