Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists

Research output: Contribution to journalReview article

212 Citations (Scopus)

Abstract

Metabolically stable receptor antagonists that are subtype selective are indispensable pharmacological tools. In this article, Philip Portoghese describes the bivalent ligand approach to drug design which has resulted in the development of several highly selective non-peptide opioid receptor antagonists, such as the κ-selective norbinaltorphimine and the δ-selective naltrindole. Models used resemble Schwyzer's message-address concept which originally described the recognition elements of peptide hormones; their success augurs well for the possibility of altering antagonist selectivity in a predictable fashion by simulating a portion of the address peptide component with a rigid non-peptide moiety.

Original languageEnglish (US)
Pages (from-to)230-235
Number of pages6
JournalTrends in Pharmacological Sciences
Volume10
Issue number6
DOIs
StatePublished - Jan 1 1989

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naltrindole
Narcotic Antagonists
Peptide Hormones
Drug Design
Pharmacology
Ligands
Peptides
Pharmaceutical Preparations
norbinaltorphimine

Keywords

  • Allyl-Tyr-Aib-Aib-Phe-Leu-OH
  • ICI-174868

Cite this

Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists. / Portoghese, Philip S.

In: Trends in Pharmacological Sciences, Vol. 10, No. 6, 01.01.1989, p. 230-235.

Research output: Contribution to journalReview article

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