The antagonism of narcotics by L-3-Hydroxy-N-Allylmorphinan (Levallorphan) L-3-Hydroxy-N-Propargylmorphinan (Propallorophan) and 2,4-Diamino-5-Phenylthiazole (Daptazole)

Abstract

In this study, propallorphan (a-3-hydroxy-N-propargylmorphina.n, Ro-1-7780) was found to be a potent alphaprodine to alphaprodine in both dog and man. The depression of general responsiveness (objective signs of central nervous system stimulation or depression) in conscious dogs by morphine and alphaprodine was reversed by propallorphan; while in anesthetized dogs, the changes in blood and expired gases as well as respiration brought about by alphaprodine were also antagonized by propallorphan. In another series of experiments, ratios of propallorphan to alphaprodine of 1:75 or 1:100 prevented the respiratory depression normally produced by the narcotic alone. It was also found that this antagonist reversed the respiratory depression produced by morphine; the effect lasted for a period of 30 minutes only before the opiate induced depression was reinstated. [TRUNCATED]