Kappa Receptor Bivalent Ligands

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

Journal Name: Current Topics in Medicinal Chemistry

Volume 7 , Issue 4 , 2007

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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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Article Details

Year: 2007
Published on: 01 March, 2012
Page: [363 - 373]
Pages: 11
DOI: 10.2174/156802607779941251
Price: $65

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