Selective natrexone-derived opioid receptor antagonists

A. E. Takemori, Philip S Portoghese

Research output: Contribution to journalReview article

125 Scopus citations

Abstract

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
Volume32
DOIs
StatePublished - 1992

Keywords

  • antagonists
  • delta
  • kappa
  • naltrexone
  • opioid receptors

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