Bossmar T, Akerlund M, Fantoni G, Szamatowicz J, Melin P, Maggi M
Department of Obstetrics and Gynecology, University Hospitals of Lund, Sweden.
Am J Obstet Gynecol. 1994 Dec;171(6):1634-42. doi: 10.1016/0002-9378(94)90415-4.
Our purpose was to study myometrial oxytocin and type V1 vasopressin receptors, the in vitro contractile effects of these hormones, and the influence of an oxytocin antagonist.
Women delivered by cesarean section preterm (n = 51) and at term (n = 71), with and without labor contractions, gave myometrium for the estimation of oxytocin and V1 vasopressin receptors. The in vitro myometrial effects of the peptides and the influence on these of the competitive oxytocin receptor blocking agent 1-deamino-2-D-Tyr(OEt)-4-Thr-8-Orn-oxytocin were also tested.
The median concentration of oxytocin receptors was 116 fmol/mg protein (range 15 to 372 fmol/mg protein) in patients delivered preterm not in labor, 134 fmol/mg protein (27 to 1421 fmol/mg protein) in the beginning of labor, and 46 fmol/mg protein (9 to 140 fmol/mg protein) in advanced labor. At term the corresponding concentrations were 172 (25 to 629), 223 (24 to 414), and 70 (21 to 92) fmol/mg protein. The concentration of V1 vasopressin receptors also decreased in advanced labor. In advanced labor after oxytocin infusion a reduction in the concentration of the receptor for this hormone was observed, which appeared to be related to the duration and dose of treatment. Oxytocin receptors did not vary between women with different indications for cesarean section. The oxytocin effects in vitro and the degree of inhibition by the antagonist of oxytocin responses correlated with the concentration of oxytocin receptors but not with that of V1 vasopressin receptors. No correlation was seen between the response to vasopressin and concentrations of oxytocin or V1 vasopressin receptors.
The effect of oxytocin on the myometrium in pregnancy is mediated by an oxytocin receptor, whereas vasopressin acts on both oxytocin and vasopressin receptors. The initiation of labor both preterm and at term may be primarily related to increased release of oxytocin, which is locally produced in the uterus and not detectable in the plasma, but oxytocin and vasopressin receptors may play a role in the regulation of labor. The analog 1-deamino-2-D-Tyr(OEt)-4-Thr-8-Orn-oxytocin, which blocks both the oxytocin and the V1 vasopressin receptor, should inhibit labor both preterm and at term, the former confirming results of recent clinical studies in Sweden and the United States.
我们的目的是研究子宫肌层的催产素和V1血管加压素受体、这些激素的体外收缩作用以及催产素拮抗剂的影响。
剖宫产分娩的早产(n = 51)和足月产(n = 71)女性,有或无宫缩,提供子宫肌层用于催产素和V1血管加压素受体的评估。还测试了肽类对子宫肌层的体外作用以及竞争性催产素受体阻断剂1-脱氨基-2-D-酪氨酸(乙酯)-4-苏氨酸-8-鸟氨酸-催产素对其的影响。
未临产的早产患者中,催产素受体的中位浓度为116 fmol/mg蛋白质(范围15至372 fmol/mg蛋白质),临产开始时为134 fmol/mg蛋白质(27至1421 fmol/mg蛋白质),产程后期为46 fmol/mg蛋白质(9至140 fmol/mg蛋白质)。足月时相应浓度分别为172(25至629)、223(24至414)和70(21至92)fmol/mg蛋白质。产程后期V1血管加压素受体浓度也降低。在产程后期输注催产素后,观察到该激素受体浓度降低,这似乎与治疗持续时间和剂量有关。剖宫产指征不同的女性之间催产素受体无差异。催产素的体外作用及拮抗剂对催产素反应的抑制程度与催产素受体浓度相关,但与V1血管加压素受体浓度无关。血管加压素反应与催产素或V1血管加压素受体浓度之间未见相关性。
催产素对妊娠子宫肌层的作用由催产素受体介导,而血管加压素作用于催产素和血管加压素受体。早产和足月分娩的启动可能主要与子宫局部产生、血浆中无法检测到的催产素释放增加有关,但催产素和血管加压素受体可能在分娩调节中起作用。同时阻断催产素和V1血管加压素受体的类似物1-脱氨基-2-D-酪氨酸(乙酯)-4-苏氨酸-8-鸟氨酸-催产素应能抑制早产和足月分娩,前者证实了瑞典和美国近期临床研究的结果。