Selective natrexone-derived opioid receptor antagonists

A. E. Takemori, Philip S Portoghese

Research output: Contribution to journalReview articlepeer-review

127 Scopus citations


Progress in opioid research relies heavily on ligands as probes to evaluate selectivity of action. The design of such ligands using naltrexone as a precursor has afforded a number of highly selective antagonists. These include the κ opioid receptor antagonist, norBNI, and δ opioid receptor antagonists, NTI and NTB. The unifying concept in the development of these antagonists was the enhancement of selectivity through simultaneous occupation of two neighboring recognition sites by a single ligand. These selective naltrexone-derived antagonists have been used widely to study the involvement of κ and δ opioid receptors in a variety of pharmacologic, physiologic, and biochemical effects.

Original languageEnglish (US)
Pages (from-to)239-269
Number of pages31
JournalAnnual review of pharmacology and toxicology
StatePublished - 1992


  • antagonists
  • delta
  • kappa
  • naltrexone
  • opioid receptors


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