| 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-methoxynaltrex-onazine. 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. © 1987. |
| Keywords: |
unclassified drug; nonhuman; animal; mice; pain; animal experiment; mice, inbred icr; central nervous system; drug receptor binding; drug antagonism; brain; rat; rats; morphine; sodium; hydromorphone; analgesia; analgesic agent; naloxone; opiate receptor; naltrexone; drug interaction; oxymorphone; binding, competitive; rats, inbred strains; subcutaneous drug administration; receptors, opioid; male; priority journal; dihydromorphine; endorphins; enkephalin, leucine-2-alanine; support, non-u.s. gov't; support, u.s. gov't, p.h.s.; enkephalin, leucine; oxymorphonazine; naltrexonazine
|
