Relevant bibliographies by topics / Opioid ligands

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  1. Journal articles
  2. Dissertations / Theses
  3. Books
  4. Book chapters
  5. Conference papers

Academic literature on the topic 'Opioid ligands'

Author: Grafiati
Published: 4 June 2021
Last updated: 16 February 2022

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Journal articles on the topic "Opioid ligands"

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Faouzi, Abdelfattah, Balazs R. Varga, and Susruta Majumdar. "Biased Opioid Ligands." Molecules 25, no. 18 (2020): 4257. http://dx.doi.org/10.3390/molecules25184257.

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Achieving effective pain management is one of the major challenges associated with modern day medicine. Opioids, such as morphine, have been the reference treatment for moderate to severe acute pain not excluding chronic pain modalities. Opioids act through the opioid receptors, the family of G-protein coupled receptors (GPCRs) that mediate pain relief through both the central and peripheral nervous systems. Four types of opioid receptors have been described, including the μ-opioid receptor (MOR), κ-opioid receptor (KOR), δ-opioid receptor (DOR), and the nociceptin opioid peptide receptor (NOP
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Che, Tao, Hemlata Dwivedi-Agnihotri, Arun K. Shukla, and Bryan L. Roth. "Biased ligands at opioid receptors: Current status and future directions." Science Signaling 14, no. 677 (2021): eaav0320. http://dx.doi.org/10.1126/scisignal.aav0320.

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The opioid crisis represents a major worldwide public health crisis that has accelerated the search for safer and more effective opioids. Over the past few years, the identification of biased opioid ligands capable of eliciting selective functional responses has provided an alternative avenue to develop novel therapeutics without the side effects of current opioid medications. However, whether biased agonism or other pharmacological properties, such as partial agonism (or low efficacy), account for the therapeutic benefits remains questionable. Here, we provide a summary of the current status
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Knapman, Alisa, Marina Santiago, Yan Ping Du, Philip R. Bennallack, Macdonald J. Christie, and Mark Connor. "A Continuous, Fluorescence-based Assay of µ-Opioid Receptor Activation in AtT-20 Cells." Journal of Biomolecular Screening 18, no. 3 (2012): 269–76. http://dx.doi.org/10.1177/1087057112461376.

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Opioids are widely prescribed analgesics, but their use is limited due to development of tolerance and addiction, as well as high variability in individual response. The development of improved opioid analgesics requires high-throughput functional assays to assess large numbers of potential opioid ligands. In this study, we assessed the ability of a proprietary “no-wash” fluorescent membrane potential dye to act as a reporter of µ–opioid receptor (MOR) activation and desensitization via activation of G-protein-coupled inwardly rectifying potassium channels. AtT-20 cells stably expressing mouse
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Root-Bernstein, Churchill, Turke, Subhramanyam, and Labahn. "Mutual Enhancement of Opioid and Adrenergic Receptors by Combinations of Opioids and Adrenergic Ligands Is Reflected in Molecular Complementarity of Ligands: Drug Development Possibilities." International Journal of Molecular Sciences 20, no. 17 (2019): 4137. http://dx.doi.org/10.3390/ijms20174137.

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Crosstalk between opioid and adrenergic receptors is well characterized and due to interactions between second messenger systems, formation of receptor heterodimers, and extracellular allosteric binding regions. Both classes of receptors bind both sets of ligands. We propose here that receptor crosstalk may be mirrored in ligand complementarity. We demonstrate that opioids bind to adrenergic compounds with micromolar affinities. Additionally, adrenergic compounds bind with micromolar affinities to extracellular loops of opioid receptors while opioids bind to extracellular loops of adrenergic r
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Micovic, Vuk, Milovan Ivanovic та Ljiljana Dosen-Micovic. "Structural requirements for ligands of the δ-opioid receptor". Journal of the Serbian Chemical Society 74, № 11 (2009): 1207–17. http://dx.doi.org/10.2298/jsc0911207m.

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The ?-opioid receptor is sensitive to ligand geometry. In order to assist the synthesis of new ?-selective opioid ligands, the structure elements of ?-selective opioid ligands necessary for their effective binding were investigated. The automated docking procedure with a flexible ligand was used to simulate the binding of 17 ?-selective ligands to the ?-receptor. It was found that voluminous N-alkyl groups reduce the binding potency of naltrindole derivatives by preventing the ligands from adopting the preferred conformation in the receptor. This was confirmed by enantiospecific binding of chi
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Gillis, Alexander, Arisbel B. Gondin, Andrea Kliewer, et al. "Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists." Science Signaling 13, no. 625 (2020): eaaz3140. http://dx.doi.org/10.1126/scisignal.aaz3140.

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Biased agonism at G protein–coupled receptors describes the phenomenon whereby some drugs can activate some downstream signaling activities to the relative exclusion of others. Descriptions of biased agonism focusing on the differential engagement of G proteins versus β-arrestins are commonly limited by the small response windows obtained in pathways that are not amplified or are less effectively coupled to receptor engagement, such as β-arrestin recruitment. At the μ-opioid receptor (MOR), G protein–biased ligands have been proposed to induce less constipation and respiratory depressant side
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Husbands, Stephen M. "Kappa-opioid receptor ligands." Expert Opinion on Therapeutic Patents 14, no. 12 (2004): 1725–41. http://dx.doi.org/10.1517/13543776.14.12.1725.

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Sencanski, Milan, Milovan Ivanovic, Sonja Vuckovic та Ljiljana Dosen-Micovic. "Modeling the ligand specific μ- and δ-opioid receptor conformations". Journal of the Serbian Chemical Society 76, № 9 (2011): 1247–62. http://dx.doi.org/10.2298/jsc110120110s.

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An automated docking procedure was applied to study the binding of a series of ?- and ?-selective ligands to ligand-specific ?- and ?-opioid receptor models. Short-time molecular dynamic simulations were used to obtain ligand-specific ?- and ?-opioid receptors from arbitrarily chosen models of the active form of these receptors. The quality of receptor model depended on the molecular volume of the ligand in the receptor-ligand complex used in the molecular dynamic simulations. Within a series of ligands of similar size (volume), the results of ligand docking to the obtained ligand-specific rec
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Kleczkowska, Patrycja, Andrzej Lipkowski, Dirk Tourwe, and Steven Ballet. "Hybrid Opioid/Non-Opioid Ligands in Pain Research." Current Pharmaceutical Design 19, no. 42 (2014): 7435–50. http://dx.doi.org/10.2174/138161281942140105165646.

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Corazziari, Enrico. "Role of Opioid Ligands in the Irritable Bowel Syndrome." Canadian Journal of Gastroenterology 13, suppl a (1999): 71A—75A. http://dx.doi.org/10.1155/1999/598659.

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Endogenous opioid peptides – enkephalins, beta-endorphin and dynorphins – are located in specific sites of the brain, the spinal cord, the autonomic ganglia and the enteric nervous system. Endogenous opioids participate in the regulation of nervous visceral afference and sensitivity as well as of several visceral motor function induced by the central nervous system and through the enteroenteric and the myoenteric reflexes. Their final effect on gut physiology is the net and harmonically balanced result of their binding to mu, delta and kappa opioid receptor subtypes. Exogenous opioid receptor
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Dissertations / Theses on the topic "Opioid ligands"

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McFadyen, Iain James. "Structure-activity relationships of opioid ligands." Thesis, Loughborough University, 1999. https://dspace.lboro.ac.uk/2134/33189.

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There are three different types of opioid receptor, namely mu, delta and kappa. Morphine and related clinically useful analgesics exert their actions through the mu opioid receptor. Such compounds represent a huge structural diversity, including both peptides and alkaloids. Nevertheless, there exists a common pharmacophore comprising two critical features, namely an amine nitrogen and an aromatic ring, usually with a hydroxyl substituent; the spatial relationship between them is also vital.
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Bergström, Jonas. "Opioid ligands and receptors of the joint /." Stockholm, 2006. http://diss.kib.ki.se/2006/91-7140-751-0/.

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Paterson, S. J. "Multiple opioid binding sites and their ligands." Thesis, University of Aberdeen, 1986. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.378093.

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The presence of μ-, δ- and κ-binding sites in homogenates of guinea-pig brain was demonstrated by the use of selective labelling techniques. In saturation experiments, the tritiated ligands [^3H]-[D-Ala^2, MePhe^4, Gly-ol^5]enkephalin, [^3H]-dihydromorphine, [^3H]-morphine and [^3H]-dihydronormorphine labelled only the μ-binding site. The δ-binding site could be labelled selectively with [^3H]-[D-Pen^2, D-Pen^5]enkephalin. However, the less selective δ-ligand, [<sup>3</sup>H]-[D-Ala<sup>2</sup>, D-Leu<sup>5</sup>] enkephalin, could only be used when its μ-binding was blocked with the unlabelle
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Jales, Andrew. "Studies of selective ligands for opioid receptors." Thesis, University of Bristol, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.302154.

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DiMattio, Kelly Marie. "Studies on Ligands of the Kappa Opioid Receptor." Diss., Temple University Libraries, 2016. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/334919.

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Pharmacology<br>Ph.D.<br>This thesis is comprised of three parts. In the first part, we investigated zyklophin, a novel selective short-acting kappa opioid receptor (KOPR) antagonist, and its effects on scratching behaviors in Swiss-Webster mice. We investigated whether zyklophin was able to induce scratching in a dose-dependent fashion, and whether this scratching behavior could be blocked by pretreatment with nor-binaltorphimine (norBNI). We also used KOPR -/- mice to further clarify the role of the KOPR in this behavior. In the second part, we examined the role of the divergent amino acid a
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Lu, Yu. "Ligands for the sigma receptor and the mu-opioid receptor." Diss., Columbia, Mo. : University of Missouri-Columbia, 2007. http://hdl.handle.net/10355/4961.

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Thesis (M.S.)--University of Missouri-Columbia, 2007.<br>The entire dissertation/thesis text is included in the research.pdf file; the official abstract appears in the short.pdf file (which also appears in the research.pdf); a non-technical general description, or public abstract, appears in the public.pdf file. Title from title screen of research.pdf file (viewed on January 4, 2008) Includes bibliographical references.
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Obeng, Samuel. "Design, Synthesis, and Biological Screening of Selective Mu Opioid Receptor Ligands as Potential Treatments for Opioid Addiction." VCU Scholars Compass, 2017. http://scholarscompass.vcu.edu/etd/4771.

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Today, more Americans die each year because of drug overdoses than are killed in motor vehicle accidents. In fact, in 2015, more than 33,000 individuals died due to an overdose of heroin or prescription opioids. Sadly, 40-60 % of patients on current opioid addiction treatment medications relapse. Studies have shown that the addiction/abuse liability of opioids are abolished in mu opioid receptor (MOR) knock-out mice; this indicates that the addiction and abuse liability of opioids are mainly mediated through MOR. Utilizing the “message-address concept”, the our laboratory reported a novel non-
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Kulkarni, Vinod V. "Novel Bifunctional Ligands For Neuropathic Pain: Design and Synthesis of Overlapping Pharmacophores of Opioid and Melanocortin Ligands." Diss., The University of Arizona, 2012. http://hdl.handle.net/10150/228191.

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Biologically many disease states lead to changes in expressed proteins. Therefore, "system changes" that occur must be considered in any treatment for the disease. This new approach to drug design and discovery would be particularly applicable to the diseases that involve adaptive changes in the central nervous system, such as neuropathic pain. There is growing evidence that drugs behave differently in pathological states than in normal states, thus preventing their effectiveness in pathological disease states. Therefore, a new paradigm for drug design is needed. In recent years, the melano
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Patel, Dinesh. "Structural and pharmacological studies of synthetic and endogenous opioid receptor ligands." Thesis, Loughborough University, 1992. https://dspace.lboro.ac.uk/2134/11073.

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The interaction of a diverse set of opioid alkaloids and peptides with various opioid receptors has been examined using biochemical and pharmacological techniques. Structural information on the compounds was obtained from single crystal X-ray diffraction and nuclear magnetic resonance studies, and modelled by computational methods. The introduction of a dithiocarbazate moiety into the 7a-position of a bridged thebaine was shown to afford a degree of μ selectivity in this class of nonselective compounds. X-ray diffraction analysis of this compound and comparison with the structure of [Met5]enke
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Oakley, Sarah M. "The influence of G-protein coupling of the #delta#-opioid receptor on the activity of #delta#-opioid receptor ligands." Thesis, University of Surrey, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.326816.

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Books on the topic "Opioid ligands"

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Ko, Mei-Chuan, and Stephen M. Husbands, eds. Research and Development of Opioid-Related Ligands. American Chemical Society, 2013. http://dx.doi.org/10.1021/bk-2013-1131.

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McFadyen, Iain James. Structure-activity relationships of opioid ligands. 1999.

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Ko, Mei-Chuan, and Stephen M. Husbands. Research and Development of Opioid-Related Ligands. Oxford University Press, Incorporated, 2014.

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Patel, Dinesh. Structural and pharmacological studies of synthetic and endogenous opioid receptor ligands. 1992.

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Bell, Katrina Margaret. A biochemical and pharmacological characterisation of some endogenous and exogenous k opioid ligands. 1994.

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Bonnet, Francis, Marc E. Gentili, and Christophe Aveline. Post-surgical analgesia and acute pain management. Edited by Jonathan G. Hardman. Oxford University Press, 2017. http://dx.doi.org/10.1093/med/9780199642045.003.0046.

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Postoperative and acute pain remains uncontrolled in many instances, leading to the risk of development of chronic pain syndromes. After tissue damage, activation of postsynaptic NMDA receptors, also induced by opioid administration, plays a key role in postoperative pain sensitization, allodynia, and hyperalgesia. Pain intensity may depend on sex, age, anxiety, and genetic factors but in clinical practice, surgical procedure is the main determinant of pain, although pain may vary from one patient to one another. Serial pain measurements are mandatory to assess pain intensity and to guide pain
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Bird, Mark F., and David G. Lambert. Deorphanization of ORL-1/LC132 by reverse pharmacology in two landmark studies. Edited by Paul Farquhar-Smith, Pierre Beaulieu, and Sian Jagger. Oxford University Press, 2018. http://dx.doi.org/10.1093/med/9780198834359.003.0026.

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Deorphanization of ORL-1/LC132 in 1995 by reverse pharmacology in two simultaneously published landmark studies added a new member to the opioid family of G-protein coupled receptors. Meunier and Reinscheid used cells expressing recombinant ORL-1 (human) or LC132 (rat) and the presumed intracellular inhibition of cyclic AMP formation to ‘fish’ for endogenous peptide ligands in rat whole-brain and pig hypothalamic extracts. Both studies reported the isolation of a 17-amino-acid peptide, which was named nociceptin and orphanin FQ by the two authors, respectively. The behaviour of the isolated pe
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Knaggs, Roger D. The molecular structure of the μ‎-opioid receptor. Редактори Paul Farquhar-Smith, Pierre Beaulieu та Sian Jagger. Oxford University Press, 2018. http://dx.doi.org/10.1093/med/9780198834359.003.0038.

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The landmark paper discussed in this chapter describes the crystal structure of the μ‎-opioid receptor (also known as MOP-1). Opioids are some of the oldest known drugs and have been used for over 4,000 years; however, in addition to having beneficial analgesic effects, they are associated with a myriad of side effects that can minimize their use. Although the gene sequences of the opioid receptors were determined in the 1990s it has taken much longer to translate this into visualizing their three-dimensional structure. The μ‎-opioid receptor consists of seven transmembrane α‎-helices that are
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Ferini-Strambi, Luigi, and Sara Marelli. Restless legs syndrome/Willis–Ekbom disease. Edited by Sudhansu Chokroverty, Luigi Ferini-Strambi, and Christopher Kennard. Oxford University Press, 2017. http://dx.doi.org/10.1093/med/9780199682003.003.0024.

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Restless legs syndrome (RLS)/Willis–Ekbom disease (WED), is a common neurological disorder characterized by uncomfortable and unpleasant sensations in the legs, with an urge to move. The general population prevalence has been estimated at approximately 5%. In 1995, the International RLS/WED Study Group established four clinical criteria for RLS/WED diagnosis, and in 2012 introduced a fifth (that symptoms are not due to another medical or behavioral condition) to improve differential diagnosis. Periodic leg movements causing sleep fragmentation may be observed in almost 80% of RLS/WED patients.
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Book chapters on the topic "Opioid ligands"

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Casy, Alan F., and George H. Dewar. "Opioid Ligands." In The Steric Factor in Medicinal Chemistry. Springer US, 1993. http://dx.doi.org/10.1007/978-1-4899-2397-4_13.

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Casy, Alan F., and George H. Dewar. "Opioid Ligands." In The Steric Factor in Medicinal Chemistry. Springer US, 1993. http://dx.doi.org/10.1007/978-1-4899-2397-4_14.

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Anand, Jessica P., and Deanna Montgomery. "Multifunctional Opioid Ligands." In Delta Opioid Receptor Pharmacology and Therapeutic Applications. Springer International Publishing, 2018. http://dx.doi.org/10.1007/164_2018_104.

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Corbett, A. D., S. J. Paterson, and H. W. Kosterlitz. "Selectivity of Ligands for Opioid Receptors." In Opioids. Springer Berlin Heidelberg, 1993. http://dx.doi.org/10.1007/978-3-642-77460-7_26.

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Terenius, Lars. "Opioid Receptors and Their Ligands." In Neuropeptides and Stress. Springer New York, 1989. http://dx.doi.org/10.1007/978-1-4612-3514-9_20.

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McCurdy, Christopher R. "Development of Opioid Receptor Ligands." In Analogue-based Drug Discovery. Wiley-VCH Verlag GmbH & Co. KGaA, 2006. http://dx.doi.org/10.1002/3527608001.ch14.

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Kane, Brian E., Bengt Svensson, and David M. Ferguson. "Molecular Recognition of Opioid Receptor Ligands." In Drug Addiction. Springer New York, 2008. http://dx.doi.org/10.1007/978-0-387-76678-2_34.

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Piñeyro, Graciela. "Functional Selectivity at Opioid Receptors." In Functional Selectivity of G Protein-Coupled Receptor Ligands. Humana Press, 2009. http://dx.doi.org/10.1007/978-1-60327-335-0_12.

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Bhatnagar, Anushree, and Sadashiva Karnik. "Functional Selectivity at Non-Opioid Peptide Receptors." In Functional Selectivity of G Protein-Coupled Receptor Ligands. Humana Press, 2009. http://dx.doi.org/10.1007/978-1-60327-335-0_13.

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M�rki, �., S. Hosztafi, F. �tv�s, H. Schmidhammer, G. T�th, and A. Borsodi. "Opioid Receptor Heterogeneity: The Use of New Ligands." In Basic and Clinical Science of Mental and Addictive Disorders. KARGER, 1997. http://dx.doi.org/10.1159/000059509.

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Conference papers on the topic "Opioid ligands"

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Dzimbova, T., F. Spundzhi, R. Mavrevski та P. Milanov. "Determination of the structural requirements of μ-Opioid receptor ligands with docking". У APPLICATION OF MATHEMATICS IN TECHNICAL AND NATURAL SCIENCES: 12th International On-line Conference for Promoting the Application of Mathematics in Technical and Natural Sciences - AMiTaNS’20. AIP Publishing, 2020. http://dx.doi.org/10.1063/5.0033529.

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Giri, Aswini Kumar, Qiong Xie, Christopher R. Apostol та ін. "Design, Synthesis and Biological Evaluation of Multivalent Ligands with μ/δ Opioid Agonist (μ-preferring) /NK-1 Antagonist Activities". У The Twenty-Third American and the Sixth International Peptide Symposium. Prompt Scientific Publishing, 2013. http://dx.doi.org/10.17952/23aps.2013.048.

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Howells, Richard D., Jyoti Joshi Mundra, Alessandro Howells, Giovanni Howells, Youyi Peng, and William Welsh. "Abstract 5548: Novel small-molecule delta opioid receptor ligands modeled from naltrindole inhibit the proliferation of human U266 multiple myeloma cells." In Proceedings: AACR 104th Annual Meeting 2013; Apr 6-10, 2013; Washington, DC. American Association for Cancer Research, 2013. http://dx.doi.org/10.1158/1538-7445.am2013-5548.

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Ferracane, Michael J., and Jane V. Aldrich. "Opioid Ligand Binding to Opioid Receptors: Insight and Implications for Peptide Design." In The 24th American Peptide Symposium. Prompt Scientific Publishing, 2015. http://dx.doi.org/10.17952/24aps.2015.022.

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M. Neto, Rayol, Bruno Souza, Thais Almeida, Fabíola Nakamura, and Eduardo Nakamura. "Uma Abordagem para Identificação de Entidades Influentes em Eventos Comentados nas Redes Sociais Online." In XIV Simpósio Brasileiro de Sistemas Colaborativos. Sociedade Brasileira de Computação - SBC, 2020. http://dx.doi.org/10.5753/sbsc.2017.9956.

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Redes Sociais Online (RSO) permitem aos usuários compartilhar conteúdo de qualquer tipo. Nestas redes, os usuários podem ser vistos como sensores sociais, onde suas opini˜oes e comentários a respeito de um evento podem ser utilizados para estudo (e.g., caracterização de eventos, reconhecimento de entidades influentes). RSO podem ser modeladas como redes complexas, onde as entidades são representadas pelos vértices e as arestas caracterizam a conexão entra elas. Utilizando esta abordagem, podemos determinar quais são as entidades mais influentes no contexto estudado através de medidas de centra
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