Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 9, Pages 2254-2258Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm061327z
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Funding
- NIDA NIH HHS [R01-DA14251, K05-DA 00360, K05 DA000360, R01 DA014251] Funding Source: Medline
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Our investigation of bivalent ligands at mu, delta, and kappa opioid receptors is focused on the preparation of ligands containing kappa agonist and mu agonist/antagonist pharmacophores at one end joined by a chain containing the mu antagonist pharmacophores (naltrexone, naloxone, or nalbuphine) at the other end. These ligands were evaluated in vitro by their binding affinity at mu, delta, and kappa opioid receptors and their relative efficacy in the [S-35]GTP gamma S assay.
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