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.
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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 |
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