A Novel Opioid Receptor Site Directed Alkylating Agent with Irreversible Narcotic Antagonistic and Reversible Agonistic Activities

Philip S. Portoghese, Dennis L. Larson, Lawrence M. Sayre, David S. Fries, A. E. Takemori

Research output: Contribution to journalArticlepeer-review

275 Scopus citations

Abstract

Sir: In 1965 the concept of multiple opioid receptors and multiple modes of interaction with a single receptor was proposed based on a detailed analysis of a broad spectrum of structure-activity relationships among analgetic ligands. The major lines of evidence for this concept were (1) the divergent stereochemical requirements for analgetic activity and (2) the different rank-order potencies among congeners, in two or more series, whose N substituent is modified in an identical manner.

Original languageEnglish (US)
Pages (from-to)233-234
Number of pages2
JournalJournal of medicinal chemistry
Volume23
Issue number3
DOIs
StatePublished - Feb 1 1980

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