AS604872

Names

[ Name ]:
AS604872

Biological Activity

[Description]:

AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour[1].

[Related Catalog]:

Research Areas >> Endocrinology

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

[In Vivo]

AS604872 (10-100 mg/kg, p.o.) 可以延缓 RU486 引起的早产。也可以剂量依赖性抑制 GD14 触发的分娩，在 30 mg/kg 和 100 mg/kg 的剂量下，平均分娩时间分别显着增加 16.5 和 33.5 小时。而对 GD17 引产的分娩延迟作用不太显着[1]。 AS604872 (3-120 mg/kg, i.v.) 可以以剂量依赖性方式抑制 PGF 2α 引发的磷酸肌醇的总合成，并显着降低 PGF 2α在 SD BR 非妊娠雌性大鼠中引起的子宫收缩，在 60 mg/kg 时的最大作用为 27%。同时也能够抑制孕鼠的自发性子宫收缩[1]。

[References]

[1]. Rocco Cirillo, et al. Arrest of preterm labor in rat and mouse by an oral and selective nonprostanoid antagonist of the prostaglandin F2alpha receptor (FP). Am J Obstet Gynecol. 2007 Jul;197(1):54.e1-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₈H₂₅N₃O₃S₂

[ Molecular Weight ]:
515.65

Related Compounds

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