Oryzatensin was synthesized and its activity in longitudinal muscle strips of the guinea pig ileum was examined. DAGO, a μ-opioid agonist peptide, inhibited the electrically-induced twitches in a dose-dependent manner, and oryzatensin completely reversed the inhibition by DAGO at about 0.5 μM. However, these reversed twitches soon decreased. The profile of this anti-opioid activity of ory zatensin differed from that of naloxone, a typical opioid antagonist, which shows a long-lasting effect. Although oryzatensin showed weak affinity for μ-opioid receptors, the apparent anti-opioid activity seemed to be associated with the slower ileumcontraction. |