2nd Department of Obstetrics and Gynecology, Aretaieio Hospital, University of Athens Medical School, 11526 Athens, Greece.
Int J Endocrinol. 2011;2011:350546. doi: 10.1155/2011/350546. Epub 2011 Dec 6.
Oxytocin, a hormone involved in numerous physiologic processes, plays a central role in the mechanisms of parturition and lactation. It acts through its receptor, which belongs to the G-protein-coupled receptor superfamily, while Gq/phospholipase C (PLC)/inositol 1,4,5-triphosphate (InsP3) is the main pathway via which it exerts its action in the myometrium. Changes in receptor levels, receptor desensitization, and locally produced oxytocin are factors that influence the effect of oxytocin on uterine contractility in labor. Activation of oxytocin receptor causes myometrial contractions by increasing intracellular Ca(+2) and production of prostaglandins. Since oxytocin induces contractions, the inhibition of its action has been a target in the management of preterm labor. Atosiban is today the only oxytocin receptor antagonist that is available as a tocolytic. However, the quest for oxytocin receptor antagonists with a better pharmacological profile has led to the synthesis of peptide and nonpeptide molecules such as barusiban, retosiban, L-368,899, and SSR-126768A. Many of these oxytocin receptor antagonists are used only as pharmacological tools, while others have tocolytic action. In this paper, we summarize the action of oxytocin and its receptor and we present an overview of the clinical and experimental data of oxytocin antagonists and their tocolytic action.
缩宫素是一种参与多种生理过程的激素，在分娩和泌乳机制中发挥着核心作用。它通过其受体发挥作用，该受体属于 G 蛋白偶联受体超家族，而 Gq/磷脂酶 C（PLC）/肌醇 1,4,5-三磷酸（InsP3）是其在子宫肌层发挥作用的主要途径。受体水平的变化、受体脱敏和局部产生的缩宫素是影响缩宫素对分娩时子宫收缩力影响的因素。缩宫素受体的激活通过增加细胞内 Ca(+2)和前列腺素的产生来引起子宫收缩。由于缩宫素诱导收缩，因此抑制其作用一直是治疗早产的目标。阿托西班是目前唯一可用作保胎药的缩宫素受体拮抗剂。然而，为了寻找具有更好药理学特性的缩宫素受体拮抗剂，人们已经合成了肽类和非肽类分子，如巴鲁昔单抗、雷托昔单抗、L-368,899 和 SSR-126768A。这些缩宫素受体拮抗剂中的许多仅用作药理学工具，而其他则具有保胎作用。本文总结了缩宫素及其受体的作用，并概述了缩宫素拮抗剂及其保胎作用的临床和实验数据。
