Demarest K T, Hahn D W, Ericson E, Capetola R J, Fuchs A R, McGuire J L
R.W. Johnson Pharmaceutical Research Institute, Ortho Pharmaceutical Corporation, Raritan, New Jersey 08869.
Am J Perinatol. 1989 Apr;6(2):200-4. doi: 10.1055/s-2007-999576.
An oxytocin antagonist, 1-deamino-[D-TYR(Oethyl)2,THR4,ORN8]oxytocin (RWJ 22164; dTVT), has recently been characterized in models of uterine contractility. Studies were undertaken to characterize the action of dTVT further on both oxytocin- and vasopressin-induced increases in uterine contractility both in vitro and in situ models and in a model of preterm labor. In these studies, dTVT was found to be a specific competitive inhibitor of both oxytocin- and vasopressin-induced contractions of both pregnant and nonpregnant guinea pig uterus in vitro. In situ, the intravenous administration of dTVT induced a dose-dependent inhibition of oxytocin- and vasopressin-induced contractions in a guinea pig model which measures uterine activity as changes in uterine perfusion pressure. Further studies demonstrated that the intravenous infusion of dTVT delays ongoing labor.
一种催产素拮抗剂，1-去氨基-[D-酪氨酸（O-乙基）2，苏氨酸4，鸟氨酸8]催产素（RWJ 22164；dTVT），最近已在子宫收缩模型中得到表征。开展了研究以进一步表征dTVT在体外和原位模型以及早产模型中对催产素和血管加压素诱导的子宫收缩增加的作用。在这些研究中，发现dTVT是体外怀孕和未怀孕豚鼠子宫中催产素和血管加压素诱导收缩的特异性竞争性抑制剂。在原位，静脉注射dTVT在以子宫灌注压变化来测量子宫活动的豚鼠模型中诱导了对催产素和血管加压素诱导收缩的剂量依赖性抑制。进一步的研究表明，静脉输注dTVT可延迟正在进行的分娩。
