摘 要: | Ohmefentanyl has significant inhibitory actions on the electrically evoked contractions of guinea pigileum and mouse vas deferens. Their IC_(50) values are 0.15 nM and 0.89 nM, respectively. In the guinea pigileum and the mouse vas deferens, both μ-antagonist naloxone and (μ+κ)-antagonist Mr. 2266 antagonizereadily the agonist action of ohmefentanyl, indicating that ohmefentanyl acts on μ-receptors in the guineapig ileum and the mouse vas deferens. Like other μ-agonists, ohmefentanyl has agonist activity but noantagonist action in the rat vas deferens. In the rabbit vas deferens, the activity of ohmefentanyl is veryweak. The IC_(50) value is 149 nM. These results further indicate that ohmefentanyl is a potent and selectiveμ-agonist.
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