Research and Development of Opioid-Related Ligands
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Research and Development of Opioid-Related Ligands: (1131 ACS Symposium Series)

Research and Development of Opioid-Related Ligands: (1131 ACS Symposium Series)


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About the Book

Research in the opioid field continues apace, with ongoing developments in our understanding of the underlying biology through to the clinical consequences of modulating opioid receptors. The sheer volume of research being carried out in this field precludes a thorough bench-to-bedside review and has necessitated a somewhat focused approach within this volume, in particular the use and potential uses of ligands that activate one, or more, of the receptors. Contributions to Research and Development of Opioid-Related Ligands include chapters describing current research into the main clinical uses of opioids, analgesia and opioid abuse treatment, as well as what the editors consider to be key areas of pre-clinical development. Not surprisingly the identification of a fourth opioid-like receptor, the NOP receptor, has provided the stimulus for many studies with the aim of determining the potential therapeutic value of modulating the activity of this receptor. A number of chapters within this volume reflect the current interest in this new member of the family. The 16 chapters of Research and Development of Opioid-Related Ligands are arranged into 5 themes, starting with the clinical studies of pain and opioid abuse treatment and followed by chapters on new ligand development, novel assays and concepts, classical opioid pharmacology and NOP receptor pharmacology. An emphasis is placed on translational science and how our increased knowledge may lead to new medicines. The development and use of ligands selective for one receptor or another continues to be of substantial interest, and indeed, the availability of such ligands has allowed the pharmacology of the NOP receptor to be studied in detail from soon after its discovery. Interestingly, ligands induce distinct receptor conformations and produce different signaling cascades, indicating that ligand-directed signaling or biased agonism may have important therapeutic implications. In addition we have now reached a point where selectively promiscuous ligands (ligands that bind to more than one receptor but with defined efficacy at each) can be designed. The rationale for, and progress in, targeting such ligands is made in a number of the chapters.

Table of Contents:
Preface .............................................................................................................................. xi Commentaries 1. Commentary on the Current Status of Clinically Used Analgesics ..................... 3 Thomas M. Dodds 2. Commentary on the Current State of Opioid-Related Research ......................... 5 John W. Lewis Clinical Studies of Pain and Opioids 3. The Clinical Importance of Conditioning Pain Modulation: A Review and Clinical Implications ................................................................................................ 9 Mellar P. Davis 4. Treatment of Pain and Opioid Abuse ................................................................... 39 Shanthi Mogali and Sandra D. Comer 5. Treatment of Opioid Dependence ......................................................................... 61 Andrew J. Saxon 6. Buprenorphine in the Treatment of Neuropathic Pain ..................................... 103 Guy H. Hans Development of New Ligands 7. Buprenorphine and Related Orvinols ................................................................ 127 Stephen M. Husbands 8. Structure-Activity Relationships of Nociceptin Receptor (NOP) Ligands and the Design of Bifunctional NOP/Mu Opioid Receptor-Targeted Ligands .................................................................................................................. 145 Nurulain T. Zaveri, Dennis Yasuda, Blair V. Journigan, Pankaj R. Daga, Faming Jiang, and Cris Olsen Novel Assays and Concepts 9. Mu, Delta and Kappa Opioid Agonist Effects In Novel Assays of Pain-Depressed Behavior .................................................................................... 163 S. Stevens Negus and Ahmad A. Altarifi 10. Functionally Biased Agonism of Mu and Kappa Opioid Receptors ............... 177 Donald J. Kyle Pharmacology of Classical Opioid Receptors 11. Peripherally Restricted Opioid Analgesics ........................................................ 201 Patrick J. Little 12. The Delta Opioid Receptor .................................................................................. 223 A. M. Symons-Liguori and T. W. Vanderah 13. Kappa Opioids: Problems and Opportunities in Analgesia ............................ 245 Eduardo R. Butelman and Mary Jeanne Kreek 14. Mixed Mu/Kappa Opioid Agonists ..................................................................... 257 Jean M. Bidlack and Brian I. Knapp Pharmacology of NOP Receptors 15. Medicinal Chemistry, Pharmacology, and Biological Actions of Peptide Ligands Selective for the Nociceptin/Orphanin FQ Receptor ......................... 275 Girolamo Calo' and Remo Guerrini 16. A Review of the NOP (ORL-1)-Nociceptin/Orphanin FQ System Covering Receptor Structure, Distribution, Role in Analgesia and Reward and Interactions with Other Receptors ..................................................................... 327 Garth T. Whiteside and Donald J. Kyle 17. Pharmacology of Mixed NOP/Mu Ligands ....................................................... 369 Lawrence Toll, Taline V. Khroyan, Willma E. Polgar, Stephen M. Husbands, and Nurulain T. Zaveri 18. Pharmacological Investigation of NOP-Related Ligands as Analgesics without Abuse Liability ....................................................................................... 393 Devki Sukhtankar and Mei-Chuan Ko Editors' Biographies .................................................................................................... 417 Indexes Author Index ................................................................................................................ 421 Subject Index

About the Author :
Mei-Chuan Ko is affiliated with the Department of Physiology and Pharmacology at Wake Forest University School of Medicine. Stephen M. Husbands is affiliated with the Department of Pharmacy and Pharmacology at the University of Bath.


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Product Details
  • ISBN-13: 9780841227828
  • Publisher: Oxford University Press Inc
  • Publisher Imprint: Oxford University Press Inc
  • Height: 231 mm
  • No of Pages: 440
  • Series Title: 1131 ACS Symposium Series
  • Weight: 732 gr
  • ISBN-10: 0841227829
  • Publisher Date: 09 Jan 2014
  • Binding: Hardback
  • Language: English
  • Returnable: N
  • Spine Width: 26 mm
  • Width: 159 mm


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