Delta-selective ligands related to naltrindole

D. J. Daniels, P. S. Portoghese

Research output: Chapter in Book/Report/Conference proceedingChapter

1 Scopus citations

Abstract

Opioid antagonists have been crucial as pharmacological tools in opioid research [1]. Historically, the ability of naloxone or naltrexone to reversibly antagonize an opioid agonist effect in an apparently competitive fashion was an important criterion for establishing the involvement of an opioid receptormediated effect. Naloxone and naltrexone are useful in this regard because they are universal antagonists; that is, they are able to antagonize the agonist effects mediated through multiple opioid receptors. However, because these ligands possess low selectivity, they are not useful for investigating the pharmacology mediated through specific opioid receptor types. Consequently, an armamentarium of highly selective opioid antagonists is now available for this purpose. Such antagonists have been invaluable for determining the selectivity of opioid ligands and opioid receptor mechanisms. In this chapter we focus on the rationale for the design of nonpeptide, deltaselective opioid antagonists related to naltrindole and their utility as pharmacological tools.

Original languageEnglish (US)
Title of host publicationThe Delta Receptor
PublisherCRC Press
Pages139-158
Number of pages20
ISBN (Electronic)9780203025765
ISBN (Print)9780824740313
StatePublished - Jan 1 2003

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ASJC Scopus subject areas

  • Neuroscience(all)
  • Health Professions(all)
  • Medicine(all)

Cite this

Daniels, D. J., & Portoghese, P. S. (2003). Delta-selective ligands related to naltrindole. In The Delta Receptor (pp. 139-158). CRC Press.