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)|
|Number of pages||5|
|Journal||Proceedings of the National Academy of Sciences of the United States of America|
|State||Published - 1976|
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