AS604872

AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a K_i of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour^[1]. In Vivo: AS604872 (10-100 mg/kg, p.o.) delays RU486-induced preterm labour. It also dose-dependently inhibits GD14-triggered labour, with a significant increase in mean time to delivery of 16.5 and 33.5 hours at 30 mg/kg and 100 mg/kg, respectively. However, the delayed effect on GD17-induced labour is less pronounced in mice^[1].
AS604872 (3-120 mg/kg, i.v.) inhibits PGF 2α-triggered total synthesis of phosphatidylinositol in a dose-dependent manner and significantly reduces PGF 2α-induced uterine contractions in SD BR non-pregnant female rats, with a maximum effect of 27% at 60 mg/kg. It also inhibited spontaneous uterine contractions in pregnant rats^[1].