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

doi:10.1021/jm00177a002

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

Medicinal Chemistry

Research output: Contribution to journal › Article › peer-review

293 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 language	English (US)
Pages (from-to)	233-234
Number of pages	2
Journal	Journal of medicinal chemistry
Volume	23
Issue number	3
DOIs	https://doi.org/10.1021/jm00177a002
State	Published - Feb 1 1980

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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.",

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AU - Fries, David S.

AU - Takemori, A. E.

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AB - 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.

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

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