Narcotic antagonists. Synthesis and evaluation of some subsituted 1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines.
A seres of (+/-)-N-substituted 6-ethyl-or -methyl-8-hydroxy-1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines has been prepared from 6 hydroxytropinone. The N-cyclopropylmethyl compounds 10a and 10b were found to be strong narcotic antagonists approximately equivalent to nalorphine. Only slight analgetic activity was found in any of these compounds including the two N-methyl analogues.
D000700:Analgesics / Q000138:chemical synthesis; D000818:Animals; D001392:Azocines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D008722:Methods; D051379:Mice; D009020:Morphine / Q000037:antagonists & inhibitors; D009292:Narcotic Antagonists / Q000138:chemical synthesis* / Q000633:toxicity; D013329:Structure-Activity Relationship
D000700:Analgesics; D001392:Azocines; D009292:Narcotic Antagonists; D009020:Morphine