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催产素受体拮抗剂。最新进展。

Oxytocin receptor antagonists. Update.

作者信息

Goodwin T M, Zograbyan A

机构信息

Department of Obstetrics and Gynecology, University of Southern California, Women's and Children's Hospital, Los Angeles, USA.

出版信息

Clin Perinatol. 1998 Dec;25(4):859-71, vi.

PMID:9891619
Abstract

For over three decades, scientists in a number of different laboratories have worked to design peptide analogues of oxytocin (OT) selective for the oxytocin receptor. Although there has been some interest in their use for treatment of dysmenorrhea, the principal clinical venue for such agents has been thought to lie in treatment of preterm labor. A major difficulty in identifying the clinical role for an OT antagonist had been our incomplete understanding of the role of OT in both term and preterm labor. This article begins with a review of the current understanding of the role of OT in the initiation and maintenance of labor in the human.

摘要

三十多年来,许多不同实验室的科学家致力于设计对催产素受体具有选择性的催产素(OT)肽类似物。尽管人们对将其用于治疗痛经有一定兴趣,但这类药物的主要临床应用领域一直被认为是治疗早产。确定OT拮抗剂临床作用的一个主要困难在于我们对OT在足月分娩和早产中作用的理解并不完整。本文首先回顾一下目前对OT在人类分娩发动和维持过程中作用的认识。

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Isosteric substitution of Asn5 in antagonists of oxytocin and vasopressin leads to highly selective and potent oxytocin and V1a receptor antagonists: new approaches for the design of potential tocolytics for preterm labor.催产素和血管加压素拮抗剂中Asn5的等排取代导致高选择性和强效的催产素及V1a受体拮抗剂:用于早产潜在宫缩抑制剂设计的新方法。
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