The metabolism of [7,8-3H]azidomorphine and the in vivo stability of the azidogroup in azidomorphine and 14-hydroxyazidomorphine was studied. Asidomorphine conjugates with glucuronic acid, and is N-demethylated by rat liver microsomes. Detection by means of infrared spectroscopy proved that the azidroup in azidomorphine and 14-hydroxyazidomorphine strongly resists biotransformation in the rat.
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Azidomorphines: a new family of potent analgesics with low dependence capacity.
Prog Neuropsychopharmacol
November 1989
Department of Pharmacology, Semmelweis University of Medicine, Budapest, Hungary.
1. Structure-activity relationship studies with new semi-synthetic isomorphine derivatives revealed that substitution of an azido group in position 6 (azidomorphines) greatly increases the analgesic potency whereas tolerance and dependence liability tend to decrease. 2.
View Article and Find Full Text PDFThe metabolism of [7,8-3H]azidomorphine and the in vivo stability of the azidogroup in azidomorphine and 14-hydroxyazidomorphine was studied. Asidomorphine conjugates with glucuronic acid, and is N-demethylated by rat liver microsomes. Detection by means of infrared spectroscopy proved that the azidroup in azidomorphine and 14-hydroxyazidomorphine strongly resists biotransformation in the rat.
View Article and Find Full Text PDF6-Deoxy-6-dihydroazido-14-hydroxyisomorphine (14-hydroxyazidomorphine) was synthesized, its analgesic potency in mice and rats, its antitussive effect in rats and its dependence liability in mice, rats and monkeys were studied. Azidomorphine the 14-nonhydroxylated parent molecule, morphine, hydromorphone and oxymorphone were used for comparison. 14-Hdroxyazidomorphine proved to be as potent an analgesic as azidomorphine, even more potent as an antitussive, and showed the same low tolerance and dependence capacity.
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