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- Volume 19, Issue 42, 2013
Current Pharmaceutical Design - Volume 19, Issue 42, 2013
Volume 19, Issue 42, 2013
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Opioid Receptor Interacting Proteins and the Control of Opioid Signaling
Authors: Jennifer T. Lamberts and John R. TraynorOpioid receptors are seven-transmembrane domain receptors that couple to intracellular signaling molecules by activating heterotrimeric G proteins. However, the receptor and G protein do not function in isolation but their activities are modulated by several accessory and scaffolding proteins. Examples include arrestins, kinases, and regulators of G protein signaling proteins. Accessory proteins contribute to the observ Read More
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Lack of Regulatory Changes of μ-Opioid Receptors by 14-Methoxymetopon Treatment in Rat Brain. Further Evidence for Functional Selectivity
Authors: Resat Cinar, Orsolya Kekesi, Erika Birkas, Gabriella Fabian, Helmut Schmidhammer and Maria SzucsHere we have studied regulatory changes of μ-opioid receptors accompanying in vivo 14-methoxymetopon treatments of rats. Previously, this ligand has been shown to be an extremely potent, centrally acting μ-opioid specific analgesic with low physical dependence, tolerance, respiratory depression, constipation and other side effects. Our work shows that it is a highly potent full agonist of μ-opioid receptor coupled G-prot Read More
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Microglia Activation Precedes the Anti-Opioid BDNF and NMDA Receptor Mechanisms Underlying Morphine Analgesic Tolerance
Authors: Yosuke Matsushita, Idowu O. Omotuyi, Takehiro Mukae and Hiroshi UedaHerein, we investigated the role of periaqueductal gray (PAG)-resident microglia in the development of morphine tolerance and its underlying mechanisms. We showed that clodronate and minocycline known as microglia inhibitors reversed morphine tolerance, providing proof that microglia activation has key role in the development of morphine tolerance. The microglia-mediated anti-opioid mechanism occurs via s Read More
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Current κ Opioid Receptor Ligands and Discovery of a New Molecular Scaffold as a κ Opioid Receptor Antagonist Using Pharmacophore-Based Virtual Screening
Authors: Mariana Spetea, Muhammad Faheem Asim, Stefan Noha, Gerhard Wolber and Helmut SchmidhammerThe κ opioid receptor (KOR) plays a significant role in many physiological functions, including pain relief, stress, depression, drug abuse, anxiety and psychotic behaviors. KORs are widely distributed in the central and peripheral nervous systems, and are specifically activated by endogenous opioids derived from prodynorphin. They are members of the G protein-coupled receptor superfamily, and the crystal structure of the h Read More
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Opiate-Induced Analgesia: Contributions From Mu, Delta and Kappa Opioid Receptors Mouse Mutants
More LessThe three opioid receptors, mu, delta and kappa all mediate analgesia, and knockout mice with opioid receptor deletion have proven unique tools to investigate in vivo opioid pharmacology. Since a few years, a number of new mouse lines have been engineered, with several distinct mutations of the mu receptor, to assess the role of specific amino acid residues or peptidic sequences of this receptor in analgesia and tolerance. Read More
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Opioid Receptors and Their Ligands in the Musculoskeletal System and Relevance for Pain Control
More LessInterest in opioid drugs like morphine, as the oldest and most potent pain-killing agents known, has been maintained through the years. One of the most frequent chronic pain sensations people experience is associated with pathological conditions of the musculoskeletal system. Chronic musculoskeletal pain is a major health problem, and an adequate management requires understanding of both peripheral and central c Read More
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Functionalization of the Carbonyl Group in Position 6 of Morphinan-6-ones. Development of Novel 6-Amino and 6-Guanidino Substituted 14-Alkoxymorphinans
The well-known opioid agonists, oxycodone and oxymorphone, and the opioid antagonists, naloxone and naltrexone, are commonly used clinical agents and research tools in the opioid field. They belong to the class of morphinan-6-ones, and produce their pharmacological effects by interacting with opioid receptors, i.e. mu (MOR), delta (DOR) and kappa (KOR). The search for potent agonists and antagonists has conti Read More
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Essential Structure of the κ Opioid Receptor Agonist Nalfurafine for Binding to the κ Receptor
Authors: Hiroshi Nagase and Hideaki FujiiThe selective κ opioid receptor agonist nalfurafine was launched in 2009 as an antipruritic drug for patients undergoing hemodialysis. It is the first clinically used compound with high selectivity for the κ opioid receptor. Nalfurafine had a different pharmacological feature from other κ opioid agonists. Nalfurafine induced neither addictive nor aversive effects, whereas other κ agonists such as U- 50,488H or salvinorin A produc Read More
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The μ Opioid Receptor and Ligands Acting at the μ Opioid Receptor, as Therapeutics and Potential Therapeutics
Authors: Mariana Spetea, Muhammad Faheem Asim, Gerhard Wolber and Helmut SchmidhammerAlthough the μ opioid receptor (MOR) was pharmacologically and biochemically identified in binding studies forty years ago, its structure, function, and true complexity only have emerged after its cloning in 1993. Continuous efforts from many laboratories have greatly advanced our understanding of MORs, ranging from their anatomic distribution to cellular and molecular mechanisms, and from cell lines to in vivo sys Read More
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Hybrid Opioid/Non-Opioid Ligands in Pain Research
Authors: Patrycja Kleczkowska, Andrzej W. Lipkowski, Dirk Tourwe and Steven BalletTo address the different types of pain (e.g. acute, chronic, neuropathic) different classes of medications, mainly non-steroidal anti-inflammatory drugs and narcotics (opioids), are used. More specifically, the alleviation or treatment of moderate to severe pain states commonly invokes the use of opioids. Unfortunately, their chronic administration induces various undesirable side effects, such as for example physical dependenc Read More
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The Use of Bifunctional NOP/Mu and NOP Receptor Selective Compounds for the Treatment of Pain, Drug Abuse, and Psychiatric Disorders
More LessThe NOP receptor, the fourth receptor in the opioid receptor family, is found throughout the brain and is involved in a variety of CNS systems and pathways. The endogenous ligand for NOP receptors, nociceptin/orphanin FQ (now called N/OFQ), was originally thought to increase a painful stimulus since intracerebroventricular (i.c.v.) administration of this heptadecapeptide led to a decrease in tail-flick and hot-plate latency Read More
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Tritiated Opioid Receptor Ligands as Radiotracers
Authors: Geza Toth and Jayapal Reddy MallareddyTritiated opioid ligands are essential tools for the identification of opioid receptors. This review deals with the syntheses of tritiated opioid peptide derivatives, including enkephalins, dynorphins, dermorphins, deltorphins and endomorphins, and also discusses tritium-labeled nonpeptide opioids. It additionally focuses on the relevance of tritium-labeled opioid compounds as research tools for investigating opioid receptor pharmac Read More
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Inhibitory Effects of Water Caltrop Pericarps on the Growth of Human Gastric Cancer Cells In Vitro
Authors: Qiusheng Lin, Junhui Shen, Ying Ning, Shengrong Shen and Undurti N. DasWater caltrop is a popular traditional vegetable in China, and its pericarps are always wasted. In the present work reported here, pericarps from three different Chinese water caltrop cultivars were collected and extracted using 70% methanol and hot water. All the extracts contained significant amounts of polyphenols (183.7-201.7 mg GAE/g), flavonoids (34.3-54.6 mg RE/g) and saponins (23.2- 36.3 mg GRE/g). These Read More
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Phase 1 Safety, Tolerability and Pharmacokinetics of 3K3A-APC in Healthy Adult Volunteers
Background and Purpose. Activated Protein C (APC) stimulates multiple cytoprotective pathways via the protease activated receptor-1 (PAR-1) and promotes anticoagulation. 3K3A-APC was designed for preserved activity at PAR-1 with reduced anticoagulation. This Phase 1 trial characterized pharmacokinetics and anticoagulation effects of 3K3A-APC. Methods. Subjects (n=64) were randomly assigned to receive 3K3A-APC (n= Read More
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Volumes & issues
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Volume 31 (2025)
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Volume 30 (2024)
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Volume 29 (2023)
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Volume 28 (2022)
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Volume 27 (2021)
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Volume 26 (2020)
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Volume 25 (2019)
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Volume 24 (2018)
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Volume 23 (2017)
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Volume 22 (2016)
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Volume 21 (2015)
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Volume 20 (2014)
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Volume 19 (2013)
- Issue 42
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- Issue 40
- Issue 39
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- Issue 15
- Issue 28
- Issue 14
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- Issue 1
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Volume 18 (2012)
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Volume 17 (2011)
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Volume 16 (2010)
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Volume 15 (2009)
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Volume 14 (2008)
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Volume 13 (2007)
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Volume 12 (2006)
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Volume 11 (2005)
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Volume 10 (2004)
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Volume 9 (2003)
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Volume 8 (2002)
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Volume 7 (2001)
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Volume 6 (2000)
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