Targeting the oxytocin receptor to relax the myometrium.

Oxytocin acting via its receptor is involved in the myometrial hyperactivity of preterm labour and possibly also in that of primary dysmenorrhoea. The closely related hormone vasopressin acting on its uterine receptor of type V1a may also contribute to the myometrial hyperactivity of these conditions. Several pharmaceutical compounds inhibiting these receptors are, therefore, under development and one substance, atosiban, has now been registered in many countries for the treatment of preterm labour. This compound blocks both the oxytocin and the vasopressin V1a receptor. The efficacy is at least as pronounced as that of other types of drugs and side effects are much reduced. In this overview, present knowledge about receptor-mediated effects of oxytocin and vasopressin on myometrial activity is summarised. Furthermore, the therapeutic use of oxytocin and vasopressin V1a receptor antagonists in preterm labour and primary dysmenorrhoea is discussed.