The inhibitory effect of azidomorphine (AM), 14 OH azidomorphine (OAM), azidocodeine (AC) in comparison to morphine, codein, hydromorphone, oxymorphone, methadone and pethidine on the propulsion of charcoal meal in mice and on the contraction of the longitudinal muscle strip of guinea pig ileum induced by electrical stimulation or polypeptides (pentagastrin, cholecystokinin) was measured and compared to their analgetic effects. While in the hot plate test the relative potencies for morphine: hydromorphone: oxymorphone: azidomorphine: 14 OH azidomorphine: azidocodeine were found to be 1:8.8:22.3:50.0:59.0:3.5 the ratios in the charcoal meal, i.e. in inhibiting propulsive contractions of the intestine were: 1:1.9:3.3:10.0:7.3:0.44, showing that the new semisynthetic derivatives are weak inhibitors of the intestinal motility. The ability of morphine derivatives to inhibit the responses of the longitudinal muscle strip to field stimulation closely correlated with their analgesic effects measured on the hot plate test.
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