Abstract
Bivalent ligands of κ opioid agonists and antagonists, such as norBNI and BNI, are used as tools to elucidate the κ receptor characteristics. Bivalent ligands may also be effective analgesics although none have this far been used clinically. Structure-activity relationships (SAR) and molecular modeling led to the development of a more potent and selective kappa antagonist (5-guanidinylnaltrindole, GNTI). Novel homo and hetero bivalent ligands with high mixed κ/μ or mixed κ/δ affinity and intriguing pharmacological properties may eventually lead to useful analgesics with fewer adverse side effects. Bivalent ligands were also developed that could act as probes of the receptor-oligomerzation and organization phenomena. A structurally unique κ antagonist (JDTic) provides an additional tool to characterize κ opioid receptor.
Keywords: Opioid Receptor, Naltrexamine, Kappa agonists, Analgesics, KDN-21
Current Topics in Medicinal Chemistry
Title: Kappa Receptor Bivalent Ligands
Volume: 7 Issue: 4
Author(s): Xuemei Peng and John L. Neumeyer
Affiliation:
Keywords: Opioid Receptor, Naltrexamine, Kappa agonists, Analgesics, KDN-21
Abstract: Bivalent ligands of κ opioid agonists and antagonists, such as norBNI and BNI, are used as tools to elucidate the κ receptor characteristics. Bivalent ligands may also be effective analgesics although none have this far been used clinically. Structure-activity relationships (SAR) and molecular modeling led to the development of a more potent and selective kappa antagonist (5-guanidinylnaltrindole, GNTI). Novel homo and hetero bivalent ligands with high mixed κ/μ or mixed κ/δ affinity and intriguing pharmacological properties may eventually lead to useful analgesics with fewer adverse side effects. Bivalent ligands were also developed that could act as probes of the receptor-oligomerzation and organization phenomena. A structurally unique κ antagonist (JDTic) provides an additional tool to characterize κ opioid receptor.
Export Options
About this article
Cite this article as:
Peng Xuemei and Neumeyer L. John, Kappa Receptor Bivalent Ligands, Current Topics in Medicinal Chemistry 2007; 7 (4) . https://dx.doi.org/10.2174/156802607779941251
DOI https://dx.doi.org/10.2174/156802607779941251 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
- Announcements
Related Articles
-
Neurotrophin Propeptides: Biological Functions and Molecular Mechanisms
Current Protein & Peptide Science Cross Talk between the Cardiovascular and Nervous Systems:Neurotrophic Effects of Vascular Endothelial Growth Factor (VEGF) and Angiogenic Effects of Nerve Growth Factor (NGF)-Implications in Drug Development
Current Pharmaceutical Design Recent Development of Peptide Drugs and Advance on Theory and Methodology of Peptide Inhibitor Design
Medicinal Chemistry Progress in Small Molecule Therapeutics for the Treatment of Retinoblastoma
Mini-Reviews in Medicinal Chemistry Ultrasound Promoted Green Synthesis, Docking Study of Indole Spliced Thiadiazole, α-amino Phosphonates as Anticancer Agents and Antityrosinase Agents
Anti-Cancer Agents in Medicinal Chemistry BK Channel Modulators: A Comprehensive Overview
Current Medicinal Chemistry Nitric Oxide Control of MYCN Expression and Multi Drug Resistance Genes in Tumours of Neural Origin
Current Pharmaceutical Design Glutamate mGlu5-Adenosine A2A-Dopamine D2 Receptor Interactions in the Striatum. Implications for Drug Therapy in Neuro-psychiatric Disorders and Drug Abuse
Current Medicinal Chemistry - Central Nervous System Agents The Therapeutic Potential of ADAM15
Current Pharmaceutical Design Fragment Based Strategies for Discovery of Novel HIV-1 Reverse Transcriptase and Integrase Inhibitors
Current Topics in Medicinal Chemistry Polymeric Carriers for Gene Delivery: Chitosan and Poly(amidoamine) Dendrimers
Current Pharmaceutical Design Infectious Agents and Neurodegenerative Diseases: Exploring the Links
Current Topics in Medicinal Chemistry Role of Glucocorticoids in Breast Cancer
Current Pharmaceutical Design Serotonin 5-HT6 Receptor Antagonists for the Treatment of Alzheimers Disease
Current Topics in Medicinal Chemistry Targeting the Akt Kinase to Modulate Survival, Invasiveness and Drug Resistance of Cancer Cells
Current Medicinal Chemistry Cholinergic Targets in Lung Cancer
Current Pharmaceutical Design Anti-Cancer Phytometabolites Targeting Cancer Stem Cells
Current Genomics Recent Progress in FKBP Ligand Development
Current Molecular Pharmacology Effects of Vitamin A Deficiency and Opioids on Parvalbumin + Interneurons in the Hippocampus of the HIV-1 Transgenic Rat
Current HIV Research Somatostatin, Somatostatin Analogs and Somatostatin Receptor Dynamics in the Biology of Cancer Progression
Current Molecular Medicine