Significant advances have been made in the last 20 years in our knowledge about the subcellular events occurring during myometrial contractions and cervical ripening and in the mechanism of action of oxytocin and prostaglandins. These advances have been instrumental in furthering our understanding of the mechanism of action of inhibitors of uterine contractility and have opened the door to clinical trials of agents such as specific COX-II inhibitors that may have the potential to inhibit labor without serious maternal or fetal side effects. There is still a long way to go, however, before all the complex actions of oxytocin and prostaglandins can be understood at a subcellular level, particularly the mechanism of action of prostaglandins in the process of cervical ripening.