Kappa Receptor Bivalent Ligands

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.

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