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Ligands For The Sigma Receptor And The Mu Opioid Receptor
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Book Synopsis Ligands for the Sigma Receptor and the Mu-opioid Receptor by : Yu Lu
Download or read book Ligands for the Sigma Receptor and the Mu-opioid Receptor written by Yu Lu and published by . This book was released on 2007 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: The sigma receptor is a unique receptor family with two subtypes: sigma-1 and sigma-2. In order to conduct structure-activity relationship studies (SAR), a series of specific 1-phenylpropyl-4-benzylpiperidine and 1-phenylpropyl-4- benzylpiperazine analogues were synthesized as sigma ligands. Sigma receptors binding assays were conducted for the piperidine analogues. The last chapter is concerned with the opioid receptors, which have three subtypes: mu, delta, and kappa. The [mu]-opioid receptor is believed to be the subtype with the most clinical importance. In order to obtain [mu]-opioid tetrapeptide ligand I-Dmt-D-Ala-Phe-Orn-NH2 with high affinity and proper lipophilicity, mono-iodination reaction was studied on the 2,6-dimethyl-L-tyrosine residue.
Book Synopsis Opioid Receptors—Advances in Research and Application: 2013 Edition by :
Download or read book Opioid Receptors—Advances in Research and Application: 2013 Edition written by and published by ScholarlyEditions. This book was released on 2013-06-21 with total page 181 pages. Available in PDF, EPUB and Kindle. Book excerpt: Opioid Receptors—Advances in Research and Application: 2013 Edition is a ScholarlyEditions™ book that delivers timely, authoritative, and comprehensive information about kappa Opioid Receptors. The editors have built Opioid Receptors—Advances in Research and Application: 2013 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about kappa Opioid Receptors in this book to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of Opioid Receptors—Advances in Research and Application: 2013 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.
Book Synopsis Opioid Receptors—Advances in Research and Application: 2012 Edition by :
Download or read book Opioid Receptors—Advances in Research and Application: 2012 Edition written by and published by ScholarlyEditions. This book was released on 2012-12-26 with total page 179 pages. Available in PDF, EPUB and Kindle. Book excerpt: Opioid Receptors—Advances in Research and Application: 2012 Edition is a ScholarlyEditions™ eBook that delivers timely, authoritative, and comprehensive information about Opioid Receptors. The editors have built Opioid Receptors—Advances in Research and Application: 2012 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about Opioid Receptors in this eBook to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of Opioid Receptors—Advances in Research and Application: 2012 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.
Book Synopsis Sigma Receptors: Their Role in Disease and as Therapeutic Targets by : Sylvia B. Smith
Download or read book Sigma Receptors: Their Role in Disease and as Therapeutic Targets written by Sylvia B. Smith and published by Springer. This book was released on 2017-03-16 with total page 311 pages. Available in PDF, EPUB and Kindle. Book excerpt: Originally confused with opioid receptors and then orphan receptors with no biological function, Sigma Receptors are now recognized as relevant to many degenerative diseases with remarkable potential as therapeutic targets. In this text, new information about the structure of sigma 1 receptor, its binding sites are provided as well as its expression in many cell types. It’s putative role in degenerative neuronal diseases including amyotrophic lateral sclerosis, Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, pain, drug addiction and locomotor activity. Their roles in possible treatments for blinding retinal diseases emphasize the tremendous far-reaching potential for ligands for these receptors. Exciting breakthroughs in this dynamic field in the last decade are reported herein, which will guide future investigators in determining the full potential of this unique, yet abundantly expressed protein.
Book Synopsis Opioid Receptors: Advances in Research and Application: 2011 Edition by :
Download or read book Opioid Receptors: Advances in Research and Application: 2011 Edition written by and published by ScholarlyEditions. This book was released on 2012-01-09 with total page 104 pages. Available in PDF, EPUB and Kindle. Book excerpt: Opioid Receptors: Advances in Research and Application: 2011 Edition is a ScholarlyEditions™ eBook that delivers timely, authoritative, and comprehensive information about Opioid Receptors. The editors have built Opioid Receptors: Advances in Research and Application: 2011 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about Opioid Receptors in this eBook to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of Opioid Receptors: Advances in Research and Application: 2011 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.
Book Synopsis Ligand-induced Trafficking of Mu and Delta Opioid Receptors by : Paulette Adel Zaki
Download or read book Ligand-induced Trafficking of Mu and Delta Opioid Receptors written by Paulette Adel Zaki and published by . This book was released on 2000 with total page 374 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis The Essence of Analgesia and Analgesics by : Raymond S. Sinatra
Download or read book The Essence of Analgesia and Analgesics written by Raymond S. Sinatra and published by Cambridge University Press. This book was released on 2010-10-14 with total page 551 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Essence of Analgesia and Analgesics is an invaluable practical resource for clinicians giving pain relief in any clinical setting, describing the pharmacologic principles and clinical use of all available pain medications. As well as detailed overviews of pain processing and analgesic theory, sections are dedicated to oral and panteral opioid analgesics, neuraxial opioids, NSAIDs, local anesthetics, anticonvulsant type analgesics, NMDA antagonists, alpha adrenergic analgesics, antidepressant analgesics, muscle relaxants, adjuvant medications, and new and emerging analgesics. The concise format of the chapters allows for quick and easy reading and assimilation of information. Enhanced by summary tables and figures, each chapter provides an overview of a particular drug, covering chemical structure, mode of activity, indications, contraindications, common doses and uses, advantages and disadvantages, and drug related adverse events. Key references are also provided. Edited by leading experts in pain management, this is essential reading for any clinician involved in pain management.
Book Synopsis Design, Synthesis and Pharmacological Characterization of Potential Mu Opioid Receptor Selective Ligands by : Abhishek S. Kulkarni
Download or read book Design, Synthesis and Pharmacological Characterization of Potential Mu Opioid Receptor Selective Ligands written by Abhishek S. Kulkarni and published by . This book was released on 2019 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis The Neuroscience of Cocaine by : Victor R Preedy
Download or read book The Neuroscience of Cocaine written by Victor R Preedy and published by Academic Press. This book was released on 2017-05-23 with total page 776 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Neuroscience of Cocaine: Mechanisms and Treatment explores the complex effects of this drug, addressing the neurobiology behind cocaine use and the psychosocial and behavioral factors that impact cocaine use and abuse. This book provides researchers with an up-to-date understanding of the mechanisms behind cocaine use, and aids them in deriving new pharmacological compounds and therapeutic regimens to treat dependency and withdrawal symptoms. Cocaine is one of the most highly abused illicit drugs worldwide and is frequently associated with other forms of drug addiction and misuse, but researchers are still struggling to understand cocaine’s neuropharmacological profile and the mechanisms of its effects and manifestations at the cognitive level. Cessation of cocaine use can lead to numerous adverse withdrawal conditions, from the cellular and molecular level to the behavioral level of the individual user. Written by worldwide experts in cocaine addiction, this book assists neuroscientists and other addiction researchers in unraveling the many complex facets of cocaine use and abuse. Contains in each chapter an abstract, key facts, mini dictionary of terms, and summary points to aid in understanding Illustrated in full color Provides unique full coverage of all aspects of cocaine and its related pathology Provides researchers with an up-to-date understanding of the mechanisms behind cocaine use, and aids them in deriving new pharmacological compounds and therapeutic regimens to treat dependency and withdrawal symptoms
Book Synopsis Imaging of the Human Brain in Health and Disease by : Philip Seeman
Download or read book Imaging of the Human Brain in Health and Disease written by Philip Seeman and published by Elsevier. This book was released on 2013-11-15 with total page 534 pages. Available in PDF, EPUB and Kindle. Book excerpt: Brain imaging technology remains at the forefront of advances in both our understanding of the brain and our ability to diagnose and treat brain disease and disorders. Imaging of the Human Brain in Health and Disease examines the localization of neurotransmitter receptors in the nervous system of normal, healthy humans and compares that with humans who are suffering from various neurologic diseases. Opening chapters introduce the basic science of imaging neurotransmitters, including sigma, acetylcholine, opioid, and dopamine receptors. Imaging the healthy and diseased brain includes brain imaging of anger, pain, autism, the release of dopamine, the impact of cannabinoids, and Alzheimer's disease. This book is a valuable companion to a wide range of scholars, students, and researchers in neuroscience, clinical neurology, and psychiatry, and provides a detailed introduction to the application of advanced imaging to the treatment of brain disorders and disease. - A focused introduction to imaging healthy and diseased brains - Focuses on the primary neurotransmitter release - Includes sigma, acetylcholine, opioid, and dopamine receptors - Presents the imaging of healthy and diseased brains via anger, pain, autism, and Alzheimer's disease
Book Synopsis Combinatorial Library by : Lisa B. English
Download or read book Combinatorial Library written by Lisa B. English and published by Springer Science & Business Media. This book was released on 2008-02-04 with total page 380 pages. Available in PDF, EPUB and Kindle. Book excerpt: The continued successes of large- and small-scale genome sequencing projects are increasing the number of genomic targets available for drug d- covery at an exponential rate. In addition, a better understanding of molecular mechanisms—such as apoptosis, signal transduction, telomere control of ch- mosomes, cytoskeletal development, modulation of stress-related proteins, and cell surface display of antigens by the major histocompatibility complex m- ecules—has improved the probability of identifying the most promising genomic targets to counteract disease. As a result, developing and optimizing lead candidates for these targets and rapidly moving them into clinical trials is now a critical juncture in pharmaceutical research. Recent advances in com- natorial library synthesis, purification, and analysis techniques are not only increasing the numbers of compounds that can be tested against each specific genomic target, but are also speeding and improving the overall processes of lead discovery and optimization. There are two main approaches to combinatorial library production: p- allel chemical synthesis and split-and-mix chemical synthesis. These approaches can utilize solid- or solution-based synthetic methods, alone or in combination, although the majority of combinatorial library synthesis is still done on solid support. In a parallel synthesis, all the products are assembled separately in their own reaction vessels or microtiter plates. The array of rows and columns enables researchers to organize the building blocks to be c- bined, and provides an easy way to identify compounds in a particular well.
Book Synopsis Nonclinical Assessment of Abuse Potential for New Pharmaceuticals by : Carrie Markgraf
Download or read book Nonclinical Assessment of Abuse Potential for New Pharmaceuticals written by Carrie Markgraf and published by Academic Press. This book was released on 2015-07-14 with total page 321 pages. Available in PDF, EPUB and Kindle. Book excerpt: Nonclinical Assessment of Abuse Potential for New Pharmaceuticals offers a complete reference on the current international regulatory guidelines and details best practice methodology for the three standard animal models used to evaluate abuse potential: physical dependence, self-administration and drug discrimination. This book also includes chapters on alternative models and examples of when you should use these alternatives. Case histories are provided at the end of the book to show how the data generated from the animal models play a pivitol role in the submission package for a new drug. By incorporating all of this information into one book, Nonclinical Assessment of Abuse Potential for New Pharmaceuticals is your single resource for everything you need to know to understand and implement the assessment of abuse liability. Provides a consolidated overview of the complex regulatory landscape Offers best practice methodology for conducting animal studies, including selection of doses and positive control agents that will help you improve your own abuse potential studies Includes real-life examples to illustrate how nonclinical data fit into the submission strategy
Book Synopsis Fundamentals of Anaesthesia by : Colin Pinnock
Download or read book Fundamentals of Anaesthesia written by Colin Pinnock and published by Cambridge University Press. This book was released on 2002-12 with total page 990 pages. Available in PDF, EPUB and Kindle. Book excerpt: The second edition of Fundamentals of Anaesthesia builds upon the success of the first edition, and encapsulates the modern practice of anaesthesia in a single volume. Written and edited by a team of expert contributors, it provides a comprehensive but easily readable account of all of the information required by the FRCA Primary examination candidate and has been expanded to include more detail on all topics and to include new topics now covered in the examination. As with the previous edition, presentation of information is clear and concise, with the use of lists, tables, summary boxes and line illustrations where necessary to highlight important information and aid the understanding of complex topics. Great care has been taken to ensure an unrivalled consistency of style and presentation throughout.
Book Synopsis Antipsychotic Drugs and Their Side-Effects by : Thomas R.E. Barnes
Download or read book Antipsychotic Drugs and Their Side-Effects written by Thomas R.E. Barnes and published by Academic Press. This book was released on 2013-10-22 with total page 304 pages. Available in PDF, EPUB and Kindle. Book excerpt: In line with other volumes in the Neuroscience Perspectives Series, this volume covers the background, pharmacology, molecular biology, and biochemistry of antipsychotic drugs, together with an overview assessment of the therapeutic considerations. Over the past 40 years, the effectiveness of conventional neuroleptic agents for psychotic illness has been offset by a wide range of adverse side-effects, including motor side-effects like parkinsonism. Studies show that lowering doses may still produce the antipsychotic effect while lessening the risk of side-effects. As all available antispychotic drugs are able to block dopamine, specifically D2 receptors, doses below the threshold level for producing acute motor disorder can still be therapeutically effective. With the identification and characterization of multiple dopamine receptors, the possibility of more selective drugs with better side-effect potential has arisen. Other novel antipsychotic agents include D1 receptor blockers, partial dopamine agonists and non-dopamine drugs such as 5-HT receptor blockers, sigma receptor antagonists and NMDA receptor agonists. This volume reviews both the basic science of the conventional and atypical neuroleptics and their present and potential therapeutic use.
Book Synopsis Characterization of the Interactions of Mu and Delta Opioid Receptor Ligands by : Ronald W. Barrett
Download or read book Characterization of the Interactions of Mu and Delta Opioid Receptor Ligands written by Ronald W. Barrett and published by . This book was released on 1983 with total page 336 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Design, Synthesis, and Biological Screening of Selective Mu Opioid Receptor Ligands as Potential Treatments for Opioid Addiction by : Samuel Obeng
Download or read book Design, Synthesis, and Biological Screening of Selective Mu Opioid Receptor Ligands as Potential Treatments for Opioid Addiction written by Samuel Obeng and published by . This book was released on 2017 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: 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-peptide, reversible MOR selective ligand 17-cyclopropylmethyl-3,14[beta]-dihydroxy-4,5[alpha]-epoxy-6[alpha] (isoquinoline-3-carboxamido)morphinan (NAQ). Molecular modeling and mutagenesis studies revealed that the selectivity of NAQ for MOR is because of the [pi]-[pi] stacking of the isoquinoline ring of NAQ with W318. Therefore, other heterocyclic ring systems were explored to obtain a diverse library of compounds with similar or different molecular interactions and pharmacologic characteristics as NAQ. The newly designed compounds were indole analogs of 6[alpha]/[beta]-naltrexamine. The compounds were synthesized and the affinity and selectivity for MOR determined using the radioligand binding assay while the functional activity at MOR was determined using the [35S]GTP[gamma]S binding assay. The indole analog of 6[alpha]-naltrexamine substituted at position 7 (compound 6) was found to be very potent and had the lowest efficacy in the [35S]GTP[gamma]S functional assay while the indole analog of 6[alpha]-naltrexamine substituted at position 2 (compound 10) was identified as a MOR agonist and had the greatest efficacy. In vivo studies were conducted using the warm-water immersion assay to find whether the synthesized compounds had antinociceptive effects and/or blocked the antinociceptive effects of morphine. Not surprisingly, compound 10 was identified as an opioid agonist while compound 6 almost completely blocked morphine's antinociceptive effects. The opioid antagonist effect of compound 6 was found to be dose dependent with an AD50 of 2.39 mg/kg (0.46-12.47). An opioid withdrawal assay was conducted on compound 6 using morphine-pelleted mice. Compound 6 produced significantly less withdrawal symptoms at 50 mg/kg than naltrexone at 1 mg/kg. Therefore, compound 6 has the potential to be used in opioid addiction and withdrawal treatment.
Book Synopsis Opioids and Their Receptors by : Mariana Spetea
Download or read book Opioids and Their Receptors written by Mariana Spetea and published by MDPI. This book was released on 2020-12-18 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistry and pharmacology of new ligands targeting the opioid receptors as effective and safe therapeutics for human diseases. Furthermore, it draws a special attention to advancing concepts and strategies in opioid drug discovery to mitigate opioid liabilities. The diversity among the discussed topics is a testimony to the complexity of the opioid system, which results from the expression, regulation, and functional role of ligands and receptors. The array of multidisciplinary research areas illustrates the rapidly developing basic research and translational activities in opioid drug discovery. This book will serve as a useful reference while also stimulating continued research in the chemistry and pharmacology of opioids and their receptors, with the prospect of developing improved therapies for human diseases, but also improving health and quality of life in general.
