Abstract
Buprenorphine is a partial agonist at the μ-opioid receptor with long duration of action and also exhibits delayed antagonist activity. Buprenorphine is finding increasing use as a treatment agent for opioid abuse, though its low efficacy is not well tolerated by all addicts. There is interest in developing a higher efficacy version of buprenorphine and in this mini-review some of the ligands recently discovered, that share with buprenorphine a profile of agonism followed by delayed antagonism, are discussed.
Keywords: opioid ligands, long-term antagonistic activity, opioid abuse, buprenorphine, methadone
Mini-Reviews in Medicinal Chemistry
Title: Opioid Ligands Having Delayed Long-Term Antagonist Activity: Potential Pharmacotherapies for Opioid Abuse
Volume: 3 Issue: 2
Author(s): Stephen M. Husbands and John W. Lewis
Affiliation:
Keywords: opioid ligands, long-term antagonistic activity, opioid abuse, buprenorphine, methadone
Abstract: Buprenorphine is a partial agonist at the μ-opioid receptor with long duration of action and also exhibits delayed antagonist activity. Buprenorphine is finding increasing use as a treatment agent for opioid abuse, though its low efficacy is not well tolerated by all addicts. There is interest in developing a higher efficacy version of buprenorphine and in this mini-review some of the ligands recently discovered, that share with buprenorphine a profile of agonism followed by delayed antagonism, are discussed.
Export Options
About this article
Cite this article as:
Husbands M. Stephen and Lewis W. John, Opioid Ligands Having Delayed Long-Term Antagonist Activity: Potential Pharmacotherapies for Opioid Abuse, Mini-Reviews in Medicinal Chemistry 2003; 3 (2) . https://dx.doi.org/10.2174/1389557033405395
DOI https://dx.doi.org/10.2174/1389557033405395 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Coumarin and Derivates as Lipid Lowering Agents
Current Topics in Medicinal Chemistry Commentary (Research Highlights: The Genetic Basis of “Running for Longevity”)
CNS & Neurological Disorders - Drug Targets Thyroid Hormones and their Metabolites: Biological Roles and Association with Non-Alcoholic Fatty Liver Disease
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Oxidative Stress and Mitochondrial Dysfunction in Sepsis: A Potential Therapy with Mitochondria-Targeted Antioxidants
Infectious Disorders - Drug Targets Neuropathic Pain: Some Clues for Future Drug Treatments
Mini-Reviews in Medicinal Chemistry Review of Childhood Obesity (Balar Athidhoola Rogam) in Traditional Siddha Indian Medicine
Current Traditional Medicine MicroRNA-155 Regulates Inflammatory Response in Ischemic Cerebral Tissues through Autophagy
Current Neurovascular Research Competitive Interaction Between Plasma Omega-3 Fatty Acids and Arachidonic Acid is Related to Down-Regulation of A Signaling Mediator
Medicinal Chemistry Commentary (Research Highlights: Targeted Inhibition of miR-155 Promotes Post-Stroke Neovascularization and Functional Recovery)
CNS & Neurological Disorders - Drug Targets Determination of Mutation Pattern in Human Androgen Receptor by Means of Amino-Acid Pair Predictability
Protein & Peptide Letters Anticholinesterase and Antioxidant Activities of Spilanthes filicaulis Whole Plant Extracts for the Management of Alzheimer’s Disease
Current Enzyme Inhibition Neuroimagenomics for the Study of Human Obesity
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Voltage-gated Calcium Channels and Autism Spectrum Disorders
Current Molecular Pharmacology Basal Ganglia Enlarged Perivascular Spaces are Linked to Cognitive Function in Patients with Cerebral Small Vessel Disease
Current Neurovascular Research Pathophysiology of Post-Operative Low Cardiac Output Syndrome
Current Vascular Pharmacology The Beneficial Effect of Rice Bran Extract Against Rotenone-Induced Experimental Parkinson’s Disease in Rats
Current Molecular Pharmacology Spiro Heterocyclic Compounds as Potential Anti-Alzheimer Agents (Part 2): Their Metal Chelation Capacity, POM Analyses and DFT Studies
Medicinal Chemistry Conference Report: 9th Clinical Trials on Alzheimer's Disease (CTAD): Marriott Marquis San Diego Marina, San Diego, CA, USA December 8-10, 2016
CNS & Neurological Disorders - Drug Targets Synthetic Sphingosine 1-Phosphate Receptor Modulators - Opportunities and Potential Pitfalls
Current Topics in Medicinal Chemistry The Role of Atypical Antipsychotics in Sexuality: Road to Recovery in Schizophrenia
Current Drug Targets