Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 7, Issue 4, Pages 363-373Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/156802607779941251
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Funding
- NIDA NIH HHS [R0-1-DA14251] Funding Source: Medline
- NATIONAL INSTITUTE ON DRUG ABUSE [R01DA014251] Funding Source: NIH RePORTER
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Bivalent ligands of K opioid agonists and antagonists, such as norBNl and BNI are used as tools to elucidate the K 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 kappa/mu or mixed kappa/delta 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 K antagonist (JDTic) provides an additional tool to characterize K opioid receptor.
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