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Journal of Neuroscience, Vol 2, 572-576, Copyright © 1982 by Society for Neuroscience

ARTICLE

Irreversible opiate agonists and antagonists: the 14- hydroxydihydromorphinone azines

EF Hahn, M Carroll-Buatti and GW Pasternak

Further investigations into the molecular actions of the 14- hydroxydihydromorphinone hydrazones (naloxazone, oxymorphazone, and naltrexazone) have suggested that their irreversible actions can be explained by the formation of their azines. These azines, naloxonazine, naltrexonazine, and oxymorphonazine, irreversibly block opiate binding in vitro 20- to 40-fold more potently than their corresponding hydrozones, naloxazone, naltrexazone, and oxymorphazone. The blockade of binding by naloxonazine shows the same selectivity for high affinity, or mu1, sites as naloxazone.

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