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  • Title: Oxymorphone-naltrexonazine, a mixed opiate agonist-antagonist.
    Author: Galetta S, Hahn EF, Nishimura S, Pasternak GW.
    Journal: Life Sci; 1987 Aug 10; 41(6):783-7. PubMed ID: 2441221.
    Abstract:
    Previous studies from our laboratories have reported the synthesis and pharmacological characteristics of a series of symmetrical opiate azines: naloxonazine, oxymorphonazine and naltrexonazine. We have now synthesized and characterized in binding assays and in vivo two asymmetrical azines: oxymorphone-naltrexonazine and oxymorphone-3-methoxynaltrexonazine. Oxymorphone-naltrexonazine, which theoretically could interact with the receptor as either an agonist or antagonist, displayed antagonist properties in vitro and in vivo. Oxymorphone-3-methoxynaltrexonazine, which theoretically could bind only as an agonist, possessed agonist properties in binding studies and was a potent analgesic in vivo.
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