EP3 antagonist 6 (compound 5), a selective and orally active EP3 receptor antagonist, exhibits potent activity with an IC 50 of 1.9 nM. It effectively inhibits PGE2-induced uterine contractions in pregnant rats [1].

EP3:1.9 nM

EP3 antagonist 6（0.1-1 mg/kg，p.o.，单剂量）在怀孕老鼠中可有效诱导剂量依赖性的子宫收缩 [1]。单剂量10 mg/kg口服给药后，EP3 antagonist 6的AUC为1.01 μg·h/mL，Cmax为0.33 μg/mL [1]。药代动力学分析显示，EP3 antagonist 6静脉注射剂量为2.7 mg/kg时，AUC为0.89 μg·h/mL，t 1/2为0.4小时，Cl tot为51.5 mL·min/kg，V ss为1.24 L/kg；口服剂量为10 mg/kg时，AUC为1.01 μg·h/mL，t 1/2为1.6小时，C max为0.33 μg/mL，绝对生物利用度F为31% [1]。