The opiate receptor: a model explaining structure activity relationships of opiate agonists and antagonists

A. P. Feinberg; I. Creese; S. H. Snyder

doi:10.1073/pnas.73.11.4215

The opiate receptor: a model explaining structure activity relationships of opiate agonists and antagonists

A. P. Feinberg, I. Creese, S. H. Snyder

School of Medicine

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

Abstract

A model of the opiate receptor is proposed which explains structure activity relationships of opiate drugs, including (i) the unique potency of certain opiates such as etonitazene, fentanyl, phenazocine, and oripavines; (ii) the role of N allyl substituents in conferring antagonist properties; (iii) chemical features that afford 'pure' antagonists. The model indicates molecular mechanisms for interconversion of the opiate receptor between respective states that bind agonists or antagonists with high affinity.

Original language	English (US)
Pages (from-to)	4215-4219
Number of pages	5
Journal	Proceedings of the National Academy of Sciences of the United States of America
Volume	73
Issue number	11
DOIs	https://doi.org/10.1073/pnas.73.11.4215
State	Published - 1976

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AB - A model of the opiate receptor is proposed which explains structure activity relationships of opiate drugs, including (i) the unique potency of certain opiates such as etonitazene, fentanyl, phenazocine, and oripavines; (ii) the role of N allyl substituents in conferring antagonist properties; (iii) chemical features that afford 'pure' antagonists. The model indicates molecular mechanisms for interconversion of the opiate receptor between respective states that bind agonists or antagonists with high affinity.

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The opiate receptor: a model explaining structure activity relationships of opiate agonists and antagonists

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