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. 1976 Nov;73(11):4215-9.
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

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

A P Feinberg et al. Proc Natl Acad Sci U S A. 1976 Nov.

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; and (iii) chemical features that afford "pure" antagonists. The model indicates mlecular mechanisms for interconversion of the opiate receptor between respective states that bind agonists or antagonists with high affinity.

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References

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