Hahn D W, Demarest K T, Ericson E, Homm R E, Capetola R J, McGuire J L
Research Laboratories, Ortho Pharmaceutical Corporation, Raritan, NJ 08869.
Am J Obstet Gynecol. 1987 Oct;157(4 Pt 1):977-82. doi: 10.1016/s0002-9378(87)80099-6.
We attempted to characterize the ability of a new oxytocin derivative, 1-deamino[D-Tyr(Oethyl)2,Thr4,Orn8] vasotocin (ORF 22164), to antagonize the action of oxytocin in several in vitro and in vivo animal models of uterine hyperactivity. In these studies, the derivative was found to be a specific competitive inhibitor of oxytocin-induced contractions of pregnant guinea pig uterus in vitro. In addition, its intravenous administration induced a dose-dependent inhibition of oxytocin-induced uterine contractions in situ. Finally, like ritodrine, the drug induced a dose-dependent delay of ongoing labor in rats. These results suggest that 1-deamino-[D-Tyr(Oethyl)2,Thr4,Orn8] vasotocin, unlike ritodrine, is a potent and specific antagonist of oxytocin-induced uterine contractions and thus may have potential clinical utility in the treatment of preterm labor.
我们试图在几种子宫活动亢进的体外和体内动物模型中，对一种新的催产素衍生物1-脱氨基[D-酪氨（O-乙基）2，苏氨酸4，鸟氨酸8]血管加压素（ORF 22164）拮抗催产素作用的能力进行表征。在这些研究中，发现该衍生物是体外催产素诱导的妊娠豚鼠子宫收缩的特异性竞争性抑制剂。此外，静脉注射该衍生物可在原位诱导对催产素诱导的子宫收缩的剂量依赖性抑制。最后，与利托君一样，该药物可诱导大鼠正在进行的分娩出现剂量依赖性延迟。这些结果表明，与利托君不同，1-脱氨基-[D-酪氨（O-乙基）2，苏氨酸4，鸟氨酸8]血管加压素是催产素诱导的子宫收缩的强效特异性拮抗剂，因此可能在早产治疗中具有潜在的临床应用价值。
