Akerlund Mats
Department of Obstetrics and Gynaecology, University Hospital, SE-221 85 Lund, Sweden.
Expert Opin Ther Targets. 2006 Jun;10(3):423-7. doi: 10.1517/14728222.10.3.423.
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.
通过其受体起作用的催产素参与早产时子宫肌层的活动亢进，并且可能也参与原发性痛经时子宫肌层的活动亢进。密切相关的激素血管加压素作用于其V1a型子宫受体，也可能促成这些情况下子宫肌层的活动亢进。因此，有几种抑制这些受体的药物正在研发中，其中一种药物阿托西班现已在许多国家注册用于治疗早产。这种化合物可阻断催产素和血管加压素V1a受体。其疗效至少与其他类型药物一样显著，且副作用大大减少。在本综述中，总结了关于催产素和血管加压素对子宫肌层活动的受体介导作用的现有知识。此外，还讨论了催产素和血管加压素V1a受体拮抗剂在早产和原发性痛经治疗中的应用。
