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, administered at a dose range of 0.1-1 mg/kg orally as a single dose, effectively induces dose-dependent uterine contractions in pregnant rats [1]. At a single oral dose of 10 mg/kg, the compound demonstrates an AUC of 1.01 μg·h/mL and a Cmax of 0.33 μg/mL [1]. Pharmacokinetic analysis for EP3 antagonist 6 shows the following parameters: for intravenous administration at 2.7 mg/kg, the AUC is 0.89 μg·h/mL, with a half-life (t 1/2) of 0.4 hours, a total clearance (Cl tot) of 51.5 mL·min/kg, and a steady-state volume of distribution (V ss) of 1.24 L/kg. For oral administration at 10 mg/kg, the AUC is 1.01 μg·h/mL, the half-life is 1.6 hours, and the Cmax is 0.33 μg/mL, with an oral bioavailability (F) of 31% [1].