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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Kappa Receptor Bivalent Ligands

Author(s): Xuemei Peng and John L. Neumeyer

Volume 7, Issue 4, 2007

Page: [363 - 373] Pages: 11

DOI: 10.2174/156802607779941251

Price: $65

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


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